m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03231
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[1] | |||
m6A modification
G9a
G9a
FTO
Demethylation
: m6A sites
Indirect
Enhancement
Histone modification
H3K9me2
G9a
OPRM1
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| m6A Modification: | |||||
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| m6A Regulator | Fat mass and obesity-associated protein (FTO) | ERASER | |||
| m6A Target | Histone-lysine N-methyltransferase EHMT2 (G9a) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Epigenetic Regulator | Histone-lysine N-methyltransferase EHMT2 (EHMT2) | WRITER | View Details | ||
| Regulated Target | Histone H3 lysine 9 dimethylation (H3K9me2) | View Details | |||
| Downstream Gene | OPRM1 | View Details | |||
| Crosstalk Relationship | m6A → Histone modification | Enhancement | |||
| Crosstalk Mechanism | m6A modification indirectly regulates histone modification through downstream signaling pathways | ||||
| Crosstalk Summary | Peripheral nerve injury increases the expression of the m6A demethylase fat-mass and obesity-associated proteins (FTO) in the injured DRG via the activation of Runx1, a transcription factor that binds to the Fto gene promoter. Mimicking this increase erases m6A in euchromatic Histone-lysine N-methyltransferase EHMT2 (EHMT2) mRNA (encoding the histone methyltransferase G9a) and elevates the level of G9a (regulating Histone H3 lysine 9 dimethylation (H3K9me2) level) in DRG and leads to the upregulation of OPRM1. Conversely, blocking this increase reverses a loss of m6A sites in Ehmt2 mRNA and destabilizes the nerve injury-induced G9a upregulation in the injured DRG and alleviates nerve injury-associated pain hypersensitivities. FTO contributes to neuropathic pain likely through stabilizing nerve injury-induced upregulation of G9a in a YTHDF2 dependent manner, a neuropathic pain initiator, in primary sensory neurons. | ||||
| Responsed Disease | Neuropathic pain | ICD-11: 8E43.0 | |||
| In-vivo Model | For the SNL model, after the animals were anesthetized with isoflurane, an incision on the lower back was made and the lumbar transverse process was removed. The underlying spinal nerve (L4 in mice and L5 in rats) was isolated and ligated with a 3-0 silk thread in rats or 7-0 silk thread in mice. The ligated nerve was then transected distal to the ligature. The skin and muscles were finally closed in layers. For the CCI model, unilateral exposed sciatic nerve was loosely ligated with 3-0 silk thread at four sites with an interval of about 1 mm proximal to trifurcation of the sciatic nerve. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Histone-lysine N-methyltransferase EHMT2 (EHMT2) | 7 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| MS012 | Preclinical | [2] | ||
| Synonyms |
CHEMBL4086403; 2089617-83-2 (free base); N2-hexyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine; BDBM50501525; N~2~-hexyl-6,7-dimethoxy-N~4~-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine
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| MOA | Inhibitor | |||
| External Link | ||||
| BIX-01294 | Preclinical | [3] | ||
| Synonyms |
BIX01294; BIX 01294
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| MOA | Inhibitor | |||
| Activity | IC50 = 67 nM | |||
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| A-366 | Preclinical | [4] | ||
| Synonyms |
A 366; A366
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| MOA | Inhibitor | |||
| Activity | IC50 = 3 nM | |||
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| UNC0321 | Investigative | [5] | ||
| Synonyms |
UNC-0321; UNC 0321
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| MOA | Inhibitor | |||
| Activity | IC50 = 9000 nM | |||
| External Link | ||||
| BRD9539 | Investigative | [6] | ||
| Synonyms |
BRD-9539; BRD 9539
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| MOA | Inhibitor | |||
| Activity | IC50 = 1500 nM | |||
| External Link | ||||
| UNC0642 | Investigative | [7] | ||
| Synonyms |
1481677-78-4; UNC 0642; UNC-0642; CHEMBL2441082; 2-(4,4-Difluoro-1-piperidinyl)-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine; Barrett; GTPL7017; SCHEMBL17372593; AOB2595; MolPort-035-765-953; EX-A2241; BCP08266; ZINC96285772; BDBM50442103; AKOS024458509; SB19046; CS-5269; NCGC00189140-01; NCGC00189140-02; AS-16721; HY-13980; BC600721; AK547424; UNC0642, > KB-146019; J-008448
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| MOA | Inhibitor | |||
| Activity | IC50 < 2.5 nM | |||
| External Link | ||||
| UNC0638 | Investigative | [8] | ||
| Synonyms |
1255580-76-7; UNC-0638; UNC 0638; UNII-26A103L2FO; 2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine; CHEMBL1231795; 26A103L2FO; 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine; 1255517-77-1; 2-cyclohexyl-6-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-4-amine; 2-Cyclohexyl-N-(1-isopropyl-4-piperidinyl)-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
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| MOA | Inhibitor | |||
| Activity | Ki = 3.7 nM | |||
| External Link | ||||
| Mu-type opioid receptor (OPRM1) | 511 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Propoxyphene Hydrochloride | Approved | [9] | ||
| Synonyms |
Darvon; Dolene; Kesso-gesic; Prophene 65; Propoxyphene Hydrochloride 65; Darvon-n; Propoxyphene Napsylate
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| MOA | Modulator | |||
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| Levomethadyl Acetate | Approved | [10] | ||
| Synonyms |
LAAM; Levacetilmetadol; Levacetylmethadol; Levacetylmethadolum; Levomethadyl; Orlaam; Levacetylmethadol [INN]; Levacetilmetadol [INN-Spanish]; Levacetylmethadol (INN); Levacetylmethadolum [INN-Latin]; Levo-Alphacetylmethadol; Levo-Methadyl acetate; Levomethadyl acetate (USAN); Orlaam (TN); A-l-acetylmethadol; Alpha-l-Acetylmethadol; L-alpha-Acetylmethadol; Levo-alpha-Acetylmethadol; N-alpha-Acetylmethadol; Alpha-(-)-Acetylmethadol; [(3S,6S)-6-(dimethylamino)-4,4-diphenylheptan-3-yl] acetate; [S-(R*,R*)]-beta-[2-Dimethylamino)propyl]-alpha-ethyl-beta-phenylbenzeneethanol acetate (ester); Benzeneethanol, beta-[(2S)-2-(dimethylamino)propyl]-alpha-ethyl-beta-phenyl-, acetate (ester), (alphaS)-(9CI); (-)-alpha-Acetylmethadol; (1S,4S)-4-(dimethylamino)-1-ethyl-2,2-diphenylpentyl acetate; (3S,6S)-6-(dimethylamino)-4,4-diphenylheptan-2-yl acetate; 1-alpha-Acetylmethadol; 3-Heptanol, 6-(dimethylamino)-4,4-diphenyl-, acetate (ester), (3S,6S)-(-)-(8CI)
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| MOA | Agonist | |||
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| Anileridine Hydrochloride | Approved | [11] | ||
| Synonyms |
Anileridine Phosphate; Leritine
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| MOA | Modulator | |||
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| Buprenorphine | Approved | [12] | ||
| Synonyms |
Buprel; Buprenex; Buprenophine; Buprenorfina; Buprenorphinum; Probuphine; Temgesic; Buprenorphine Hcl; RX 6029M; Buprenex (TN); Buprenorfina [INN-Spanish]; Buprenorphine [INN:BAN]; Buprenorphinum [INN-Latin]; Subutex (TN); Temgesic (TN); Buprenorphine (JAN/INN); RX-6029-M; Suboxone (TN); [5alpha,7alpha(S)]-17-(Cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-6,14-ethenomorphinan-7-methanol; (-)-buprenorphine; (5alpha,6beta,14beta,18R)-17-(cyclopropylmethyl)-18-[(1S)-1-hydroxy-1,2,2-trimethylpropyl]-6-(methyloxy)-18,19-dihydro-4,5-epoxy-6,14-ethenomorphinan-3-ol; (5alpha,6beta,14beta,18R)-17-(cyclopropylmethyl)-18-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-6-methoxy-18,19-dihydro-4,5-epoxy-6,14-ethenomorphinan-3-ol; 17-Cyclopropylmethyl-4,5alpha-epoxy-7alpha-((S)-1-hydroxy-1,2,2-trimethylpropyl-6-methoxy-6,14-endo-ethanomorphinan-3-ol; 17-cyclopropylmethyl-4,5alpha-epoxy-7alpha-((S)-1-hydroxy-1,2,2-trimethylpropyl)-6-methoxy-6,14-endo-ethanomorphinan-3-ol; 2-(N-Cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-7alpha-yl)-3,3-dimethyl-2-butanol; 2-(N-cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-6alpha-yl)-3,3-dimethyl-2-butanol; 21-(Cyclopropyl-7alpha-((S)-1-hydroxy-1,2,2-trimethylpropyl-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine; 21-cyclopropyl-7alpha-(2-hydroxy-3,3-dimethyl-2-butyl)-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine; 21-cyclopropyl-7alpha-[(S)-1-hydroxy-1,2,2-trimethylpropyl]-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine; 6,14-Ethenomorphinan-7-methanol; 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-, (alphaS,5alpha,7alpha)-(9CI); 6029-M
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| MOA | Agonist | |||
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| Naloxegol | Approved | [13] | ||
| Synonyms |
NKTR-118
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| MOA | Modulator | |||
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| Alvimopan | Approved | [14] | ||
| Synonyms |
Alvimopan anhydrous; LY 246736; LY246736; Adl 8-2698; Entereg (TN); Trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine; Glycine, N-[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl; 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid
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| MOA | Antagonist | |||
| Activity | Ki = 0.3162 nM | |||
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| Fentanyl | Approved | [15] | ||
| Synonyms |
Fentanil; Phentanyl; Fentora; Sublimaze; Fentanila; Fentanest; Duragesic; Fentanylum; Durogesic; Sentonil; 437-38-7; Duragesic-100; IONSYS; Duragesic-25; Duragesic-75; Duragesic-50; Duragesic-12; Fentanyl-25; Fentanyl-75; Fentanyl-12; Fentanyl-50; Fentanylum [INN-Latin]; Fentanila [INN-Spanish]; Fentanyl-100; 1-Phenethyl-4-N-propionylanilinopiperidine; Matrifen; Sublimase; N-(1-Phenethylpiperidin-4-yl)-N-phenylpropionamide; N-(1-Phenethyl-4-piperidyl)propionanilide; N-Phenethyl-4-(N-propionylanilino)piperidine; Fentanil [DCIT]; Subsys; Fentanyl-37; Fentanyl-62; Fentanyl-87; Abstral; Actiq; Lazanda; Onsolis; Fentanyl Citrate; Fentanyl Citrate Preservative Free; Sublimaze Preservative Free; fentanyl (transmucosal film, pain), Auxilium Pharmaceuticals
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| MOA | Modulator | |||
| Activity | EC50 = 0.51 nM | |||
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| Alfentanil | Approved | [16] | ||
| Synonyms |
Alfenta; Alfentanilum; Alfentanyl; Alfenta (TN); Alfentanil (INN); Alfentanil [INN:BAN]; Alfentanilum [INN-Latin]; Rapifen (TN); N-[1-[2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl]-4-(methoxymethyl)-4-piperidyl]propionanilide; N-[1-[2-(4-ethyl-5-oxotetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl]-N-phenylpropanamide; N-(1-(2-(4-Ethyl-4,5-dihydro-5-oxotetrazolyl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilid; N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide; N-(1-(2-(4-Ethyl-4,5-dihydro-5-oxotetrazolyl)ethyl)-4-(methoxymethyl)-4-piperidyl)-N-phenylpropionamid; N-{1-[2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl]-4-(methoxymethyl)piperidin-4-yl}-N-phenylpropanamide; N-{1-[2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl]-4-[(methyloxy)methyl]piperidin-4-yl}-N-phenylpropanamide
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| MOA | Agonist | |||
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| Methadyl Acetate | Approved | [17] | ||
| Synonyms |
ALPHACETYLMETHADOL; Acemethadone; Acetilmetadol; Acetylmethadol; Acetylmethadolum; Amidolacetate; Levamethadyl; Acetilmetadol [INN-Spanish]; Acetylmethadol (INN); Acetylmethadolum [INN-Latin]; Methadyl acetate (USAN); Methadyl acetate [USAN:BAN]; N-LAMM; Race-Acetylmethadol; [6-(dimethylamino)-4,4-diphenylheptan-3-yl] acetate; Benzeneethanol, beta-(2-(dimethylamino)propyl)-alpha-ethyl-beta-phenyl-, acetate (ester); Benzeneethanol, .beta.-[2-(dimethylamino)propyl]-.alpha.-ethyl-.beta.-phenyl-, acetate; (R,S)-4-Dimethylamino-1-ethyl-2,2-diphenylpentyl acetat; 1-Ethyl-4-dimethylamino-2,2-diphenylpentylacetat; 3-Acetoxy-6-dimethylamino-4,4-diphenylheptane; 4-(Dimethylamino)-1-ethyl-2,2-diphenylpentyl acetate; 6-(Dimethylamino)-4,4-Diphenyl-3-Heptanol Acetate
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| MOA | Agonist | |||
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| Buprenorphine + naloxone | Approved | [18] | ||
| Synonyms |
Buprenorphine/naloxone; [5 ,7 (S)]-17-(Cyclopropylmethyl)- -(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy- -methyl-6,14-ethenomorphinan-7-methanol; SCHEMBL18085614; Buprenorphine 10 mg/ml in Methanol; Buprenorphine 01 mg/ml in Methanol; ALKS5461
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| MOA | Agonist | |||
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| Diphenoxylate | Approved | [19] | ||
| Synonyms |
Difenossilato; Difenoxilato; Diphenoxalate; Diphenoxylatum; Difenossilato [DCIT]; Difenoxilato [Spanish]; Diphenoxylate HCl; Diphenoxylate Monohydrochloride; Diphenoxylate hydrochloride; Diphenoxylatum [Latin]; NIH 7562; R 1132; Difenoxilato [INN-Spanish]; Diphenoxylate (INN); Diphenoxylate [INN:BAN]; Diphenoxylate hydrochloride (USP); Diphenoxylate hydrochloride(usp); Diphenoxylatum [INN-Latin]; R 1132 (antiperistaltic); R-1132; Co-phenotrope (TN); Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylisonipecotate; Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylisonipecotate monohydrochloride; Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylate; Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylate; Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylate hydrochloride; Isonipecotic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester; Ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidin-1-ium-4-carboxylate chloride; Isonipecotic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester, hydrochloride; 1-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylic acid ethyl ester; 1-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-isonipecotic acid ethyl ester; 1-(3-Cyano-3,3-diphenylpropyl)-4-phenylisonipecotic acid ethyl ester hydrochloride; 1-(3-cyano-3,3-diphenylpropyl)-4-(ethoxycarbonyl)-4-phenylpiperidinium chloride; 2,2-Diphenyl-4-(4-carbethoxy-4-phenylpiperidino)butyronitrile; 4-Ethoxycarbonyl-alpha,alpha,4-triphenyl-1-piperidinebutyronitrile, hydrochloride; 4-Piperidinecarboxylic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester; 4-Piperidinecarboxylic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester (9CI); 4-Piperidinecarboxylic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester, monohydrochloride; 4-ethoxycarbonyl-alpha,alpha,4-triphenyl-1-piperidinebutyronitrile hydrochloride
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| MOA | Agonist | |||
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| Naldemedine Tosylate | Approved | [20] | ||
| MOA | Antagonist | |||
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| Remifentanil | Approved | [21] | ||
| Synonyms |
Remifentanyl; Ultiva; GI 87084B; GI 87084X; GI87084B; Remifentanil (INN); Remifentanil [INN:BAN]; Ultiva (TN); Methyl 1-(3-methoxy-3-oxopropyl)-4-(N-propanoylanilino)piperidine-4-carboxylate; 1-Piperidinepropanoic acid, 4-(methoxy-carbonyl)-4-((1-oxopropyl)phenylamino)-, methyl ester; 3-(4-methoxycarbonyl-4-((1-oxopropyl)phenylamino)-1-piperidine)propanoic acid methyl ester; 4-carboxy-4-(n-phenylpropionamido)-1-piperidinepropionic acid dimethyl ester
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| MOA | Agonist | |||
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| Morphine | Approved | [22] | ||
| Synonyms |
Avinza; Kadian; Morphine Sulfate; Depodur; Astramorph Pf; Duramorph Pf; Infumorph; Ms Contin; Oramorph Sr
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| MOA | Modulator | |||
| Activity | Ki = 0.14 nM | |||
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| Naloxone | Approved | [23] | ||
| Synonyms |
Nalone; Nalossone; Naloxona; Naloxonum; Narcan; Narcanti; Narcon; DBL Naloxone; Nalossone [DCIT]; Naloxone HCl; EN 1530base; DBL Naloxone (TN); L-Naloxone; N-Allylnoroxymorphone; Nalone (TN); Naloxona [INN-Spanish]; Naloxone (INN); Naloxone [INN:BAN]; Naloxonum [INN-Latin]; Narcan (TN); Narcanti (TN); N-Allyl-noroxymorphone; L-N-Allyl-14-hydroxynordihydromorphinone; L-N-Allyl-7,8-dihydro-14-hydroxynormorphinone; N-Allyl-4,5alpha-epoxy-3,14-dihydroxy-6-morphinanon; Morphinan-6-one, 17-allyl-4,5alpha-epoxy-3,14-dihydroxy-(8CI); Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, (5alpha)-(9CI); (-)-N-allyl-14-hydroxynordihydroxymorphinan-6-one; (-)-Naloxone; (5alpha)-3,14-dihydroxy-17-prop-2-en-1-yl-4,5-epoxymorphinan-6-one; (5alpha)-4,5-Epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-one; 1-N-Allyl-14-hydroxynordihydromorphinone; 1-N-Allyl-7,8-dihydro-14-hydroxynormorphinone; 12-Allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4aH-8,9c-iminoethanophenanthro(4,5-bcd)furanone; 12-Allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4aH-8,9c-iminoethanophenanthro[4,5-bcd]furan-5(6H)-one; 17-Allyl-4,5-alpha-epoxy-3,14-dihydroxymorphinan-6-one; 17-Allyl-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one; 17-allyl-3,14-dihydroxy-4,5alpha-epoxymorphinan-6-one; 3,14-dihydroxy-17-(prop-2-en-1-yl)-4,5alpha-epoxymorphinan-6-one
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| MOA | Antagonist | |||
| Activity | Ki = 0.23 nM | |||
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| Hydrocodone | Approved | [24] | ||
| Synonyms |
Dihydrocodeinone; Hydrocodon; Hydrocone; Hydroconum; Codinovo; Dicodid; Multacodin; Bekadid; hidrocodona; Idrocodone; Hydrocodonum; Idrocodone [DCIT]; DICO; (-)-Dihydrocodeinone; Hydrocodonum [INN-Latin]; 125-29-1; Hidrocodona [INN-Spanish]; Codeinone, dihydro-; Hydrocodone polistirex; Hydrocodone [INN:BAN]; UNII-6YKS4Y3WQ7; 4,5-alpha-Epoxy-3-methoxy-17-methylmorphinan-6-one; 6-Oxo-3-methoxy-N-methyl-4,5-epoxymorphinan; 4,5alpha-Epoxy-3-methoxy-17-methylmorphinan-6-one; HSDB 3097; EINECS 204-733-9; BRN 0094193; Hydrocodeinonebitartrate; Hydrocon; Anexsia (TN); Dicodid (TN); Duodin (TN); Hycet (TN); Hycodan (TN); Hycomine (TN); Hydrocodone (INN); Hydrokon (TN); Hydrovo (TN); Kolikodol (TN); Lorcet (TN); Lortab (TN); Mercodinone (TN); Norco (TN); Norgan (TN); Novahistex (TN); Orthoxycol (TN); Symtan (TN); Synkonin (TN); Vicodin (TN); Morphinan-6-one, 4,5alpha-epoxy-3-methoxy-17-methyl-(8CI); Morphinan-6-one, 4,5-epoxy-3-methoxy-17-methyl-, (5alpha)-(9CI); (5alpha)-17-methyl-3-(methyloxy)-4,5-epoxymorphinan-6-one; 3-methoxy-17-methyl-4,5alpha-epoxymorphinan-6-one; KP-201 hydrocodone prodrug
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| MOA | Modulator | |||
| Activity | Ki = 9.5 nM | |||
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| Anileridine | Approved | [25] | ||
| Synonyms |
Adopol; Alidine; Anileridina; Anileridinum; Apidol; Apodol; Leritin; Nipecotan; Anileridina [INN-Spanish]; Anileridine [INN:BAN]; Anileridinum [INN-Latin]; Leritine (TN); Anileridine (USP/INN); N-beta-(p-Aminophenyl)ethylnormeperidine; Ethyl 1-(4-aminophenethyl)-4-phenylisonipecotate; Ethyl 1-(p-aminophenethyl)-4-phenylisonipecotate; Ethyl 1-[2-(4-aminophenyl)ethyl]-4-phenylpiperidine-4-carboxylate; Isonipecotic acid, 1-(p-aminophenethyl)-4-phenyl-, ethyl ester; Ethyl 1-(2-(4-aminophenyl)ethyl)-4-phenyl-4-piperidinecarboxylate; N-(beta-(p-Aminophenyl)ethyl)-4-phenyl-4-carbethoxypiperidine; 1-(2-(4-Aminophenyl)ethyl)-4-phenyl-4-piperidinecarboxylic acid ethyl ester; 1-(p-Aminophenethyl)-4-phenylisonipecotic acid ethyl ester; 1-(p-Aminophenethyl)-4-phenylpiperidine-4-carboxylic acid ethyl ester; 1-[2-(4-Aminophenyl)ethyl]-4-phenyl-4-piperidinecarboxlic acid ethyl ester; 4-Piperidinecarboxylic acid, 1-(2-(4-aminophenyl)ethyl)-4-phenyl-, ethyl ester; 4-Piperidinecarboxylic acid, 1-[2-(4-aminophenyl)ethyl]-4-phenyl-, ethyl ester
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| MOA | Agonist | |||
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| Nalfurafine hcl | Approved | [26] | ||
| Synonyms |
Nalfurafine hydrochloride; TRK-820; Remitch; Nalfurafine (hydrochloride); 152658-17-8; UNII-25CC4N0P8J; 25CC4N0P8J; CHEMBL490665; AC 820; Nalfurafine hydrochloride [USAN:JAN]; (-)-17-(Cyclopropylmethyl)-3,14; A-dihydroxy-4,5; A-epoxy-6; A-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan Hydrochloride; (2E)-N-[(5; A)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide Hydrochloride; SCHEMBL19856501; DTXSID70426071; DJSFYNINGIMKAG-FQJQBBMWSA-N; BCP15625; Remitch (TN)
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| MOA | Inhibitor | |||
| Activity | EC50 = 1.7 nM | |||
| External Link | ||||
| Oxycodone | Approved | [27] | ||
| MOA | Modulator | |||
| Activity | Ki = 12 nM | |||
| External Link | ||||
| Methylnaltrexone bromide | Approved | [28] | ||
| Synonyms |
Relistor; Methylnaltrexone (Bromide); Naltrexone methobromide; 73232-52-7; N-Methylnaltrexone Bromide; MRZ-2663BR; N-Cyclopropylmethyl-noroxymorphone Methobromide; Methylnaltrexone; MNTX; C21H26NO4Br; MOA-728; Relistor (TN); MRZ 2663BR; Naltrexone Methyl Bromide; N-Methyl Naltrexone Bromide; MNTX-302; SCHEMBL2798188; CHEMBL1201770; IFGIYSGOEZJNBE-KNLJMPJLSA-N; ONO-3849; Methylnaltrexone bromide (JAN/USAN); 3844AH; AKOS015896214; CS-0762; AN-37324; HY-75766; Methylnaltrexone bromide, > W-5330; CHIR-01020
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| MOA | Modulator | |||
| Activity | Ki = 5.48 nM | |||
| External Link | ||||
| Hydromorphone | Approved | [29] | ||
| Synonyms |
Dihydromorphinone; Dimorphone; Idromorfone; Hydromorphon; Dihydromorfinon; Hydromorfona; Laudacon; DiMo; Hydromorphonum; 7,8-Dihydromorphinone; Novolaudon; Hidromorfona; Dilaudid; Dilaudid Oros; Hydromorfona [Spanish]; Dihydromorfinon [Czech]; 466-99-9; Hydromorphonum [INN-Latin]; Hidromorfona [INN-Spanish]; Palladone; 6-Deoxy-7,8-dihydro-6-oxomorphine; Morphinone, dihydro-; Idromorfone [DCIT]; Laudicon; Hydromorphone [INN:BAN]; Dilaudid-hp; 4,5-Epoxy-3-hydroxy-17-methylmorphinan-6-one; Hydromorphone HCL; Dilaudid (TN); Hydromorphone (INN); Palladone (TN); Palladone SR (TN); Morphinan-6-one, 4,5alpha-epoxy-3-hydroxy-17-methyl-(8CI); (-)-(5R)-4,5-Epoxy-3-hydroxy-9alpha-methylmorphinan-6-one; (-)-Hydromorphone; (5alpha)-3-hydroxy-17-methyl-4,5-epoxymorphinan-6-one; 3-hydroxy-17-methyl-4,5alpha-epoxymorphinan-6-one; 4,5alpha-Epoxy-3-hydroxy-17-methyl-6-morphinanone; Hydromorphone prodrug
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| MOA | Inhibitor | |||
| Activity | Ki = 0.28 nM | |||
| External Link | ||||
| Eluxadoline | Approved | [30] | ||
| Synonyms |
MuDelta
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| MOA | Modulator | |||
| Activity | EC50 = 1 nM | |||
| External Link | ||||
| Levopropoxyphene Napsylate Anhydrous | Approved | [11] | ||
| Synonyms |
Novrad
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| MOA | Modulator | |||
| External Link | ||||
| Tapentadol hydrochloride | Approved | [28] | ||
| Synonyms |
Tapentadol; 175591-23-8; Nucynta; Palexia; UNII-H8A007M585; 3-((1R,2R)-3-(Dimethylamino)-1-ethyl-2-methylpropyl)phenol; 3-((2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl)phenol; phenol, 3-[(1r,2r)-3-(dimethylamino)-1-ethyl-2-methylpropyl]-; BN-200; H8A007M585; CG-5503; (R,R)-Tapentadol; Tapentadol [USAN:INN]; 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol; Phenol, 3-((1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl)-; CG5503; BN 200; CG 5503; Tapentadol (USAN/INN); 3-(1-DIMETHYLAMINO-2-METHYL-PENTAN-3-YL)PHENOL
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| MOA | Modulator | |||
| External Link | ||||
| Morphine-6-glucuronide | Phase 3 | [31] | ||
| Synonyms |
Morphine 6-glucuronide; 20290-10-2; UNII-64Y9KYM60R; Morphine 6-beta-D-glucopyranosiduronide; 64Y9KYM60R; CHEBI:80581; MORPHINE GLUCURONIDE; MORPHINE 6-GLUCURONIDE(MINOR); beta-D-Glucopyranosiduronic acid, (5alpha,6alpha)-7,8-didehydro-4,5-epoxy-3-hydroxy-17-methylmorphinan-6-yl; Morphine 6-beta-D-Glucuronide; Glucopyranosiduronic acid, 7,8-didehydro-4,5-alpha-epoxy-3-hydroxy-17-methylmorphinan-6-alpha-yl-, beta-D-; Morphine glucuronide [INN]; morphine-glucuronide
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| MOA | Agonist | |||
| Activity | Ki = 12.9 nM | |||
| External Link | ||||
| GRT-6005 | Phase 3 | [32] | ||
| Synonyms |
Cebranopadol; 863513-91-1; GRT6005; UNII-7GDW9S3GN3; GRT 6005; 7GDW9S3GN3; Cebranopadol [USAN:INN]; Cebranopadol (USAN/INN); Cebranopadol(GRT-6005); SCHEMBL566256; SCHEMBL154336; GTPL8866; CHEMBL3545616; CHEMBL2364605; SCHEMBL10035739; CHEMBL3962932; SCHEMBL19336241; SCHEMBL14183935; MolPort-039-063-422; BDBM177926; ZINC3950145; EX-A1095; BCP09612; BDBM50101095; BDBM50101112; AKOS032953927; AKOS025402576; AKOS025290738; DB12830; CS-1323; SB16531; NCGC00378895-01; AK170452; HY-15536; AS-35183; Centrally-acting nociceptin agonist analgesic (oral liquid, pain/diabetic neuropathy), Grunenthal; GRT 6005/06
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| MOA | Modulator | |||
| Activity | Ki = 0.7 nM | |||
| External Link | ||||
| NKTR-181 | Phase 3 | [33] | ||
| MOA | Agonist | |||
| External Link | ||||
| TD-1211 | Phase 2 | [34] | ||
| Synonyms |
Axelopran; UNII-85U7ROB149; 85U7ROB149; 949904-48-7; Axelopran [USAN:INN]; TD 1211; SCHEMBL1773803; SCHEMBL1773801; CHEMBL3137313; AKOS027337117; SB16947; DB12013; Benzamide, 3-((3-endo)-8-(2-((cyclohexylmethyl)((2S)-2,3-dihydroxy-1-oxopropyl)amino)ethyl)-8-azabicyclo(3.2.1)oct-3-yl)-
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| MOA | Modulator | |||
| External Link | ||||
| OPNT001 | Phase 2 | [35] | ||
| MOA | Antagonist | |||
| External Link | ||||
| ALKS33 | Phase 2 | [36] | ||
| Synonyms |
Samidorphan
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| MOA | Inhibitor | |||
| Activity | Ki = 0.052 nM | |||
| External Link | ||||
| Met-enkephalin | Phase 2 | [37] | ||
| Synonyms |
H-Tyr-Gly-Gly-Phe-Met-OH; 58569-55-4; Tyr-Gly-Gly-Phe-Met-OH; METENKEFALIN; [Met]enkephalin; [5-Methionine]Enkephalin; TYR-GLY-GLY-PHE-MET; Enkephalin M; UNII-9JEZ9OD3AS; (Met5)-enkephalin; Lupex; 9JEZ9OD3AS; CHEMBL13786; CHEBI:6618; ENKEPHALIN, METHIONINE; Opioid growth factor; [Met5]-ENKEPHALIN; [Met5]Enkephalin acetate salt hydrate; Porcine beta-endorphin 1-5; (2S,5S,14S)-14-Amino-5-benzyl-15-(4-hydroxyphenyl)-2-(2-(methylthio)ethyl)-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecan-1-oic
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| MOA | Inhibitor | |||
| Activity | IC50 = 13 nM | |||
| External Link | ||||
| ORP-101 | Phase 2 | [38] | ||
| Synonyms |
1820753-68-1; 6,14-ETHENOMORPHINAN-7-METHANOL, 3,3'-(1,2-ETHANEDIYLBIS(OXY))BIS(17-(CYCLOPROPYLMETHYL)-.ALPHA.-(1,1-DIMETHYLETHYL)-4,5-EPOXY-18,19-DIHYDRO-6-METHOXY-.ALPHA.-METHYL-, (.ALPHA.S,5.ALPHA.,7.ALPHA.)-(.ALPHA.'S,5'.ALPHA.,7'.ALPHA.)-; 6,14-Ethenomorphinan-7-methanol, 3,3'-(1,2-ethanediylbis(oxy))bis(17-(cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-6-methoxy-alpha-methyl-, (alphaS,5alpha,7alpha)-(alpha'S,5'alpha,7'alpha)-; Buprenorphine dimer; CHEMBL4594402; EX-A6870; ORP-101; SCHEMBL19231198; SE6KE496VO; UNII-SE6KE496VO
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| MOA | Inhibitor | |||
| External Link | ||||
| Carfentanil | Phase 2 | [39] | ||
| Synonyms |
Carfentanyl; Carfentanila; Carfentanilum; Wildnil; 59708-52-0; Carfentanil [INN]; Carfentanila [Spanish]; UNII-LA9DTA2L8F; Carfentanilum [INN-Latin]; Carfentanila [INN-Spanish]; Methyl 1-phenylethyl-4-(N-phenylpropionamido)isonipecotate; CHEBI:61084; Methyl 4-(N-propionyl-N-phenylamino)-1-(2-phenylethyl)-4-piperidine-carboxylate; Methyl 4-(N-(1-oxopropyl)-N-phenylamino)-1-(2-phenylethyl)-4-piperidinecarboxylate; 4-((1-Oxopropyl)phenylamino)-1-(2-phenylethyl)-4-piperidinecarboxylic acid methyl ester
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| MOA | Agonist | |||
| Activity | EC50 = 0.0049 nM | |||
| External Link | ||||
| TPM-1/Morphine | Phase 2 | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Cyt-1010 | Phase 1 | [41] | ||
| MOA | Agonist | |||
| External Link | ||||
| GSK1521498 | Phase 1 | [42] | ||
| Synonyms |
GSK-1521498; GSK-1521498B
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| MOA | Agonist | |||
| External Link | ||||
| TRV734 | Phase 1 | [43] | ||
| MOA | Agonist | |||
| External Link | ||||
| NOCICEPTIN | Phase 1 | [44] | ||
| Synonyms |
Orphanin FQ; Nociceptin/orphanin FQ; 170713-75-4; Orphanin FQ (rat); Orphanin FQ (swine); Orphanin FQ (human); Nociceptin (1-17); UNII-7AYI9N34FF; Orphanin FQ (pig); 7AYI9N34FF; CHEBI:80266; Human nociceptin; L-Glutamine, L-phenylalanylglycylglycyl-L-phenylalanyl-L-threonylglycyl-L-alanyl-L-arginyl-L-lysyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-leucyl-L-alanyl-L-asparaginyl-; Nociceptin (human); Nociceptin(1-17)-OH; FGGFTGARKSARKLANQ; Orphaninfq(swine)(9ci); GTPL1681; CHEMBL396460; BDBM50004178; AKOS024458690
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| MOA | Inhibitor | |||
| Activity | Ki = 270 nM | |||
| External Link | ||||
| AIKO-150 | Phase 1 | [29] | ||
| Synonyms |
6beta-Naltrexol; beta-Naltrexol; 6beta-Hydroxynaltrexone; 6alpha-Hydroxynaltrexone; 49625-89-0; 6alpha-Naltrexol; UNII-J0W963M37T; CHEMBL140278; J0W963M37T; naltrexol; Naltrexone-6-beta-ol; alpha-Naltrexol; 6beta-Naltrexone; 6alpha-Naltrexone; 6-alpha-naltrexol; N-Cyclopropylmethyl-7,8-dihydro-14-hydroxynorisomorphine; SCHEMBL679700; DTXSID80197942; JLVNEHKORQFVQJ-PYIJOLGTSA-N; ZINC6092289; BDBM50001709; NCGC00165851-01; FT-0672600; Opioid neutral antagonists (iv, pain), Aiko Biotechnology; 6-beta-naltrexol
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| MOA | Antagonist | |||
| Activity | Ki = 0.19 nM | |||
| External Link | ||||
| MCP-201 | Phase 1 | [45] | ||
| MOA | Agonist | |||
| External Link | ||||
| SALVINORIN A | Phase 1 | [46] | ||
| Synonyms |
Salvinorin; Divinorin A; 83729-01-5; UNII-T56W91NG6J; CHEMBL445332; T56W91NG6J; CHEBI:67900; 2H-Naphtho(2,1-c)pyran-7-carboxylic acid, 9-(acetyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-, methyl ester, (2S-(2alpha,4aalpha,6abeta,7beta,9beta,10aalpha,10bbeta))-; (2S,4aR,6aR,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(3-furanyl)dodechydro-6a,10b-dimethyl-4,10-dioxo-2H-naphtho[2,1-c]pyran-7-carboxylic acid methyl ester; (-)-Salvinorin A; herbal ecstasy; Mexican mint; salvinorin-A; Salvonorin A; Diviner's S
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| MOA | Inhibitor | |||
| Activity | Ki > 1000 nM | |||
| External Link | ||||
| BCH-2687 | Discontinued in Phase 2 | [47] | ||
| MOA | Agonist | |||
| External Link | ||||
| Transdur-sufentanil | Discontinued in Phase 2 | [48] | ||
| Synonyms |
Sufentanil transdermal patch
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| MOA | Agonist | |||
| External Link | ||||
| ADL-5945 | Discontinued in Phase 2 | [49] | ||
| Synonyms |
OpRA III
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| MOA | Antagonist | |||
| External Link | ||||
| TREFENTANIL HYDROCHLORIDE | Discontinued in Phase 2 | [50] | ||
| Synonyms |
A-3665; ANQ-3665; Trefentanil hydrochloride < Rec INNM; N-[1-[2-(4-Ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl]-4-phenylpiperidin-4-yl]-N-(2-fluorophenyl)propionamide hydrochloride; 1-[2-(4-Ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl]-4-[N-(2-fluorophenyl)propionamido]-4-phenylpiperidine hydrochloride
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| MOA | Agonist | |||
| External Link | ||||
| Frakefamide | Discontinued in Phase 2 | [51] | ||
| Synonyms |
BCH-3963; LEF-553; LEF-576; SPD-759; LEF, AstraZeneca/BioChem Pharma
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| MOA | Agonist | |||
| External Link | ||||
| MIRFENTANIL HYDROCHLORIDE | Discontinued in Phase 2 | [52] | ||
| Synonyms |
A-3508 hydrochloride; ANQ-3508 HCl; Mirfentanil hydrochloride < Rec INNM; OHM-10579 (free base); N-(1-Phenethyl-4-piperidinyl)-N-(2-pyrazinyl)furan-2-carboxamide hydrochloride
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| MOA | Agonist | |||
| External Link | ||||
| DPI-3290 | Discontinued in Phase 2 | [53] | ||
| Synonyms |
DPI-3290W93; (+)-3-[1(R)-[4-Allyl-2(S),5(R)-dimethylpiperazin-1-yl]-1-(3-hydroxyphenyl)methyl]-N-(3-fluorophenyl)-N-methylbenzamide; 3290W93
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| MOA | Agonist | |||
| External Link | ||||
| Dynorphin a | Discontinued in Phase 2 | [54] | ||
| Synonyms |
80448-90-4; Dynorphin A porcine; Dynorphin-(1-17); UNII-9M18T0TD14; 9M18T0TD14; MFCD00076351; Dynorphin A1-17; Dynorphin A (swine); Dynorphin acetate; Dynorphin A (1-17), porcine; JMNJYGMAUMANNW-FIXZTSJVSA-N; BDBM50096785; AKOS024457469; Dynorphin A porcine, > NCGC00167144-01
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| MOA | Inhibitor | |||
| External Link | ||||
| ADL-7445 | Discontinued in Phase 1 | [49] | ||
| Synonyms |
Mu-opioid antagonists (opioid-induced bowel disorder), Adolor; 14-beta-aminonaltrexone
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| MOA | Antagonist | |||
| External Link | ||||
| KN-203 | Discontinued in Phase 1 | [55] | ||
| Synonyms |
Mu-opioid recceptor agonist (urinary incontinence), Grunenthal/KeyNeurotek
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| MOA | Agonist | |||
| External Link | ||||
| VP004 | Discontinued in Phase 1 | [56] | ||
| External Link | ||||
| GNTI | Preclinical | [57] | ||
| Synonyms |
G 3416; GNTI di-trifluoroacetate; Guanidinyl-naltrindole di-trifluoroacetate; 5'-Guanidinonaltrindole di(trifluoroacetate) salt hydrate; 5'-Guanidinylnaltrindole dihydrochloride
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| MOA | Antagonist | |||
| External Link | ||||
| LY-25582 | Preclinical | [58] | ||
| Synonyms |
3-[1-(3-Cyclohexyl-3-hydroxy-propyl)-3,4-dimethyl-piperidin-4-yl]-phenol; LY-255582; LY255582; CHEMBL300662; 119193-09-8; LY 255582; SCHEMBL2740453; AOB5354; (3R,4R)3-[1-(3-Cyclohexyl-3-hydroxy-propyl)-3,4-dimethyl-piperidin-4-yl]-phenol; ZINC3783617; BDBM50045775; NCGC00408804-01; AS-16869; LY255582, > 3-[(3R,4R)-1-((S)-3-Cyclohexyl-3-hydroxy-propyl)-3,4-dimethyl-piperidin-4-yl]-phenol; 3-((3R,4R)-1-((S)-3-cyclohexyl-3-hydroxypropyl)-3,4-dimethylpiperidin-4-yl)phenol; 1-Piperidinepropanol,
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| MOA | Antagonist | |||
| Activity | Ki = 0.043 nM | |||
| External Link | ||||
| 443C81 | Terminated | [59] | ||
| Synonyms |
BW 443C; BW-443C81
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| MOA | Modulator | |||
| External Link | ||||
| BCH-150 | Terminated | [60] | ||
| MOA | Modulator | |||
| External Link | ||||
| Sameridine | Terminated | [61] | ||
| Synonyms |
143257-97-0; UNII-NQP2Y50Y6B; NQP2Y50Y6B; Sameridine [INN]; sameridine[inn]; AC1Q5ICP; SCHEMBL419071; AC1L24E2; CHEMBL2104504; DTXSID30162367; 4-Piperidinecarboxamide,N-ethyl-1-hexyl-N-methyl-4-phenyl-; ZINC3797855; AKOS015909863; N-Ethyl-1-hexyl-N-methyl-4-phenylisonipecotamide; I14-31849
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| MOA | Modulator | |||
| External Link | ||||
| DBO-11 | Terminated | [31] | ||
| Synonyms |
166374-49-8; Naxifylline (USAN/INN)
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| MOA | Agonist | |||
| External Link | ||||
| DBO-17 | Terminated | [31] | ||
| MOA | Agonist | |||
| External Link | ||||
| BIPHALIN | Terminated | [62] | ||
| Synonyms |
(Tyr-ala-gly-phe-NH2)2; D-Enk-O; Dala(2); D-ENK; Bis(tyr-ala-gly-phenh2)hydrazide; CHEMBL200199; 83916-01-2; (Tyrosyl-alanyl-glycyl-phenylalaninamide)dimer; Bis(tyrosyl-alanyl-glycyl-phenylalaninamide)hydrazide; L-Phenylalanine, N-(N-(N-L-tyrosyl-D-alanyl)glycyl)-, 2-(N-(N-(N-L-tyrosyl-D-alanyl)glycyl)-L-phenylalanyl)hydrazide; enkephalin dimer; AC1NUPQ3; BDBM21014; DTXSID80232802; ZINC150345473; LS-187519; LS-186863
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| MOA | Inhibitor | |||
| Activity | EC50 = 1 nM | |||
| External Link | ||||
| SB-213698 | Terminated | [63] | ||
| Synonyms |
TAN-67
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| MOA | Inhibitor | |||
| External Link | ||||
| SNF-9007 | Terminated | [64] | ||
| Synonyms |
CHEMBL407057; BDBM21146; Asp-Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2; (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-[(3S)-3-amino-3-formamidopropanoic acid]-3-(4-hydroxyphenyl)propanamido]-3-phenylpropanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| Dmt-Sar-Phe-D-2-Nal-NH | Investigative | [65] | ||
| Synonyms |
CHEMBL254927; BDBM50232770
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| MOA | Inhibitor | |||
| External Link | ||||
| NE-2 | Investigative | [27] | ||
| MOA | Agonist | |||
| External Link | ||||
| CODEINONE | Investigative | [66] | ||
| Synonyms |
6-Codeinone; 467-13-0; UNII-22B5AW0ANN; (5alpha)-7,8-Didehydro-4,5-epoxy-3-methoxy-17-methylmorphinan-6-one; EINECS 207-386-1; BRN 0094188; 22B5AW0ANN; CHEBI:18399; 3-methoxy-17-methyl-7,8-didehydro-4,5alpha-epoxymorphinan-6-one; Morphinan-6-one, 7,8-didehydro-4,5-alpha-epoxy-3-methoxy-17-methyl-; 6-Oxocodeine; (-)-Codeinone; SCHEMBL100655; CHEMBL257627; DTXSID70196909; XYYVYLMBEZUESM-CMKMFDCUSA-N; ZINC4097036; API0000487; LS-92114; C06171; 7,8-Didehydro-4,5; A-epoxy-3-methoxy-17-methyl-morphinan-6-one
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| MOA | Inhibitor | |||
| Activity | EC50 = 294 nM | |||
| External Link | ||||
| AIKO-152 | Investigative | [27] | ||
| Synonyms |
AIKO-150 + opioid analgesic (pain/opiate dependence), Aiko Biotechnology
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| MOA | Modulator | |||
| External Link | ||||
| [Tyr-Pro-Phe-Phe-NH-]2 | Investigative | [67] | ||
| Synonyms |
CHEMBL386887
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| MOA | Inhibitor | |||
| External Link | ||||
| DC6S | Investigative | [68] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Hfe-Phe-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL378466
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| MOA | Inhibitor | |||
| External Link | ||||
| AIKO-151 | Investigative | [27] | ||
| Synonyms |
Mu-opioid antagonist (oral, opiate dependence), Aiko Biotechnology
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| MOA | Antagonist | |||
| External Link | ||||
| MM3A6S | Investigative | [68] | ||
| Synonyms |
CHEMBL379928
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| MOA | Inhibitor | |||
| External Link | ||||
| BREMAZOCINE | Investigative | [70] | ||
| Synonyms |
(-)-Bremazocine; Bremazocine, (-)-; 75684-07-0; 2-(1-Hydroxy-cyclopropylmethyl)-5-ethyl-9,9-dimethyl-2'-hydroxy-6,7-benzomorphan; 2,6-Methano-3-benzazocin-8-ol, 6-ethyl-1,2,3,4,5,6-hexahydro-3-((1-hydroxycyclopropyl)methyl)-11,11-dimethyl-, (2R)-; SureCN157210; AC1Q2C6X; SCHEMBL157210; CHEBI:3171; GTPL1603; ZINC3870315; PDSP2_001570; PDSP1_001586; C11791; UNII-ISF76M2DBE component ZDXGFIXMPOUDFF-XLIONFOSSA-N
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Hfe-Pro-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL380286
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| MOA | Inhibitor | |||
| External Link | ||||
| NCT-400 | Investigative | [27] | ||
| MOA | Modulator | |||
| External Link | ||||
| Tyr-Pro-D-(NMe)Phe-D-Pro-NH2 | Investigative | [71] | ||
| Synonyms |
CHEMBL163808
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| MOA | Inhibitor | |||
| External Link | ||||
| 6-(4-(2-(benzylamino)ethyl)phenoxy)picolinamide | Investigative | [72] | ||
| Synonyms |
CHEMBL235560; SCHEMBL3702023; JKDWSAGAQLISRL-UHFFFAOYSA-N; BDBM50219927
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| MOA | Inhibitor | |||
| Activity | Ki = 643.47 nM | |||
| External Link | ||||
| Tyr-Pro-Phe-Phg-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL378111
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| MOA | Inhibitor | |||
| External Link | ||||
| SL-3111 | Investigative | [73] | ||
| Synonyms |
CHEMBL143592; SCHEMBL9881223; BDBM50068132
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-D-Phg-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL208990
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Sar-Phe-D-2-Nal-NH2 | Investigative | [65] | ||
| Synonyms |
CHEMBL254926
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| MOA | Inhibitor | |||
| External Link | ||||
| Ac-D-pro-L-Phe-D-trp-L-Phe-NH2 | Investigative | [74] | ||
| Synonyms |
CHEMBL450818
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| MOA | Inhibitor | |||
| Activity | Ki = 340 nM | |||
| External Link | ||||
| [D-Ala2]Met-enkephalinamide | Investigative | [75] | ||
| Synonyms |
CHEMBL287480
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| MOA | Inhibitor | |||
| External Link | ||||
| ORIPAVINE | Investigative | [66] | ||
| Synonyms |
UNII-575AOU51CR; 467-04-9; EINECS 207-385-6; BRN 0046094; CHEBI:7782; 575AOU51CR; 6,7,8,14-Tetradehydro-4,5-alpha-epoxy-6-methoxy-17-methyl-morphinan-3-ol; (5alpha)-6,7,8,14-Tetradehydro-4,5-epoxy-6-methoxy-17-methylmorphinan-3-ol; Morphinan-3-ol, 6,7,8,14-tetradehydro-4,5-alpha-epoxy-6-methoxy-17-methyl-; 3-O-demethyl-thebaine; SCHEMBL37889; 4-27-00-02270 (Beilstein Handbook Reference); CHEMBL437602; DEA No. 9330; SCHEMBL19880919; DTXSID10196908; ZKLXUUYLEHCAMF-UUWFMWQGSA-N; Oripavine 0.1 mg/ml in Methanol
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| MOA | Inhibitor | |||
| Activity | EC50 = 277 nM | |||
| External Link | ||||
| YGGWL-NH2 | Investigative | [76] | ||
| Synonyms |
CHEMBL504973
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| MOA | Inhibitor | |||
| Activity | Ki = 12.1 nM | |||
| External Link | ||||
| KIN-4044 | Investigative | [27] | ||
| Synonyms |
Mu opioid antagonist (NSCLC), Kinentia
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| MOA | Antagonist | |||
| External Link | ||||
| Tyr-D-Ala-Gly-NMePhe | Investigative | [77] | ||
| Synonyms |
CHEMBL583426
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| MOA | Inhibitor | |||
| External Link | ||||
| M3B6S | Investigative | [68] | ||
| Synonyms |
CHEMBL209751
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| MOA | Inhibitor | |||
| External Link | ||||
| Endomorphins | Investigative | [27] | ||
| Synonyms |
EM-1; EM-2; Endomorphins (chronic inflammation); Endomorphin EM-1, University of Bristol; Endomorphin EM-2, University of Bristol; Endomorphins (chronic inflammation), University of Bristol
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| MOA | Modulator | |||
| External Link | ||||
| DM3A6S | Investigative | [68] | ||
| Synonyms |
CHEMBL437682
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-Hfe-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL211147
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| MOA | Inhibitor | |||
| External Link | ||||
| (+/-)-TRANS-U-50488 METHANESULFONATE | Investigative | [78] | ||
| Synonyms |
NCG-C00093883-01
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-(2-Methyl-2-aza-bicyclo[3.3.1]non-5-yl)-phenol | Investigative | [79] | ||
| Synonyms |
CHEMBL285250; 27107-68-2; CTK0I5787; DTXSID80494706; BDBM50000570; AKOS022657931; 3-(2-Methyl-2-azabicyclo[3.3.1]nonan-5-yl)phenol; Phenol, 3-(2-methyl-2-azabicyclo[3.3.1]non-5-yl)-; 2-Methyl-5-(3-hydroxyphenyl)-2-azabicyclo[3.3.1]nonane
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| MOA | Inhibitor | |||
| External Link | ||||
| AKUAMMINE | Investigative | [78] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Semorphone | Investigative | [80] | ||
| Synonyms |
(-)-4,5alpha-Epoxy-3,14-dihydroxy-17-(2-methoxyethyl)morphinan-6-one hydrochloride; (-)-4,5alpha-Epoxy-3,14-dihydroxy-N-(2-methoxyethyl)morphinan-6-one hydrochloride; MR-2264 (free base); MRZ-2264 (free base); N-(2-Methoxyethyl)noroxymorphone hydrochloride; Semorphone hydrochloride
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| MOA | Modulator | |||
| External Link | ||||
| YGWFL-NH2 | Investigative | [76] | ||
| Synonyms |
CHEMBL455502
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| MOA | Inhibitor | |||
| Activity | Ki = 112.5 nM | |||
| External Link | ||||
| YRFB | Investigative | [81] | ||
| Synonyms |
CHEMBL215513
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| MOA | Inhibitor | |||
| External Link | ||||
| NRT-300 | Investigative | [27] | ||
| Synonyms |
NCT-300
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| MOA | Modulator | |||
| External Link | ||||
| H-Tyr-D-Ala-(R or S)Atc-Asp-Val-Val-Gly-NH2 | Investigative | [82] | ||
| Synonyms |
CHEMBL124941; BDBM50001459; 3-[(2-{2-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-N-{1-[1-(carbamoylmethyl-carbamoyl)-2-methyl-propylcarbamoyl]-2-methyl-propyl}-succinamic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phg-Pro-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL425421
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| MOA | Inhibitor | |||
| External Link | ||||
| C6S | Investigative | [68] | ||
| Synonyms |
CHEMBL1417
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-D-2-Nal-NH2 | Investigative | [65] | ||
| Synonyms |
CHEMBL375070
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| MOA | Inhibitor | |||
| Activity | Ki > 1000 nM | |||
| External Link | ||||
| Tyr-D-Ala-Phe-Thr[-D-Glc(OAc)4]-Tyr-Pro-Ser-NH2 | Investigative | [83] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-D-Ala-Bn | Investigative | [84] | ||
| Synonyms |
CHEMBL577748
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| MOA | Inhibitor | |||
| Activity | Ki = 8.67 nM | |||
| External Link | ||||
| naloxonazine | Investigative | [85] | ||
| Synonyms |
NSC 612113
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| MOA | Antagonist | |||
| Activity | Ki = 1.445 nM | |||
| External Link | ||||
| Tyr-Pro-Phg-Phe-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL211119
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| MOA | Inhibitor | |||
| External Link | ||||
| KNT-5 | Investigative | [86] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| N-alpha-amidino-Tyr(Me)-D-Pro-Gly-Trp-Phe-NH2 | Investigative | [87] | ||
| Synonyms |
CHEMBL243724; BDBM50201411; N alpha-amidino-Tyr(Me)-D-Pro-Gly-Trp-Phe-NH2
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| MOA | Inhibitor | |||
| External Link | ||||
| Ac-L-Phe-D-trp-L-Phe-D-pro-NH2 | Investigative | [74] | ||
| Synonyms |
CHEMBL442612
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| MOA | Inhibitor | |||
| Activity | Ki = 360 nM | |||
| External Link | ||||
| DM3B6S | Investigative | [68] | ||
| Synonyms |
CHEMBL213737
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-Ala-Bn | Investigative | [84] | ||
| Synonyms |
CHEMBL577749
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| MOA | Inhibitor | |||
| Activity | Ki = 122 nM | |||
| External Link | ||||
| YPAA-NH2 | Investigative | [76] | ||
| Synonyms |
CHEMBL466147
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| MOA | Inhibitor | |||
| Activity | Ki = 705 nM | |||
| External Link | ||||
| KIN-3031 | Investigative | [27] | ||
| Synonyms |
Mu opioid angonist (CNS formulation, pain), Kinentia
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| MOA | Modulator | |||
| External Link | ||||
| Tyr-Pro-Phe-D-Val-Bn | Investigative | [84] | ||
| Synonyms |
CHEMBL577746
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| MOA | Inhibitor | |||
| Activity | Ki = 4.97 nM | |||
| External Link | ||||
| [Tyr-Pro-Phe-NH-CH2-]2 | Investigative | [67] | ||
| Synonyms |
CHEMBL180286
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| MOA | Inhibitor | |||
| External Link | ||||
| YAWF-NH2 | Investigative | [76] | ||
| Synonyms |
CHEMBL445690
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| MOA | Inhibitor | |||
| Activity | Ki = 3190 nM | |||
| External Link | ||||
| Tyr-Pro-Trp-D-Val-Bn | Investigative | [84] | ||
| Synonyms |
CHEMBL577745
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| MOA | Inhibitor | |||
| Activity | Ki = 2.32 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Tic-Asp-Val-Val-Gly-NH2 | Investigative | [82] | ||
| Synonyms |
CHEMBL330991; BDBM50001460; 3-[(2-{2-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-propionyl}-1,2,3,4-tetrahydro-isoquinoline-3-carbonyl)-amino]-N-{1-[1-(carbamoylmethyl-carbamoyl)-2-methyl-propylcarbamoyl]-2-methyl-propyl}-succinamic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| YPWA-NH2 | Investigative | [76] | ||
| Synonyms |
CHEMBL512955
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| MOA | Inhibitor | |||
| Activity | Ki = 72.7 nM | |||
| External Link | ||||
| Ethylmorphine | Investigative | [88] | ||
| Synonyms |
Codethyline; DIONINE; 76-58-4; Morphine, ethyl-; Ethyl morphine; UNII-RWO67D87EU; Ethylmorphine [BAN]; 3-O-Ethylmorphine; EINECS 200-970-7; RWO67D87EU; CHEBI:4902; DEA No. 9190; Dionin; Ethylmorphine (BAN); NCGC00168251-01; Ethomorphine; Morphinan-6-alpha-ol, 7,8-didehydro-4,5-alpha-epoxy-3-ethoxy-17-methyl-; (4R,4aR,7S,7aR,12bS)-9-ethoxy-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-ol; Morphine 3-ethyl ether; AC1Q37UW; Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-ethoxy-17-methyl-
Click to Show/Hide
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| MOA | Agonist | |||
| External Link | ||||
| THEBAINE | Investigative | [66] | ||
| Synonyms |
Paramorphine; 3-O-Methyl-oripavin; 115-37-7; UNII-2P9MKG8GX7; Thebain; 4,5alpha-Epoxy-3,6-dimethoxy-17-methyl-6,8-morphinadien; EINECS 204-084-1; 2P9MKG8GX7; (5R,9R,13S)-4,5-Epoxy-3,6-dimethoxy-9alpha-methyl-6,8-morphinadien; CHEBI:9519; DEA No. 9333; NCGC00160239-01; DSSTox_RID_81337; DSSTox_CID_26099; DSSTox_GSID_46099; Morphinan, 6,7,8,14-tetradehydro-4,5-alpha-epoxy-3,6-dimethoxy-17-methyl-; 3,6-dimethoxy-17-methyl-6,7,8,14-tetradehydro-4,5alpha-epoxymorphinan
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | EC50 = 5600 nM | |||
| External Link | ||||
| [Tyr-Pro-Phe-Phe-NH-CH2-]2 | Investigative | [67] | ||
| Synonyms |
CHEMBL409336
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| MOA | Inhibitor | |||
| External Link | ||||
| Ac-YGGFL-NH2 | Investigative | [76] | ||
| Synonyms |
CHEMBL500212
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| MOA | Inhibitor | |||
| Activity | Ki = 37.3 nM | |||
| External Link | ||||
| Tyr-(R)-spiro-Aba-Gly-Phe-NH2 | Investigative | [89] | ||
| Synonyms |
CHEMBL401142
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| MOA | Inhibitor | |||
| External Link | ||||
| D-Phe-Cys-Tyr--Trp-Lys-Thr-Pen-Thr-NH2 | Investigative | [90] | ||
| Synonyms |
CHEMBL274400
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| MOA | Inhibitor | |||
| External Link | ||||
| MORPHICEPTIN | Investigative | [91] | ||
| Synonyms |
Deproceptin; Tyr-pro-phe-pro amide; Tyr-pro-phe-D-pro-NH2; beta-Casomorphine(1-4) amide; NH(4)-Tyr-pro-phe-pro-conh(2); Tyr-Pro-Phe-Pro-NH2; Tyrosyl-prolyl-phenylalanyl-D-prolinamide; UNII-97TZA8ANPC; H-Tyr-Pro-Phe-Pro-NH2; L-Tyrosyl-L-prolyl-L-phenylalanyl-L-prolinamide; 74135-04-9; b-Casomorphin-4-amide; 97TZA8ANPC; CHEMBL362991; L-Prolinamide, L-tyrosyl-L-prolyl-L-phenylalanyl-
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| MOA | Inhibitor | |||
| Activity | Ki = 150 nM | |||
| External Link | ||||
| DIHYDROAKUAMMINE | Investigative | [78] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 6-(2-benzylisoindolin-5-yloxy)nicotinamide | Investigative | [58] | ||
| Synonyms |
CHEMBL238362; SCHEMBL3690327; GGVSFVBTUMOASO-UHFFFAOYSA-N; BDBM50226248
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| MOA | Inhibitor | |||
| Activity | Ki = 1008 nM | |||
| External Link | ||||
| Tyr-Pro-Trp-Gly-Bn | Investigative | [84] | ||
| Synonyms |
CHEMBL570634
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| MOA | Inhibitor | |||
| Activity | Ki = 56.23 nM | |||
| External Link | ||||
| CYPRODIME | Investigative | [92] | ||
| Synonyms |
CHEMBL322796; N-(Cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one; SCHEMBL3619261; BDBM50148071; ZINC13580323; NCGC00344512-01; Morphinan-6-one, 17-(cyclopropylmethyl)-4,14-dimethoxy-; (-)-N-(Cycloproylmethyl)-4,14-dimethoxymorphinan-6-one(Cyprodime); 17-cyclopropylmethyl-3,10-dimethoxy-(1R,9R,10S)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-13-one; 17-cyclopropylmethyl-10-hydroxy-4,14-dimethoxy-(1S,9R,10S)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3-dien-6-one(cyprodime)
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| MOA | Inhibitor | |||
| Activity | Ki = 10.6 nM | |||
| External Link | ||||
| MORPHINONE | Investigative | [66] | ||
| Synonyms |
467-02-7; UNII-28MBK63MAW; EINECS 207-384-0; BRN 0042464; 28MBK63MAW; Didehydro-4,5-alpha-epoxy-3-hydroxy-17-methylmorphinan-6-one; CHEBI:16315; (5alpha)-7,8-Didehydro-4,5-epoxy-3-hydroxy-17-methylmorphinan-6-one; Morphinan-6-one, 7,8-didehydro-4,5-epoxy-3-hydroxy-17-methyl-, (5-alpha)-; SCHEMBL427946; CHEMBL255467; CTK1D7902; DTXSID50196907; ZINC4095712; AKOS030240636; LS-92113; C01735; 3-hydroxy-17-methyl-7,8-didehydro-4,5-epoxy-5alpha-morphinan-6-one
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| MOA | Inhibitor | |||
| Activity | EC50 = 28 nM | |||
| External Link | ||||
| PL017 | Investigative | [93] | ||
| Synonyms |
3-N-Me-Phe-morphiceptin; PL-017; PL 017
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| MOA | Agonist | |||
| External Link | ||||
| ADC-5510 | Investigative | [27] | ||
| Synonyms |
ADC-02265510; ADL-5510; Centrally acting mu opoid receptor antagonists, Adolor
Click to Show/Hide
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| MOA | Antagonist | |||
| External Link | ||||
| MM3B6S | Investigative | [68] | ||
| Synonyms |
CHEMBL211374
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| MOA | Inhibitor | |||
| External Link | ||||
| M3S | Investigative | [68] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Trp-D-Ala-Bn | Investigative | [84] | ||
| Synonyms |
CHEMBL577747
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| MOA | Inhibitor | |||
| Activity | Ki = 4.56 nM | |||
| External Link | ||||
| Beta-funaltrexamine | Investigative | [77] | ||
| Synonyms |
beta-Fna; Naltrexone fumarate methyl ester; 72782-05-9; CHEMBL473136; CHEBI:81527; 2-Butenoic acid, 4-(((5alpha,6beta)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl)amino)-4-oxo-, methyl ester, (E)-; Beta Funaltrexamine; Beta-Funeltrexamine; SCHEMBL1240811; GTPL1631; ZINC3995756; PDSP2_001549; PDSP2_000394; BDBM50247803; NCGC00163180-01; LS-47116; C18127; methyl 3-[4-cyclopropylmethyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-ylcarbamoyl]-
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.41 nM | |||
| External Link | ||||
| KRP-110 | Investigative | [27] | ||
| Synonyms |
IDDBCP262221
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| MOA | Modulator | |||
| External Link | ||||
| H-Tyr-D-Ala-Aic-Asp-Val-Val-Gly-NH2 | Investigative | [82] | ||
| Synonyms |
CHEMBL124435; BDBM50001462; 3-[(2-{2-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-indane-2-carbonyl)-amino]-N-{1-[1-(carbamoylmethyl-carbamoyl)-2-methyl-propylcarbamoyl]-2-methyl-propyl}-succinamic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| KRP-100 | Investigative | [27] | ||
| Synonyms |
Mu opioid receptor antagonist, Kyorin
Click to Show/Hide
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| MOA | Antagonist | |||
| External Link | ||||
| [Tyr-Pro-Phe-NH-]2 | Investigative | [67] | ||
| Synonyms |
CHEMBL179946
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Aba-ser-Gly-Phe-Leu-Thr-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL246479
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 640 nM | |||
| External Link | ||||
| Tyr-(R)-Aba-Gly-Phe-NH2 | Investigative | [89] | ||
| Synonyms |
CHEMBL250448
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Lys-NH-Ph | Investigative | [94] | ||
| Synonyms |
SCHEMBL8224099
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Gly-NH-CH2-Bid | Investigative | [95] | ||
| Synonyms |
(3S)-N-[(1H-Benzimidazole-2-ylmethyl)carbamoylmethyl]-2-[(S)-3-(2,6-dimethyl-4-hydroxyphenyl)-2-aminopropionyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-D-Asp-N(Me)-Ph | Investigative | [96] | ||
| Synonyms |
CHEMBL502302
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid | Investigative | [96] | ||
| Synonyms |
CHEMBL444197
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) | Investigative | [97] | ||
| Synonyms |
CHEMBL208916
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-D-Phe-Pro-NH2 | Investigative | [71] | ||
| Synonyms |
CHEMBL162564
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| MOA | Inhibitor | |||
| External Link | ||||
| H-mCpa-ala-Gly-Phe-leu-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL246682
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| MOA | Inhibitor | |||
| Activity | Ki = 560 nM | |||
| External Link | ||||
| H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 | Investigative | [98] | ||
| Synonyms |
CHEMBL371856
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH | Investigative | [98] | ||
| Synonyms |
CHEMBL370701
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Aba-ala-Gly-Phe-Met-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL246572
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| MOA | Inhibitor | |||
| Activity | Ki = 100 nM | |||
| External Link | ||||
| Tyr-D-Ala-Gly-Phe-Met-NH2 | Investigative | [62] | ||
| Synonyms |
Tyr-DAla-Gly-Phe-Met-NH2
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-3,5Dmp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL413892
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH2-CH2-NH2 | Investigative | [100] | ||
| Synonyms |
CHEMBL241010
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| MOA | Inhibitor | |||
| External Link | ||||
| Ac-RYYRIK-GGG-K-(NH2)-YRFB-GGGGG | Investigative | [81] | ||
| Synonyms |
CHEMBL441930
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-Phe-OCH2CH3 | Investigative | [101] | ||
| Synonyms |
CHEMBL505502
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| MOA | Inhibitor | |||
| External Link | ||||
| N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 | Investigative | [87] | ||
| Synonyms |
CHEMBL243189; BDBM50201412; N alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2
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| MOA | Inhibitor | |||
| External Link | ||||
| (H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) | Investigative | [97] | ||
| Synonyms |
CHEMBL426320
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-c[D-Orn-Aic-Glu]-NH2 | Investigative | [102] | ||
| Synonyms |
CHEMBL106849
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| MOA | Inhibitor | |||
| External Link | ||||
| 3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone | Investigative | [103] | ||
| Synonyms |
CHEMBL200890
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-Benzylaminomethyl-3-hydroxymorphinan | Investigative | [104] | ||
| Synonyms |
CHEMBL578173
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| MOA | Inhibitor | |||
| Activity | Ki = 190 nM | |||
| External Link | ||||
| PTI-601 | Investigative | [27] | ||
| MOA | Modulator | |||
| External Link | ||||
| M6S | Investigative | [68] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Antanal 1 | Investigative | [105] | ||
| Synonyms |
CHEMBL507442
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| MOA | Inhibitor | |||
| External Link | ||||
| KETOCYCLAZOCINE | Investigative | [106] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| UFP-502 | Investigative | [107] | ||
| Synonyms |
CHEMBL109390; H-Dmt-Tic-NH-CH2-Bid; 2-[2-Amino-3-(4-hydroxy-2,6-dimethyl-phenyl)-propionyl]-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid (1H-benzoimidazol-2-ylmethyl)-amide; BDBM50179191; (S)-N-((1H-benzo[d]imidazol-2-yl)methyl)-2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-D-Asp-NH-Ph | Investigative | [96] | ||
| Synonyms |
CHEMBL498799
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| MOA | Inhibitor | |||
| External Link | ||||
| Dimethylthiambutene | Investigative | [108] | ||
| Synonyms |
Dimethibutin; Ohton; Dimetiltiambuteno; Aminobutene; Dimethylthiambutenum; Kobaton; N,N,1-Trimethyl-3,3-di-2-thienylallylamine; 3-Dimethylamino-1,1-bis(2-thienyl)-1-butene; 524-84-5; 3-Dimethylamino-1,1-di-(2'-thienyl)-1-butene; Dimetiltiambutene [DCIT]; N,N,1-Trimethyl-3,3-di(2-thienyl)-2-propenylamine; Dimetiltiambuteno [INN-Spanish]; Dimethylthiambutenum [INN-Latin]; Dimethylthiambutene [INN:BAN:DCF]; 338C48; Allylamine, N,N,1-trimethyl-3,3-di-2-thienyl-; BRN 0084891; DEA No. 9619; CHEBI:59781; NIH4542
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| MOA | Agonist | |||
| External Link | ||||
| H-Dmt-Tic-Asp-NH-Bzl | Investigative | [96] | ||
| Synonyms |
CHEMBL450566
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| MOA | Inhibitor | |||
| External Link | ||||
| Etorphine | Investigative | [109] | ||
| Synonyms |
19-Propylorvinol; 6,14-Ethenomorphinan-7-methanol, 4,5-epoxy-3-hydroxy-6-methoxy-.alpha.,17-dimethyl-.alpha.-propyl-, [5.alpha.,7.alpha.(R)]-; 7.alpha.-Etorphine; AC1LARGT; ETORPHINE - HCI; GTPL1625; SCHEMBL10031275; Oripavine, 6,14-endo-ethylenetetrahydro-7-(1-hydroxy-1-methylbutyl)-; BDBM82425; CAHCBJPUTCKATP-UHFFFAOYSA-N; M99; CAS_61677; NSC_61677; FT-0668440; L024016; Tetrahydro-7-.alpha.-(1-hydroxy-1-methylbutyl)-6,14-endo-ethenooripavine; 6,14-endo-Ethenotetrahydrooripavine, 7.alpha.-(1-hydroxy-1-methylbuty
Click to Show/Hide
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| MOA | Agonist | |||
| External Link | ||||
| H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H | Investigative | [100] | ||
| Synonyms |
CHEMBL392469
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-L-Phe-Pro-NH2 | Investigative | [71] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 | Investigative | [83] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Dmt-Pro-Trp-D-2-Nal-NH2 | Investigative | [110] | ||
| Synonyms |
CHEMBL218433
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-Tic-Phe-Phe-OH | Investigative | [111] | ||
| Synonyms |
Tyrosyl-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-phenylalanyl-phenylalanine; TIPP; 146369-65-5; Tyr-tic-phe-phe-OH; CHEMBL191751; L-Phenylalanine, L-tyrosyl-L-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-phenylalanyl-; Tyr-Tic-Phe-PheOH; AC1LD8RR; TIPP (opioid antagonist); DTXSID60163362; ZINC3942635; BDBM50068664; tyrosyl-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl- phenylalanyl-phenylalanine; L-Tyrosyl-L-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L- phenylalanyl-L-phenylalanine; 147780-77-6
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| MOA | Inhibitor | |||
| Activity | Ki > 4500 nM | |||
| External Link | ||||
| 6-(2-phenethylisoindolin-5-yloxy)nicotinamide | Investigative | [58] | ||
| Synonyms |
CHEMBL235154; SCHEMBL3696847
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| MOA | Inhibitor | |||
| Activity | Ki = 658.8 nM | |||
| External Link | ||||
| UFP-512 | Investigative | [107] | ||
| Synonyms |
CHEMBL442577; GTPL9006; BDBM50272169; H-Dmt-Tic-NH-CH(CH2-COOH)-Bid; H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid; (3S)-3-[[(3S)-2-[(2S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]3,4-dihydro-1H-isoquinoline-3-carbonyl]amino]-3-(1H-benzimidazol-2-yl)propanoic acid; (S)-3-((S)-2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamido)-3-(1H-benzo[d]imidazol-2-yl)propanoic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| SPIROINDANYLOXYMORPHONE | Investigative | [112] | ||
| Synonyms |
7-Spiroindanyloxymorphone; SIOM; 7-(Spiroindano)Oxymorphone; CHEMBL399708; 150380-34-0; SCHEMBL12013205; 7-(2'-spiroindanyl)oxymorphone; 7-(2''-spiroindanyl)oxymorphone; BDBM50297170; 1',3',7,7a,8,9-Hexahydro-3,7a-dihydroxy-12-methylspiro(6H-8,9c-(iminoethano)phenanthro(4,5-bcd)furan-6,2'-(2H)inden)-5(4aH)-one (4aR-(4aalpha,7aalpha,8alpha,9calpha))-; Spiro(6H-8,9c-(iminoethano)phenanthro(4,5-bcd)furan-6,2'-(2H)inden)-5(4aH)-one, 1',3',7,7a,8,9-hexahydro-3,7a-dihydroxy-12-methyl-, (4aR-(4aalpha
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 14.3 nM | |||
| External Link | ||||
| Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 | Investigative | [71] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Gly-N(Me)-Ph | Investigative | [96] | ||
| Synonyms |
CHEMBL500937
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H | Investigative | [113] | ||
| Synonyms |
CHEMBL375359
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH | Investigative | [111] | ||
| Synonyms |
CHEMBL375094
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| MOA | Inhibitor | |||
| External Link | ||||
| NalBzOH | Investigative | [68] | ||
| Synonyms |
Naloxone benzoylhydrazone; 119630-94-3; 6-Desoxy-6-benzoylhydrazido-N-allyl-14-hydroxydihydronormorphinone; Benzoic acid, ((5alpha)-4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-ylidene)hydrazide; Lopac0_000882; [(5alpha)-4,5-Epoxy-; MLS000860072; Naloxone benzoylhydrazone, solid; SCHEMBL15423902; CHEMBL1256836; MolPort-003-958-927; MFCD05662358; AKOS024456586; CCG-204964; NCGC00092281-03; NCGC00092281-02; NCGC00092281-04; NCGC00092281-01; SMR000326930; N-165; EU-0100882; SR-01000075513; SR-01000075513-1
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| MOA | Inhibitor | |||
| External Link | ||||
| CTAP | Investigative | [93] | ||
| MOA | Antagonist | |||
| External Link | ||||
| Leucine-enkephalin | Investigative | [114] | ||
| Synonyms |
YGGFL; URLZCHNOLZSCCA-UHFFFAOYSA-N; 2-[[2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid; Spectrum_001429; AC1L1GYW; Spectrum5_000656; Spectrum4_001048; Spectrum2_001177; Spectrum3_001521; AC1Q1P3H; KBioSS_001909; KBioGR_001316; BSPBio_002902
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| MOA | Inhibitor | |||
| Activity | EC50 = 1.3 nM | |||
| External Link | ||||
| MCL-457 | Investigative | [115] | ||
| Synonyms |
CHEMBL242967; BDBM50210558
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| MOA | Inhibitor | |||
| Activity | Ki = 160 nM | |||
| External Link | ||||
| DADLE | Investigative | [116] | ||
| Synonyms |
63631-40-3; H-TYR-D-ALA-GLY-PHE-D-LEU-OH; DADL; (D-Ala2,D-Leu5)-Enkephalin; [D-Ala2, D-Leu5]-enkephalin; CHEMBL340032; BW-180C; Tyr-D-Ala-Gly-Phe-D-Leu; (2R,5S,11R,14S)-14-Amino-5-benzyl-15-(4-hydroxyphenyl)-2-isobutyl-11-methyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazapentadecan-1-oic acid; (2R)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid; UNII-HB4QD9GL6F; HB4QD9GL6F; DADLE-OH; AC1OCEJN; ZINC14952092; H-Tyr-D-Ala-Gly-Phe-D-Leu
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| MOA | Inhibitor | |||
| Activity | EC50 = 128.82 nM | |||
| External Link | ||||
| H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Investigative | [117] | ||
| Synonyms |
CHEMBL384571
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Investigative | [118] | ||
| Synonyms |
CHEMBL208801
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| MOA | Inhibitor | |||
| Activity | Ki > 10000 nM | |||
| External Link | ||||
| Tyr-Pro-Dmt-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL228512
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 | Investigative | [102] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 | Investigative | [119] | ||
| Synonyms |
CHEMBL29078; Tyr-Ala-Phe-Asp-Val-Val-Gly; GTPL1615
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Aba-Gly-Gly-Phe-Leu-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL247759
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| MOA | Inhibitor | |||
| Activity | Ki = 1200 nM | |||
| External Link | ||||
| Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 | Investigative | [119] | ||
| Synonyms |
CHEMBL32202; BDBM50009180; 3-(2-{2-[2-(2-{2-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-4-methylsulfanyl-butyrylamino}-3-phenyl-propionylamino)-3-(1H-imidazol-4-yl)-propionylamino]-4-methyl-pentanoylamino}-4-methylsulfanyl-butyrylamino)-succinamic ac
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| MOA | Inhibitor | |||
| External Link | ||||
| C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL506211
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| MOA | Inhibitor | |||
| Activity | Ki = 43 nM | |||
| External Link | ||||
| D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) | Investigative | [90] | ||
| Synonyms |
CHEMBL413950
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| MOA | Inhibitor | |||
| External Link | ||||
| N-isobutylnoroxymorphone | Investigative | [120] | ||
| Synonyms |
CHEMBL490418; 17-Isobutyl-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one; SCHEMBL3835355; OEQLILQNMUXCHV-XFWGSAIBSA-N
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H | Investigative | [121] | ||
| Synonyms |
CHEMBL372130
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| MOA | Inhibitor | |||
| External Link | ||||
| 1,10-bis-(Dmt-Tic-amino)decane | Investigative | [103] | ||
| Synonyms |
CHEMBL373192
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH2-Bta | Investigative | [122] | ||
| Synonyms |
CHEMBL258704
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-D-Phg-Phe-NH2 | Investigative | [69] | ||
| Synonyms |
CHEMBL210247
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| MOA | Inhibitor | |||
| External Link | ||||
| KNT-63 | Investigative | [26] | ||
| Synonyms |
CHEMBL593980
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| MOA | Inhibitor | |||
| External Link | ||||
| SB-0304 | Investigative | [123] | ||
| Synonyms |
CHEMBL409225
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| MOA | Inhibitor | |||
| Activity | EC50 = 5.17 nM | |||
| External Link | ||||
| H-Dmt-Aba-Gly-NH-CH2-Ph | Investigative | [95] | ||
| Synonyms |
CHEMBL208683; BDBM50189920
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| MOA | Inhibitor | |||
| Activity | Ki = 0.46 nM | |||
| External Link | ||||
| Tyr-Pro-L-(NMe)Phe-Pro-NH2 | Investigative | [71] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone | Investigative | [103] | ||
| Synonyms |
CHEMBL381874
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| MOA | Inhibitor | |||
| External Link | ||||
| C[L-Phe-D-pro-L-Phe-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL502411; SCHEMBL7980647
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| MOA | Inhibitor | |||
| Activity | IC50 = 21 nM | |||
| External Link | ||||
| Ac-RYYRIK-K-(NH2)-YRFB | Investigative | [81] | ||
| Synonyms |
CHEMBL412939
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph | Investigative | [94] | ||
| Synonyms |
SCHEMBL8222648
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| MOA | Inhibitor | |||
| External Link | ||||
| H-2',6'-dimethyltyrosine-Tic-OH | Investigative | [124] | ||
| Synonyms |
CHEMBL571492; 2,6-Dimethyl-L-Tyr-L-Tic-OH; BDBM50299565; H-2'',6''-dimethyltyrosine-Tic-OH; (S)-2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 894 nM | |||
| External Link | ||||
| H-Dmt-Aba-Gly-NH-CH2-Bid | Investigative | [95] | ||
| Synonyms |
CHEMBL211543
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| MOA | Inhibitor | |||
| Activity | Ki = 19.9 nM | |||
| External Link | ||||
| FLUPERAMIDE | Investigative | [125] | ||
| Synonyms |
UNII-6H13T09362; 53179-10-5; CHEMBL421665; 6H13T09362; R-18910; Fluperamide [USAN:INN]; AC1L2ZCI; AC1Q4JI5; SCHEMBL120826; ZINC4216287; BDBM50017686; R 18,910; 4-[4-[4-chloro-3-(trifluoromethyl)phenyl]-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide; 4-(4-Chloro-alpha,alpha,alpha-trifluoro-m-tolyl)-4-hydroxy-N,N-dimethyl-alpha,alpha-diphenyl-1-piperidinebutyramide; 4-[4-(4-Chloro-3-trifluoromethyl-phenyl)-4-hydroxy-piperidin-1-yl]-N,N-dimethyl-2,2-diphenyl-butyramide; 1-Piperidinebutanamide, 4-(4-
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.11 nM | |||
| External Link | ||||
| H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) | Investigative | [96] | ||
| Synonyms |
XFKPEXYNTQLONY-MPYJOUPCSA-N; CHEMBL450263
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| MOA | Inhibitor | |||
| External Link | ||||
| C[L-Ala-D-pro-L-Phe-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL499595; SCHEMBL7991248
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| MOA | Inhibitor | |||
| Activity | Ki = 22 nM | |||
| External Link | ||||
| H-mCpa-ser-Gly-Phe-Leu-Thr-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL393867
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| MOA | Inhibitor | |||
| Activity | Ki = 1100 nM | |||
| External Link | ||||
| H-Dmt-Tic-Lys(Z)-NH-Ph | Investigative | [94] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-Phe-N(CH3)2 | Investigative | [101] | ||
| Synonyms |
CHEMBL505975
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Mmp-Phe-NH | Investigative | [99] | ||
| Synonyms |
CHEMBL413676
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| MOA | Inhibitor | |||
| External Link | ||||
| N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 | Investigative | [87] | ||
| Synonyms |
CHEMBL390271; BDBM50201414; N alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2
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| MOA | Inhibitor | |||
| External Link | ||||
| D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 | Investigative | [90] | ||
| Synonyms |
CHEMBL384284
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| MOA | Inhibitor | |||
| External Link | ||||
| Dynorphin(1-8) | Investigative | [114] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| C[L-Phe-D-pro-L-Tyr-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL486388
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| MOA | Inhibitor | |||
| Activity | Ki = 120 nM | |||
| External Link | ||||
| KNT-62 | Investigative | [26] | ||
| Synonyms |
CHEMBL594654
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| MOA | Inhibitor | |||
| External Link | ||||
| DM6S | Investigative | [68] | ||
| Synonyms |
CHEMBL385448
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid | Investigative | [94] | ||
| Synonyms |
CHEMBL386309; SCHEMBL8228625
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| MOA | Inhibitor | |||
| External Link | ||||
| (-)-eseroline | Investigative | [78] | ||
| Synonyms |
Eseroline; UNII-Q22H41O18D; CHEMBL310934; CHEBI:48845; C13H18N2O; HKGWQUVGHPDEBZ-OLZOCXBDSA-N; Q22H41O18D; (3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-ol; 469-22-7; (3as-cis)-1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol; Pyrrolo(2,3-b)indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, (3aS,8aR)-; (3aS-cis)-1,2,3,3a,8,8a-Hexahydro-1,3a,8-trimethylpyrrolo(2,3-b)indol-5-ol; Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, (3aS,8aR)-
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| 1,4-bis-(Dmt-Tic-amino)butane | Investigative | [103] | ||
| Synonyms |
CHEMBL370197
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| MOA | Inhibitor | |||
| External Link | ||||
| MR-2034 | Investigative | [106] | ||
| Synonyms |
MR 2034; (-)-alpha-(1R,5R,9R)-5,9-Dimethyl-2-(L-tetrahydrofurfuryl)-2'-hydroxy-6,7-benzomorphan; 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-((tetrahydro-2-furanyl)methyl)-, (2R-(2-alpha,3(R*),6-alpha,11R*))-; 57236-85-8; AC1Q7AHJ; (2r,6r)-6,11-dimethyl-3-[(2r)-tetrahydrofuran-2-ylmethyl]-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-8-ol; BDBM81932; MR2034; LS-90624; CAS_57236-85-8
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| MOA | Inhibitor | |||
| External Link | ||||
| Ac-RYYRIK-GGG-K-(NH2)-YAFGYPS-GG | Investigative | [81] | ||
| Synonyms |
CHEMBL414736
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH | Investigative | [111] | ||
| Synonyms |
CHEMBL219482
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Gly-NH-Ph | Investigative | [96] | ||
| Synonyms |
CHEMBL501451; BDBM50272081; (3S)-N-(Phenylcarbamoylmethyl)-2-[(S)-3-(2,6-dimethyl-4-hydroxyphenyl)-2-aminopropionyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide; 2-[2-Amino-3-(4-hydroxy-2,6-dimethyl-phenyl)-propionyl]-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid phenylcarbamoylmethyl-amide
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.16 nM | |||
| External Link | ||||
| H-Dmt-Tic-Lys(Ac)-NH-Ph | Investigative | [94] | ||
| Synonyms |
SCHEMBL8228366
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| MOA | Inhibitor | |||
| External Link | ||||
| DSLET | Investigative | [27] | ||
| Synonyms |
DSTLE; Dislet; [D-Ser2, Leu5, Thr6]-enkephalin
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| MOA | Agonist | |||
| External Link | ||||
| H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 | Investigative | [111] | ||
| Synonyms |
CHEMBL415426
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc | Investigative | [126] | ||
| Synonyms |
CHEMBL413644
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-cyclopropylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL398039
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| MOA | Inhibitor | |||
| Activity | Ki = 18365 nM | |||
| External Link | ||||
| Tyr-Pro-Tmp-Phe-NH | Investigative | [99] | ||
| Synonyms |
CHEMBL389023
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Gly-NH-Bzl | Investigative | [96] | ||
| Synonyms |
CHEMBL458631; H-Dmt-Tic-Gly-NH-CH2-Ph; GTPL9838; BDBM50266025; 2-[2-Amino-3-(4-hydroxy-2,6-dimethyl-phenyl)-propionyl]-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid (benzylcarbamoyl-methyl)-amide; (S)-2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-N-(2-(benzylamino)-2-oxoethyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide; (3S)-N-(Benzylcarbamoylmethyl)-2-[(S)-3-(2,6-dimethyl-4-hydroxyphenyl)-2-aminopropionyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.16 nM | |||
| External Link | ||||
| Tyr-Pro-Imp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL434559
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| MOA | Inhibitor | |||
| External Link | ||||
| AMINOFENTANYL | Investigative | [128] | ||
| Synonyms |
CHEMBL385168; BDBM50191054
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| MOA | Inhibitor | |||
| External Link | ||||
| M3Pr6S | Investigative | [68] | ||
| Synonyms |
CHEMBL385048; 3-Propionylmorphine 6-sulfate
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 | Investigative | [83] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-Phe-NHCH3 | Investigative | [101] | ||
| Synonyms |
CHEMBL453689
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| MOA | Inhibitor | |||
| External Link | ||||
| Dmt-Pro-Phe-D-1-Nal-NH2 | Investigative | [110] | ||
| Synonyms |
CHEMBL385583
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 | Investigative | [83] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone | Investigative | [103] | ||
| Synonyms |
CHEMBL198800
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| MOA | Inhibitor | |||
| External Link | ||||
| DELTORPHIN-II | Investigative | [107] | ||
| Synonyms |
Delt II; Delt-II; (Ala(2))deltorphin II; deltorphin II, Ala(2)-; (Ala(2),glu(4))deltorphin; Deltorphin, ala(2)-glu(4)-; Tyr-ala-phe-glu-val-val-gly-NH2; Deltorphin, alanyl(2)-glutamyl(4)-; Glycinamide, L-tyrosyl-D-alanyl-L-phenylalanyl-L-alpha-glutamyl-L-valyl-L-valyl-; AC1L3XB1; LS-72217
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| MOA | Inhibitor | |||
| External Link | ||||
| MR-1029 | Investigative | [129] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Dmp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL266122
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| MOA | Inhibitor | |||
| External Link | ||||
| DELTORPHIN | Investigative | [130] | ||
| Synonyms |
Dermenkephalin; Deltorphin A; 119975-64-3; CHEMBL20775; CHEBI:81455; Tyr-met-phe-his-leu-met-asp-NH2; AC1MHYOS; DTXSID60152630; BDBM50000518; Tyrosyl-methionyl-phenylalanyl-histidyl-leucyl-methionyl-aspartamide; ZINC169301619
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-D-Phe-D-Pro-NH2 | Investigative | [71] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH2-ImidPh | Investigative | [122] | ||
| Synonyms |
CHEMBL259917
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| MOA | Inhibitor | |||
| External Link | ||||
| MR-2266 | Investigative | [129] | ||
| Synonyms |
Mrz 2266 BS; MR 2266; MR-2266-BS; (-)-Mr 2266; (-)-2-(3-Furylmethyl)-5,9-diethyl-2'-hydroxy-6,7-benzomorphan; 56649-76-4; (+/-)-2-(3-Furylmethyl)-2'-hydroxy-5,9alpha-diethyl-6,7-benzomorphan hydrochloride; 2,6-Methano-3-benzazocin-8-ol, 6,11-diethyl-3-(3-furanylmethyl)-1,2,3,4,5,6-hexahydro-, (2R,6R,11R)-; 2,6-Methano-3-benzazocin-8-ol, 6,11-diethyl-3-(3-furanylmethyl)-1,2,3,4,5,6-hexahydro-, (2R-(2alpha,6alpha,11R*))-; Mr1302 MS; Mr2267; Mr 2267; SCHEMBL4404993; BDBM82508; Mr2266; ZINC5492542; CAS_56649-76-4
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 | Investigative | [97] | ||
| Synonyms |
CHEMBL411335
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| MOA | Inhibitor | |||
| External Link | ||||
| H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH | Investigative | [124] | ||
| Synonyms |
CHEMBL555206; BDBM50299557; H-2'',6''-dimethyltyrosine-Tic-Phe-Phe-OH; (S)-2-((S)-2-((S)-2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamido)-3-phenylpropanamido)-3-phenylpropanoic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| Dmt-Pro-Phe-D-2-Nal-NH2 | Investigative | [110] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| CTOP | Investigative | [85] | ||
| Synonyms |
Ctop-NH2; CTOPA; CHEMBL507214; 103429-31-8; AC1NSJX5; H-D-Phe-c[Cys-Tyr-DTrp-Orn-Thr-Pen]-Thr-NH2; GTPL1674; CTOP, > BDBM50252861; (4R,7S,10S,13R,16S,19R)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-10-(3-aminopropyl)-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-3,3-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
Click to Show/Hide
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| MOA | Antagonist | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH2-Indn | Investigative | [122] | ||
| Synonyms |
CHEMBL260127
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| MOA | Inhibitor | |||
| External Link | ||||
| Antanal 2 | Investigative | [105] | ||
| Synonyms |
CHEMBL454035
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-Phe-OC(CH3)3 | Investigative | [101] | ||
| Synonyms |
CHEMBL500195
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| MOA | Inhibitor | |||
| External Link | ||||
| DERMORPHIN | Investigative | [81] | ||
| Synonyms |
77614-16-5; H-Tyr-D-ala-phe-gly-tyr-pro-ser-NH2; UNII-2SEC01B703; DERMORPHIN ACETATE; Tyrosyl-alanyl-phenylalanyl-glycyl-tyrosyl-prolyl-serinamide; CHEMBL278789; 2SEC01B703; Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2; AC1NUNYZ; YAFGYPS-NH2; SCHEMBL237169; Tyr-Ala-Phe-Gly-Tyr-Pro-Ser; DTXSID40228281; HY-P0244
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 1.585 nM | |||
| External Link | ||||
| Tyr-Pro-Phe-Phe-OCH3 | Investigative | [101] | ||
| Synonyms |
CHEMBL361922; Tyr-Pro-Phe-Phe-OMe
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid | Investigative | [94] | ||
| Synonyms |
SCHEMBL8230993; CHEMBL377960
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 | Investigative | [111] | ||
| Synonyms |
CHEMBL269314
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| MOA | Inhibitor | |||
| External Link | ||||
| MR-1526 | Investigative | [129] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Asp-N(Me)-Ph | Investigative | [96] | ||
| Synonyms |
CHEMBL448360
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-(2-methylquinolin-4-ylamino)-N-phenylacetamide | Investigative | [131] | ||
| Synonyms |
CHEMBL594511
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 | Investigative | [111] | ||
| Synonyms |
CHEMBL218781
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Glu-NH-(CH2)5-NH2 | Investigative | [132] | ||
| Synonyms |
CHEMBL225479
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| MOA | Inhibitor | |||
| External Link | ||||
| C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL507127
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| MOA | Inhibitor | |||
| Activity | Ki = 170 nM | |||
| External Link | ||||
| Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 | Investigative | [71] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH2-Indl | Investigative | [122] | ||
| Synonyms |
CHEMBL408975
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Asp-NH-Ph | Investigative | [96] | ||
| Synonyms |
CHEMBL501202
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Aba-ala-Gly-Phe-leu-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL247064
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| MOA | Inhibitor | |||
| Activity | Ki = 1200 nM | |||
| External Link | ||||
| H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Investigative | [117] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac | Investigative | [126] | ||
| Synonyms |
CHEMBL408889
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) | Investigative | [96] | ||
| Synonyms |
CHEMBL499099; BDBM50272228
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| MOA | Inhibitor | |||
| External Link | ||||
| C[L-Tyr-D-pro-L-Phe-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL506217
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| MOA | Inhibitor | |||
| Activity | Ki = 670 nM | |||
| External Link | ||||
| Tyr-(S)-Aba-Gly-Phe-NH2 | Investigative | [89] | ||
| Synonyms |
CHEMBL399796
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Lys-NH-CH2-Ph | Investigative | [94] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid | Investigative | [94] | ||
| Synonyms |
CHEMBL212172
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH | Investigative | [111] | ||
| Synonyms |
CHEMBL375095
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH | Investigative | [111] | ||
| Synonyms |
CHEMBL376453
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Apa-ala-Gly-Phe-leu-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL247363
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| MOA | Inhibitor | |||
| Activity | Ki = 1400 nM | |||
| External Link | ||||
| 1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane | Investigative | [103] | ||
| Synonyms |
CHEMBL370399
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Lys(Z)-NH-CH2-Ph | Investigative | [94] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 | Investigative | [117] | ||
| Synonyms |
CHEMBL268162
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| MOA | Inhibitor | |||
| External Link | ||||
| 1,6-bis-(Dmt-Tic-amino)hexane | Investigative | [103] | ||
| Synonyms |
CHEMBL197185
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| MOA | Inhibitor | |||
| External Link | ||||
| ZYKLOPHIN | Investigative | [133] | ||
| Synonyms |
GTPL9193; CHEMBL574568
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| MOA | Inhibitor | |||
| External Link | ||||
| M3P6S | Investigative | [68] | ||
| Synonyms |
CHEMBL213228
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| MOA | Inhibitor | |||
| External Link | ||||
| CARBOXYFENTANYL | Investigative | [134] | ||
| Synonyms |
CHEBI:61106; CHEMBL216239; 4-oxo-4-{phenyl[1-(2-phenylethyl)piperidin-4-yl]amino}butanoic acid; 4-anilidopiperidine, 8; Epitope ID:153518; SCHEMBL5163413; BDBM21114; ZINC14975441; 4-Oxo-4-[N-(1-phenethylpiperidine-4-yl)anilino]butyric acid; 3-{phenyl[1-(2-phenylethyl)piperidin-4-yl]carbamoyl}propanoic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-(CH2)6-NH-Phe-H | Investigative | [121] | ||
| Synonyms |
CHEMBL198909
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-[3-(3-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol | Investigative | [118] | ||
| Synonyms |
CHEMBL212743; SCHEMBL14506371
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| MOA | Inhibitor | |||
| Activity | Ki = 1000 nM | |||
| External Link | ||||
| Tyr-Pro-Phe-Phe-OCH2OH | Investigative | [101] | ||
| Synonyms |
CHEMBL522293
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| MOA | Inhibitor | |||
| External Link | ||||
| 3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone | Investigative | [103] | ||
| Synonyms |
CHEMBL373668
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|
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH2-Imid | Investigative | [122] | ||
| Synonyms |
CHEMBL407957
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Phe-Phe-NHNH2 | Investigative | [101] | ||
| Synonyms |
CHEMBL180777
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| MOA | Inhibitor | |||
| External Link | ||||
| [3H]U69593 | Investigative | [68] | ||
| Synonyms |
U-69593; U69593; 96744-75-1; U 69593; UNII-J5S4K6TKTG; U 69,593; J5S4K6TKTG; N-Methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro(4,5)dec-8-yl)benzeneacetamide; CHEBI:73357; n-methyl-2-phenyl-n-[(5r,7s,8s)-7-(pyrrolidin-1-yl)-1-oxaspiro[45]dec-8-yl]acetamide; Benzeneacetamide, N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro(45)dec-8-yl)-, (5alpha,7alpha,8beta)-(-)-; NCGC00163179-01; DSSTox_CID_26326; DSSTox_RID_81542; U69,593; DSSTox_GSID_46326; [3H]-U69593
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 250 nM | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH2-Boa | Investigative | [122] | ||
| Synonyms |
CHEMBL258458
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-Glu-NH2 | Investigative | [132] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| M3A6S | Investigative | [68] | ||
| Synonyms |
CHEMBL214040; 3-Acetylmorphine 6-sulfate; 3-O-acetylmorphine-6-sulfate
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid | Investigative | [94] | ||
| Synonyms |
CHEMBL378082
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| MOA | Inhibitor | |||
| External Link | ||||
| M3IBu6S | Investigative | [68] | ||
| Synonyms |
CHEMBL211576
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-NH-(CH2)6-NH-Tic-H | Investigative | [121] | ||
| Synonyms |
CHEMBL380590
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Cdp-ser-Gly-Phe-Leu-Thr-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL247760
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|
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| MOA | Inhibitor | |||
| Activity | Ki = 19 nM | |||
| External Link | ||||
| D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) | Investigative | [90] | ||
| Synonyms |
CHEMBL437283
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|
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-(S)-spiro-Aba-Gly-Phe-NH2 | Investigative | [89] | ||
| Synonyms |
CHEMBL401143
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Aba-Gly-NH-Ph | Investigative | [95] | ||
| Synonyms |
CHEMBL377392
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|
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| MOA | Inhibitor | |||
| Activity | Ki = 1.48 nM | |||
| External Link | ||||
| Ac-RYYRIK-K-(NH2)-YAFGYPS | Investigative | [81] | ||
| Synonyms |
CHEMBL404792
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-Emp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL375274
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Pro-L-Phe-D-Pro-NH2 | Investigative | [71] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-Pro-Ala-Phe-NH2 | Investigative | [76] | ||
| Synonyms |
YPAF-NH2
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| MOA | Inhibitor | |||
| Activity | Ki = 225.9 nM | |||
| External Link | ||||
| Oxymorphone semicarbazone hydrochloride | Investigative | [114] | ||
| Synonyms |
CHEMBL1202432; Oxymorphone Semicarbazone HCl
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-Tic-Cha-Phe-OH | Investigative | [111] | ||
| Synonyms |
CHEMBL197937
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-Pro-Dap(6DMN)-Phe-NH2 | Investigative | [97] | ||
| Synonyms |
CHEMBL207661
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 | Investigative | [111] | ||
| Synonyms |
CHEMBL218782
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-Methylthiofentanyl | Investigative | [135] | ||
| Synonyms |
3-Methyl-thiofentanyl; UNII-C9C204973M; 86052-04-2; CHEBI:53763; N-(3-Methyl-1-(2-thienyl)ethyl-4-piperidinyl)-N-phenylpropanamide; C9C204973M; Propanamide, N-(3-methyl-1-(2-(2-thienyl)ethyl)-4-piperidinyl)-N-phenyl-; N-{3-methyl-1-[2-(2-thienyl)ethyl]piperidin-4-yl}-N-phenylpropanamide; DEA No. 9833; 3-Methylthiofentanil; Epitope ID:153515; AC1Q5I8I; AC1L1WU2; SCHEMBL1742151; CHEMBL2365680; DB01439; FT-0672232
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| MOA | Agonist | |||
| External Link | ||||
| (-)-cyclorphan | Investigative | [136] | ||
| Synonyms |
CHEMBL291468; BDBM50105483; 17-cyclopropylmethyl-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2,4,6-trien-4-ol; 17-cyclopropylmethyl-(1R,9R)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-ol
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| 5-(4-((phenethylamino)methyl)phenoxy)picolinamide | Investigative | [72] | ||
| Synonyms |
CHEMBL236376; SCHEMBL3771658
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|
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| MOA | Inhibitor | |||
| Activity | Ki = 0.44 nM | |||
| External Link | ||||
| MCL-117 | Investigative | [136] | ||
| Synonyms |
CHEMBL1790045; (-)3-hydroxy-N-propargylmorphinan; BDBM50366764
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| MOA | Inhibitor | |||
| Activity | Ki = 0.003 nM | |||
| External Link | ||||
| 17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine | Investigative | [104] | ||
| Synonyms |
CHEMBL568757
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| MOA | Inhibitor | |||
| Activity | Ki = 0.08 nM | |||
| External Link | ||||
| 1-benzhydryl-4-isopropylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL233721
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| MOA | Inhibitor | |||
| Activity | Ki = 13230 nM | |||
| External Link | ||||
| Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 4; CHEMBL205965; BDBM21134; (3S)-3-[(2S)-2-[(2S)-2-(2-{[(2R)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidin-2-yl]formamido}acetamido)-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| BUTORPHAN | Investigative | [137] | ||
| Synonyms |
CHEMBL301160; MCL-101; SCHEMBL11805323; ZINC3982790; 3-Hydroxy-N-cyclobutylmethylmorphinan; BDBM50135808; 3-hydroxy-n-cyclobutylmethyl morphinan
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.12 nM | |||
| External Link | ||||
| 1-benzhydryl-4-tert-butylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL234771
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| MOA | Inhibitor | |||
| Activity | Ki = 3599 nM | |||
| External Link | ||||
| 8-carboxamidocyclazocine | Investigative | [138] | ||
| Synonyms |
CHEMBL58646; 8-CAC; SCHEMBL12014004; (6S,11R)-3-Cyclopropylmethyl-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocine-8-carboxylic acid amide; PDSP1_000954; PDSP2_000939
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.31 nM | |||
| External Link | ||||
| quadazocine | Investigative | [27] | ||
| Synonyms |
(-)-WIN 44,441; (-)-quadazocine
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| MOA | Antagonist | |||
| External Link | ||||
| 17-methyl-4'-methyldihydromorphinone | Investigative | [139] | ||
| Synonyms |
CHEMBL607018
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| MOA | Inhibitor | |||
| External Link | ||||
| MCL-443 | Investigative | [140] | ||
| Synonyms |
CHEMBL394624
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| MOA | Inhibitor | |||
| Activity | Ki = 0.7 nM | |||
| External Link | ||||
| H-Cpa-Gly-Gly-Phe-Met-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL391580
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| MOA | Inhibitor | |||
| Activity | Ki = 28 nM | |||
| External Link | ||||
| MCL-450 | Investigative | [141] | ||
| Synonyms |
CHEMBL373984; BDBM50194274
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| MOA | Inhibitor | |||
| Activity | Ki = 0.69 nM | |||
| External Link | ||||
| Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Investigative | [142] | ||
| Synonyms |
CHEMBL373489
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| MOA | Inhibitor | |||
| External Link | ||||
| OXYMORPHINDOLE | Investigative | [143] | ||
| Synonyms |
ACMC-20di42; AC1L9G6X; CHEMBL1985511; CTK7J9928; 4,8-Methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9H)-diol,5,6,7,8,14,14b-hexahydro-7-methyl-, (4bS,8R,8aS,14bR)-; NSC707844; NSC-707844; NCI60_038277
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| MOA | Inhibitor | |||
| Activity | Ki = 105 nM | |||
| External Link | ||||
| MCL-458 | Investigative | [115] | ||
| Synonyms |
CHEMBL390912; BDBM50210556
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| MOA | Inhibitor | |||
| Activity | Ki = 5.8 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Investigative | [126] | ||
| Synonyms |
CHEMBL442483
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| MOA | Inhibitor | |||
| External Link | ||||
| Naltrexone-6-alpha-ol | Investigative | [106] | ||
| Synonyms |
CHEMBL468469; 20410-98-4; SCHEMBL679581; ZINC1656961; BDBM50254511; FT-0672601; 17-(Cyclopropylmethyl)-4,5; A-epoxy-morphinan-3,6; A,14-triol; A)-17-(Cyclopropylmethyl)-4,5-epoxy-morphinan-3,6,14-triol; 6alpha-Naltrexol solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material
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| MOA | Inhibitor | |||
| Activity | Ki = 0.21 nM | |||
| External Link | ||||
| MCL-139 | Investigative | [136] | ||
| Synonyms |
CHEMBL203251
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| MOA | Inhibitor | |||
| Activity | Ki = 0.16 nM | |||
| External Link | ||||
| Dmt-Pro-Dmt-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL388800
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| MOA | Inhibitor | |||
| External Link | ||||
| MCL-429 | Investigative | [140] | ||
| Synonyms |
CHEMBL397035
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| MOA | Inhibitor | |||
| Activity | Ki = 0.11 nM | |||
| External Link | ||||
| naltriben | Investigative | [27] | ||
| Synonyms |
Naltrindole benzofuran; 4,8-Methano-5H-bisbenzofuro(3,2-e:2',3'-g)isoquinoline-1,8a(9H)-diol, 7-(cyclopropylmethyl)-6,7,8,14b-tetrahydro-, (8R-(4bS*,8alpha,8beta,14bbeta))-; 111555-58-9; C26H25NO4; [3H]naltriben; [3H]-naltriben; NTB; naltrindolebenzofuran; GTPL1640; SCHEMBL1240717; CHEMBL100940; GTPL3828; BDBM82552; HMS2089G18; ZINC3874478; PDSP2_001551; LS-172157; CAS_111555-58-9; C20166; AB00691672-07
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| MOA | Antagonist | |||
| External Link | ||||
| Dmt-Pro-Phe-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL331325; 596792-36-8; Dmt-endomorphin-2; CTK1E6813; DTXSID10435187; BDBM50149384; AKOS030610408; L-Phenylalaninamide, 2,6-dimethyl-L-tyrosyl-L-prolyl-L-phenylalanyl-; (S)-1-[(S)-2-Amino-3-(4-hydroxy-2,6-dimethyl-phenyl)-propionyl]-pyrrolidine-2-carboxylic acid [(S)-1-((S)-1-carbamoyl-2-phenyl-ethylcarbamoyl)-2-phenyl-ethyl]-amide
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| MOA | Inhibitor | |||
| Activity | EC50 = 0.1 nM | |||
| External Link | ||||
| CYCLORPHAN | Investigative | [137] | ||
| Synonyms |
17-(Cyclopropylmethyl)morphinan-3-ol; 4163-15-9; UNII-U6Z73N36V0; EINECS 224-007-5; CHEMBL49269; (-)-3-Hydroxy-N-cyclopropylmethylmorphinan; U6Z73N36V0; Morphinan, (-)-3-hydroxy-N-cyclopropylmethyl-; Morphinan-3-ol, 17-(cyclopropylmethyl)- (8CI,9CI); SCHEMBL159134; CTK4I5050; ZINC4215487; PDSP2_000668; BDBM50135800; N-cyclopropylmethyl 3-hydroxymorphinan; 3-Hydroxy-N-cyclopropylmethylmorphinan; LS-91818; (-)-17-(Cyclopropylmethyl)morphinan-3-ol; (-)-3-Hydroxy-N-cycloproypylmethylmorphinan Mandelate
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| MOA | Inhibitor | |||
| Activity | Ki = 0.062 nM | |||
| External Link | ||||
| MCL-145 | Investigative | [136] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 0.2 nM | |||
| External Link | ||||
| NORBINALTORPHIMINE | Investigative | [144] | ||
| Synonyms |
nor-Binaltorphimine; UNII-36OOQ86QM1; 36OOQ86QM1; CHEBI:81529; C18130; 4,8:11,15-Dimethano-20H-bisbenzofuro(2,3-a:3',2'-i)dipyrido(4,3-b:3',4'-h)carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-20-methyl-, (8R-(4bR*,8alpha,8abeta,10aalpha,11beta,14aR*,19aalpha,20bbeta))-; Nor-Binaltorphamine; (-)-norbinaltorphimine; NOR-BNI (HCI)2; Lopac0_000806; GTPL1642; CHEMBL573214; SCHEMBL12013206; BDBM82551; APSUXPSYBJVPPS-YAUKWVCOSA-N
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| MOA | Inhibitor | |||
| Activity | Ki = 0.94 nM | |||
| External Link | ||||
| 3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole | Investigative | [145] | ||
| Synonyms |
CHEMBL210770; SCHEMBL14280723; NRIVFQIOYWIUPX-UHFFFAOYSA-N; BDBM50185792
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 230 nM | |||
| External Link | ||||
| Dmt-Pro-3,5Dmp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL389949
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| MOA | Inhibitor | |||
| External Link | ||||
| [3H]diprenorphine | Investigative | [85] | ||
| Synonyms |
[15,16-3H]diprenorphine
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| MOA | Antagonist | |||
| External Link | ||||
| 6beta-naltrexol HCl | Investigative | [146] | ||
| Synonyms |
CHEMBL558140; UNII-765G11MG24; 765G11MG24; 55488-86-3; Naltrexone metabolite 6; A-Naltrexol (hydrochloride); 6beta-Naltrexol hydrochloride; HY-G0019; 6beta-Hydroxynaltrexone hydrochloride; Morphinan-3,6,14-triol, 17-(cyclopropylmethyl)-4,5-epoxy-, hydrochloride, (5alpha,6beta)-; Naltrexone metabolite 6AfAE'A centa' notA inverted exclamation markAfasA'A; AfAE'Adaggeratrade markAfA centA centasA notA em leaderA inverted exclamation mark-Naltrexol (hydrochloride)
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| MOA | Inhibitor | |||
| Activity | Ki = 2.12 nM | |||
| External Link | ||||
| MCL-153 | Investigative | [147] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 29 nM | |||
| External Link | ||||
| C[L-Phe-D-pro-L-Phe-L-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL506616; CJ-15208; SCHEMBL12368055
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| MOA | Inhibitor | |||
| Activity | IC50 = 25 nM | |||
| External Link | ||||
| Dmt-Pro-Mmp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL389948
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| MOA | Inhibitor | |||
| External Link | ||||
| CYCLAZOCINE | Investigative | [137] | ||
| Synonyms |
(-)-cyclazocine; 7313-86-2; l-Cyclazocine; (-)-cis-Cyclazocine; A-Cyclazocine; AC1L55DZ; GTPL1604; CTK8F1400; DTXSID20617937; MCV 4512; (2R,6R,11R)-3-(Cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-2,6-methano-3-benzazocin-8-ol; NIH 10450; AKOS030242899; FT-0665329
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| MOA | Inhibitor | |||
| Activity | Ki = 0.16 nM | |||
| External Link | ||||
| MCL-433 | Investigative | [140] | ||
| Synonyms |
CHEMBL245049
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| MOA | Inhibitor | |||
| Activity | Ki = 1.4 nM | |||
| External Link | ||||
| 4-phenyl-1-(1-phenylpropyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL433814; SCHEMBL9520650
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| MOA | Inhibitor | |||
| Activity | Ki = 2298 nM | |||
| External Link | ||||
| NRP290 | Investigative | [27] | ||
| MOA | Agonist | |||
| External Link | ||||
| M6G thiosaccharide analogue | Investigative | [149] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| MCL-434 | Investigative | [140] | ||
| Synonyms |
CHEMBL241824
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| MOA | Inhibitor | |||
| Activity | Ki = 5.3 nM | |||
| External Link | ||||
| 4-phenyl-1-(1-phenylethyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL230249
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| MOA | Inhibitor | |||
| Activity | Ki = 6265 nM | |||
| External Link | ||||
| MCL-446 | Investigative | [115] | ||
| Synonyms |
CHEMBL428038; BDBM50210549
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| MOA | Inhibitor | |||
| Activity | Ki = 12 nM | |||
| External Link | ||||
| H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 | Investigative | [150] | ||
| Synonyms |
CHEMBL220333
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| MOA | Inhibitor | |||
| External Link | ||||
| MCL-435 | Investigative | [140] | ||
| Synonyms |
CHEMBL242046
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| MOA | Inhibitor | |||
| Activity | Ki = 1.2 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | Investigative | [151] | ||
| Synonyms |
CHEMBL261390; BDBM21007; C-terminal modified bifunctional peptide, 1; [3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]pyrrolidin-2-yl]formamido}-4-methylpentanamido]-3-(1H-indol-3-yl)propanoate
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Investigative | [152] | ||
| Synonyms |
tDADAE(9); CHEMBL229440; BDBM21126; (5S,8R,10E,13R)-13-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-5-benzyl-3,6,14-trioxo-1,4,7-triazacyclotetradec-10-ene-8-carboxylic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | EC50 = 2.65 nM | |||
| External Link | ||||
| 6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol | Investigative | [153] | ||
| Synonyms |
CHEMBL171118
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 3; CHEMBL408330; BDBM21133; (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| MCL-182 | Investigative | [115] | ||
| Synonyms |
CHEMBL49143; 3-aminobutorphan; 3-Amino-N-cyclobutylmethylmorphinan
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| MOA | Inhibitor | |||
| Activity | Ki = 3.7 nM | |||
| External Link | ||||
| TQ-1017 | Investigative | [154] | ||
| MOA | Agonist | |||
| External Link | ||||
| MCL-447 | Investigative | [115] | ||
| Synonyms |
CHEMBL394573; BDBM50210555
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| MOA | Inhibitor | |||
| Activity | Ki = 3.2 nM | |||
| External Link | ||||
| 17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate | Investigative | [104] | ||
| Synonyms |
CHEMBL568989
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.34 nM | |||
| External Link | ||||
| N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine | Investigative | [104] | ||
| Synonyms |
CHEMBL571998; MCL-610
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| MOA | Inhibitor | |||
| Activity | Ki = 0.26 nM | |||
| External Link | ||||
| MCL-183 | Investigative | [115] | ||
| Synonyms |
CHEMBL390866; SCHEMBL14419223
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 7.1 nM | |||
| External Link | ||||
| Deprotected cogener of M6G | Investigative | [149] | ||
| Synonyms |
CHEMBL362202
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| MOA | Inhibitor | |||
| Activity | Ki = 3.5 nM | |||
| External Link | ||||
| MCL-144 | Investigative | [155] | ||
| Synonyms |
CHEMBL147511; BDBM50135806; di[17-cyclobutylmethyl-(1R,9R,10R)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-yl] sebacate
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| MOA | Inhibitor | |||
| Activity | Ki = 0.09 nM | |||
| External Link | ||||
| MCL-428 | Investigative | [140] | ||
| Synonyms |
CHEMBL242048
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| MOA | Inhibitor | |||
| Activity | Ki = 0.12 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 | Investigative | [151] | ||
| Synonyms |
CHEMBL406030; BDBM21013; C-terminal modified bifunctional peptide, 6
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| MOA | Inhibitor | |||
| External Link | ||||
| MCL-448 | Investigative | [115] | ||
| Synonyms |
CHEMBL242968; BDBM50210550
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| MOA | Inhibitor | |||
| Activity | Ki = 1.4 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl | Investigative | [151] | ||
| Synonyms |
CHEMBL261608; BDBM21009; C-terminal modified bifunctional peptide, 2; benzyl (2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]pyrrolidin-2-yl]formamido}-4-methylpentanamido]-3-(1H-indol-3-yl)propanoate
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| MOA | Inhibitor | |||
| External Link | ||||
| [Dcp1]Dyn A(1-11)-NH2 | Investigative | [142] | ||
| Synonyms |
CHEMBL412997
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| MOA | Inhibitor | |||
| External Link | ||||
| SN-23 | Investigative | [63] | ||
| Synonyms |
CHEMBL564538
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| MOA | Inhibitor | |||
| External Link | ||||
| 6-desoxonaltrexone | Investigative | [36] | ||
| Synonyms |
CHEMBL511816; SCHEMBL3825815; XBPQMXFKKJADMC-WOUAJJJCSA-N; BDBM50278385; 3,14-Dihydroxy-17-cyclopropylmethyl-4,5alpha-epoxymorphinan
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| MOA | Inhibitor | |||
| Activity | Ki = 0.24 nM | |||
| External Link | ||||
| 1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL393971
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| MOA | Inhibitor | |||
| Activity | Ki = 11540 nM | |||
| External Link | ||||
| 4-(4-((phenethylamino)methyl)phenoxy)benzamide | Investigative | [72] | ||
| Synonyms |
CHEMBL238317; SCHEMBL3692341; FARQYUHOSNLRKV-UHFFFAOYSA-N; BDBM50219921
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| MOA | Inhibitor | |||
| Activity | Ki = 0.15 nM | |||
| External Link | ||||
| Dmt-Pro-Imp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL228516
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| MOA | Inhibitor | |||
| External Link | ||||
| 14-O-phenylpropylnaltrexone | Investigative | [156] | ||
| Synonyms |
CHEMBL514774; SCHEMBL3167650; BDBM50249017
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| MOA | Inhibitor | |||
| Activity | Ki = 0.34 nM | |||
| External Link | ||||
| MC-CAM | Investigative | [157] | ||
| Synonyms |
CHEMBL386272; BDBM50195674; BDBM50091405; 14-[(4-Chlorocinnamoyl)amino]-4,5alpha-epoxy-17-(cyclopropylmethyl)-3-methoxymorphinan-6-one; 1N-[4-cyclopropylmethyl-10-methoxy-14-oxo-(17S)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7,9,11(18)-trien-17-yl]-3-(4-chlorophenyl)-(E)-2-propenamide(Methyoclocinnamox (MC-CAM))
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| MOA | Inhibitor | |||
| Activity | Ki = 0.46 nM | |||
| External Link | ||||
| MCL-432 | Investigative | [140] | ||
| Synonyms |
CHEMBL242047
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| MOA | Inhibitor | |||
| Activity | Ki = 3.7 nM | |||
| External Link | ||||
| DAMGO | Investigative | [158] | ||
| Synonyms |
DAGO; glyol; Dagol; DAMGE; 78123-71-4; 2-Ala-4-mephe-5-gly-enkephalin; Tyr-ala-gly-(nme)phe-gly-ol; Enkephalin, ala(2)-mephe(4)-gly(5)-; RX 783006; (D-Ala(2)-mephe(4)-gly-ol(5))enkephalin; Ala(2)-mephe(4)-gly-ol(5) enkephalin; CHEBI:272; CHEMBL38874; Tyr-D-Ala-Gly-MePhe-Gly-ol; Enkephalin, Ala(2)-MePhe(4)-Gly-ol(5)-; H-Tyr-D-Ala-Gly-N-Me-Phe-Glycinol; Enkephalin, alanyl(2)-methylphenylalanyl(4)-glycine(5)-; [3H]DAMGO; L-Phenylalaninamide, L-tyrosyl-D-alanylglycyl-N-(2-hydroxyethyl)-Nalpha-methyl-
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| MOA | Inhibitor | |||
| Activity | Ki = 0.28 nM | |||
| External Link | ||||
| DPDPE | Investigative | [158] | ||
| Synonyms |
2,5-Pen-enkephalin; (D-Pen2,D-Pen5)-Enkephalin; Enkephalin, D-penicillamine (2,5)-; (4s,7s,13s)-7-benzyl-3,3,14,14-tetramethyl-6,9,12-trioxo-13-(l-tyrosylamino)-1,2-dithia-5,8,11-triazacyclotetradecane-4-carboxylic acid; DPLPE; c[D-Pen(2,5)]-enkephalin; CHEMBL31421; CHEBI:73356; Enkephalin, penicillamine(2,5)-; cyclo-[D-Pen(2,5)]-enkephalin; 88373-73-3; D-penicillamine-(2,5)-enkephalin; H-Tyr-c(D-Pen-Gly-Phe-D-Pen)-OH; [D-Pen(2)-D-Pen(5)]-enkephaline; H-Tyr-cyclo-(D-Pen-Gly-Phe-D-Pen)-OH; [3H]DPDPE; D-Valine, L-tyros
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| MOA | Inhibitor | |||
| Activity | IC50 = 1.6 nM | |||
| External Link | ||||
| Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl | Investigative | [159] | ||
| Synonyms |
CHEMBL448998
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| MOA | Inhibitor | |||
| External Link | ||||
| MCL-147 | Investigative | [115] | ||
| Synonyms |
CHEMBL242756; SCHEMBL14419222; Aminothiazolo-N-Cyclopropylmorphinan
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| MOA | Inhibitor | |||
| Activity | Ki = 1.5 nM | |||
| External Link | ||||
| 6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide | Investigative | [72] | ||
| Synonyms |
CHEMBL236170; SCHEMBL3697663; FZBJOVYOONJNIG-UHFFFAOYSA-N; BDBM50219917
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| MOA | Inhibitor | |||
| Activity | Ki = 22.26 nM | |||
| External Link | ||||
| dynorphin B | Investigative | [27] | ||
| Synonyms |
rimorphin
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| MOA | Agonist | |||
| External Link | ||||
| H-Cdp-Gly-Gly-Phe-Leu-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL246739
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| MOA | Inhibitor | |||
| Activity | Ki = 9.8 nM | |||
| External Link | ||||
| Dimepheptanol | Investigative | [153] | ||
| Synonyms |
Methadol; Racemethadol; Pangerin; Bimethadol; 545-90-4; NIH 2933; Betamethadol; Betametadol; 6-DIMETHYLAMINO-4,4-DIPHENYL-3-HEPTANOL; 3-HEPTANOL, 6-(DIMETHYLAMINO)-4,4-DIPHENYL-; Dimepheptanolum; Dimefeptanol; Dimefeptanolo; Bimethadolum; (-)-beta-Methadol; Betametadolo [DCIT]; (3S,6R)-Methadol; beta-Methadol, (-)-; Betametadol [INN-Spanish]; Dimefeptanolo [DCIT]; Betamethadolum [INN-Latin]; 3-Heptanol,4-diphenyl-, hydrochloride; Betamethadol [INN:BAN:DCF]; DEA No. 9609; Dimefeptanol [INN-Spanish]; Dimepheptanolum [IN
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 | Investigative | [150] | ||
| Synonyms |
CHEMBL220219
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| MOA | Inhibitor | |||
| External Link | ||||
| 6-(4-((phenethylamino)methyl)phenoxy)nicotinamide | Investigative | [58] | ||
| Synonyms |
CHEMBL238361; SCHEMBL3702187
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| MOA | Inhibitor | |||
| Activity | Ki = 0.07 nM | |||
| External Link | ||||
| C[L-mTyr-D-pro-L-Phe-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL510506
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| MOA | Inhibitor | |||
| Activity | Ki = 37 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H | Investigative | [113] | ||
| Synonyms |
CHEMBL218651
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| MOA | Inhibitor | |||
| External Link | ||||
| PHENAZOCINE | Investigative | [106] | ||
| Synonyms |
PHENAZOCINE HYDROBROMIDE; Narphen; Phenazocine (+-)- hydrobromide; EINECS 214-982-5; 1239-04-9; 1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-phenethyl-2,6-methano-3-benzazocin-8-ol hydrobromide; 2'-Hydroxy-5,9-dimethyl-2-phenethyl-6,7-benzomorphan hydrobromide; 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-phenethyl-, hydrobromide; NIH 7519 hydrobromide; AC1L24DX; C22H27NO.HBr; SCHEMBL396395; PHENETHYLAZOCINE BROMIDE; 127-35-5 (Parent); CHEMBL2107297; DTXSID20872382; AKOS022180090; LS-90611
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL393675
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| MOA | Inhibitor | |||
| Activity | Ki = 11430 nM | |||
| External Link | ||||
| MCL-445 | Investigative | [115] | ||
| Synonyms |
CHEMBL243195; BDBM50210553
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| MOA | Inhibitor | |||
| Activity | Ki = 22 nM | |||
| External Link | ||||
| MCL-449 | Investigative | [140] | ||
| Synonyms |
CHEMBL427862
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| MOA | Inhibitor | |||
| Activity | Ki = 0.29 nM | |||
| External Link | ||||
| N-(17-Methylmorphinan-3-yl)-N'-phenylurea | Investigative | [104] | ||
| Synonyms |
CHEMBL568829; BDBM50303599
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| MOA | Inhibitor | |||
| Activity | Ki = 11 nM | |||
| External Link | ||||
| MCL-431 | Investigative | [140] | ||
| Synonyms |
CHEMBL241823
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| MOA | Inhibitor | |||
| Activity | Ki = 4.8 nM | |||
| External Link | ||||
| Dmt-Pro-Tmp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL228503
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| MOA | Inhibitor | |||
| External Link | ||||
| Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 | Investigative | [142] | ||
| Synonyms |
CHEMBL386043
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 | Investigative | [151] | ||
| Synonyms |
CHEMBL438389; BDBM21012; C-terminal modified bifunctional peptide, 5
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| MOA | Inhibitor | |||
| Activity | Ki = 9.5 nM | |||
| External Link | ||||
| MCL-149 | Investigative | [115] | ||
| Synonyms |
CHEMBL299220; 3-aminocyclorphan; SCHEMBL13383188; 3-Amino-N-cyclopropylmethylmorphinan; ZINC13532322
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| MOA | Inhibitor | |||
| Activity | Ki = 1.3 nM | |||
| External Link | ||||
| LOFENTANIL | Investigative | [160] | ||
| Synonyms |
Lofentanil oxalate; Lofentanil oxalate [USAN]; Lofentanil oxalate (USAN); 61380-41-4; Lofentaniloxalat; R 34995; EINECS 262-750-7; cis-(-)-4-(Methoxycarbonyl)-3-methyl-1-phenethyl-4-(N-phenylpropionylamino)piperidinium hydrogen oxalate; R 34,995; AC1L23D4; (-)-Methyl cis-3-methyl-1-phenethyl-4-(N-phenylpropionamido)isonipecotate oxalate (1:1); FT-0670830; D04764; UNII-6C1599T3OQ component CBKLICUQYUTWQL-XWGBWKJCSA-N; methyl (3S,4R)-3-methyl-1-phenethyl-4-(N-propanoylanilino)piperidine-4-carboxylate
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| MOA | Inhibitor | |||
| Activity | Ki = 0.14 nM | |||
| External Link | ||||
| H-Tyr-Gly-Gly-Phe-Met-NH2 | Investigative | [37] | ||
| Synonyms |
[Met5]-Enkephalin Amide; [Met5]-Enkephalin, amide; CHEMBL247368; 60117-17-1; Tyr-Gly-Gly-Phe-Met-NH2; Met-enkephalinamide; L-Methioninamide, L-tyrosylglycylglycyl-L-phenylalanyl-; Enkephalinamide-met-; Methionine enkephalinamide; AC1L3X5D; CTK2F3118; HY-P1467; ZINC28893234; BDBM50207823; AKOS030610304; CS-0044396; A833448; (2S)-2-[[(2S)-2-[2-[2-[[(2S)-2-azanyl-3-(4-hydroxyphenyl)propanoyl]amino]ethanoylamino]ethanoylamino]-3-phenyl-propanoyl]amino]-4-methylsulfanyl-butanamide
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| MOA | Inhibitor | |||
| Activity | Ki = 12 nM | |||
| External Link | ||||
| ELAEOCARPENINE | Investigative | [161] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 18000 nM | |||
| External Link | ||||
| Beta-endorphin | Investigative | [162] | ||
| Synonyms |
UNII-3S51P4W3XQ; 3S51P4W3XQ; 61214-51-5; LPH (61-91); beta-Endorphin, human; SCHEMBL6238339; CHEMBL1866903; EINECS 262-330-3; beta-Endorphin human, > NCGC00163196-01; NCGC00163196-02; 27-L-Tyrosine-31-L-glutamic acid-beta-endorphin (sheep); beta-Endorphin (sheep), 27-L-tyrosine-31-L-glutamic acid-
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| MOA | Antagonist | |||
| External Link | ||||
| MCL-451 | Investigative | [141] | ||
| Synonyms |
CHEMBL384915; H-Dmt-Tic-beta-Ala-OH
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| MOA | Inhibitor | |||
| Activity | Ki = 1100 nM | |||
| External Link | ||||
| normorphine | Investigative | [27] | ||
| Synonyms |
466-97-7; Desmethylmorphine; UNII-XUI1Y24IMI; Demethylmorphine; N-Normorphine; XUI1Y24IMI; NSC 270042; CHEBI:7633; ONBWJWYUHXVEJS-ZTYRTETDSA-N; Normorfina [INN-Spanish]; Normorphinum [INN-Latin]; 4,5-Epoxy-3,6-dihydroxymorphin-7-ene; Normorphine [INN:BAN:DCF]; Normorfina; Normorphinum; EINECS 207-381-4; N-Demethylmorphine; BRN 5297209; CHEMBL1227; DEA No. 9313; Normorphine (7,8-Didehydro-4,5alpha-epoxymorphinan-3,6alpha-diol)
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| MOA | Agonist | |||
| External Link | ||||
| 6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide | Investigative | [58] | ||
| Synonyms |
CHEMBL237066; 6-[4-(2-benzylamino-ethyl)-phenoxy]-nicotinamide; SCHEMBL3698270; FCDWJNPFPYAKET-UHFFFAOYSA-N; BDBM50219925
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| MOA | Inhibitor | |||
| Activity | Ki = 2.25 nM | |||
| External Link | ||||
| Diprenorphine | Investigative | [163] | ||
| Synonyms |
14357-78-9; UNII-1F0L5N25ZZ; CHEMBL281786; CHEBI:4650; 1F0L5N25ZZ; DEA No. 9058; M50-50 Injection; Diprenorphine [INN:BAN]; Diprenorphinum [INN-Latin]; Diprenorfina [INN-Spanish]; Diprenorphinum; Diprenorfina; EINECS 238-325-7; 21-Cyclopropyl-6,7,8,14-tetrahydro-7alpha-(1-hydroxy-1-methylethyl)-6,14-endo-ethanooripavine; Diprenorfin; (5 ,7 )-17-(Cyclopropylmethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy- , -dimethyl-6,14-ethenomorphinan-7-methanol; 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-4
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| MOA | Antagonist | |||
| Activity | Ki = 0.07 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl | Investigative | [151] | ||
| Synonyms |
CHEMBL272665; BDBM21011; C-terminal modified bifunctional peptide, 4
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-Hydroxymethyl-3-hydroxymorphinan | Investigative | [104] | ||
| Synonyms |
CHEMBL570449
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| MOA | Inhibitor | |||
| Activity | Ki = 15 nM | |||
| External Link | ||||
| N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine | Investigative | [104] | ||
| Synonyms |
CHEMBL571560; MCL-630
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| MOA | Inhibitor | |||
| Activity | Ki = 1.7 nM | |||
| External Link | ||||
| MCL-154 | Investigative | [147] | ||
| Synonyms |
CHEMBL151872; BDBM50135811; (1R,9R,10R)-17-(cyclobutylmethyl)-4-[(10-{[(1R,9R,10R)-17-(cyclobutylmethyl)-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2(7),3,5-trien-4-yl]oxy}decyl)oxy]-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2(7),3,5-triene
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| MOA | Inhibitor | |||
| Activity | Ki = 66 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl | Investigative | [151] | ||
| Synonyms |
CHEMBL271619; BDBM21010; C-terminal modified bifunctional peptide, 3
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH | Investigative | [152] | ||
| Synonyms |
rDADAE (11); CHEMBL229441; BDBM21127; single bond H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH; reduced bond-c[2-D-allylglycine, 5-D-allylglycine]enkephalin; (5S,8R,13R)-13-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-5-benzyl-3,6,14-trioxo-1,4,7-triazacyclotetradecane-8-carboxylic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| HERKINORIN | Investigative | [46] | ||
| Synonyms |
CHEMBL363324; 862073-77-6; BF3DNCA methyl ester; 9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2H-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester; SCHEMBL3540059; DTXSID30235444; MolPort-003-983-869; PYDQMXRFUVDCHC-XAGHGKQISA-N; ZINC28461930; BDBM50170678; (3S,4aR,4bS,6S,8R,8aR,10aR)-6-Benzoyloxy-3-furan-3-yl-4a,8a-dimethyl-1,5-dioxo-dodecahydro-2-oxa-phenanthrene-8-carboxylic acid methyl ester
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| MOA | Inhibitor | |||
| Activity | Ki = 12 nM | |||
| External Link | ||||
| ENDOMORPHIN-1 | Investigative | [164] | ||
| Synonyms |
Endomorphin 1; 189388-22-5; Tyr-Pro-Trp-Phe-Nh2; H-Tyr-Pro-Trp-Phe-NH2; CHEMBL316446; L-Phenylalaninamide,L-tyrosyl-L-prolyl-L-tryptophyl-; (S)-N-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-1-((S)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide; (2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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| MOA | Inhibitor | |||
| Activity | EC50 = 0.001 nM | |||
| External Link | ||||
| Clocinnamox | Investigative | [156] | ||
| Synonyms |
Methoclocinnamox; C-CAM; 14-beta-(4-Chlorocinnamoylamino)-7,8-dihydro-N-cyclopropylmethylnorpmorphine mesylate; Clocinnamox mesylate; 117332-69-1; 2-Propenamide, 3-(4-chlorophenyl)-N-((5alpha)-17-(cyclopropylmethyl)-4,5-epoxy-3-hydroxy-6-oxomorphinan-14-yl)-, monomethanesulfonate; NIH 10443 mesylate; NIH 10989; SCHEMBL4404383; AKOS024259103
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| MOA | Inhibitor | |||
| Activity | Ki = 0.25 nM | |||
| External Link | ||||
| Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | Investigative | [152] | ||
| Synonyms |
cDADAE(8); CHEMBL375025; BDBM21125; (5S,8R,10Z,13R)-13-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-5-benzyl-3,6,14-trioxo-1,4,7-triazacyclotetradec-10-ene-8-carboxylic acid
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| MOA | Inhibitor | |||
| Activity | EC50 = 2.35 nM | |||
| External Link | ||||
| H-Cdp-ala-Gly-Phe-leu-OH | Investigative | [37] | ||
| Synonyms |
CHEMBL247758
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| MOA | Inhibitor | |||
| Activity | Ki = 9.8 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Investigative | [113] | ||
| Synonyms |
CHEMBL217957
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| MOA | Inhibitor | |||
| External Link | ||||
| Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate | Investigative | [136] | ||
| Synonyms |
CHEMBL372823
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| MOA | Inhibitor | |||
| Activity | Ki = 14 nM | |||
| External Link | ||||
| ethylketocyclazocine | Investigative | [27] | ||
| Synonyms |
CHEMBL71301; AC1L28LJ; GTPL1602; BDBM50017232; L024009
Click to Show/Hide
|
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| MOA | Agonist | |||
| External Link | ||||
| 3-desoxy-3-carboxamidonaltrexone | Investigative | [36] | ||
| Synonyms |
CHEMBL56695; SCHEMBL2785528; QAICPHMNUHNDMC-WUHBCXKYSA-N; BDBM50128411; 6-Oxo-17-(cyclopropylmethyl)-14-hydroxy-4,5alpha-epoxymorphinan-3-carboxamide; (5a)-17-(cyclopropylmethyl)-14-hydroxy-6-oxo-4,5-epoxymorphinan-3-carboxamide
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.71 nM | |||
| External Link | ||||
| Dmt-Pro-Emp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL374818
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|
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| MOA | Inhibitor | |||
| External Link | ||||
| METAZOCINE | Investigative | [75] | ||
| Synonyms |
Methobenzmorphan; 2,6-Methano-3-benzazocin-8-ol, 1,2,3,4,5,6-hexahydro-3,6,11-trimethyl-; NSC611380; 3734-52-9; 2'-Hydroxy-2,5,9-trimethyl-6,7-benzomorphan; AC1Q7AHP; AC1L1XA2; SCHEMBL26347; CHEMBL33376; YGSVZRIZCHZUHB-UHFFFAOYSA-N; PDSP1_001246; PDSP2_001230; NSC-611380; LS-90663; LS-90665
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| SN-28 | Investigative | [165] | ||
| Synonyms |
CHEMBL552308; SCHEMBL16248949
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| MOA | Inhibitor | |||
| External Link | ||||
| ETONITAZENE | Investigative | [143] | ||
| Synonyms |
Etonitazine; Etonitazinum; Ciba 20-684BA; ARC 1G2; Etobedolum; 911-65-9; Etonitazenum [INN-Latin]; NIH 7607; Etonitazeno [INN-Spanish]; Etonitazene [INN:BAN:DCF]; UNII-9U3GT3353T; EINECS 213-009-1; Ba-20684; Ba 20684; BRN 0363324; CHEMBL312040; DEA No. 9624; PXDBZSCGSQSKST-UHFFFAOYSA-N; C22H28N4O3; 9U3GT3353T; 1-(2-(Diethylamino)ethyl)-2-(p-ethoxybenzyl)-5-nitrobenzimidazole; 1-(2-Diethylaminoethyl)-2-(p-ethoxybenzyl)-5-nitrobenzimidazole; 1H-Benzimidazole-1-ethanamine, 2-((4-ethoxyphenyl)methyl)-N,N-diethyl-5-nitro-
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | Ki = 0.2 nM | |||
| External Link | ||||
| H-Cpa-Gly-Gly-Phe-Met-NH2 | Investigative | [37] | ||
| Synonyms |
CHEMBL246956
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|
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| MOA | Inhibitor | |||
| Activity | Ki = 18 nM | |||
| External Link | ||||
| SN-11 | Investigative | [63] | ||
| Synonyms |
CHEMBL559518
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| MOA | Inhibitor | |||
| External Link | ||||
| Benzyl derivative of M6G | Investigative | [149] | ||
| Synonyms |
CHEMBL366917
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| MOA | Inhibitor | |||
| Activity | Ki = 0.5 nM | |||
| External Link | ||||
| Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 15; CHEMBL205306; BDBM21145; (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 | Investigative | [133] | ||
| Synonyms |
CHEMBL216640; Dynorphin A (1-11) amide; Dynorphin A(1-11) amide; 79985-48-1; Dyn A(1-11)-NH2; Linear Dyn A-(1-11)NH2; BDBM50010704; BDBM50033143; H-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-NH2; Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-D-Lys-NH2; TYR-GLY-GLY-PHE-LEU-ARG-ARG-ILE-ARG-PRO-LYS-LEU-LYS-TRP-ASP-ASN-GLN-NH2
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | Ki = 5.62 nM | |||
| External Link | ||||
| 17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine | Investigative | [104] | ||
| Synonyms |
CHEMBL570225
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| MOA | Inhibitor | |||
| Activity | Ki = 1.7 nM | |||
| External Link | ||||
| MCL-444 | Investigative | [140] | ||
| Synonyms |
CHEMBL263096
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| MOA | Inhibitor | |||
| Activity | Ki = 0.3 nM | |||
| External Link | ||||
| H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 | Investigative | [150] | ||
| Synonyms |
CHEMBL220327
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| MOA | Inhibitor | |||
| External Link | ||||
| Dmt-Pro-Dmp-Phe-NH2 | Investigative | [99] | ||
| Synonyms |
CHEMBL228409
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 | Investigative | [150] | ||
| Synonyms |
CHEMBL373572
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CHEMBL336381; CCK-Opioid Peptide, 6; BDBM21136; (3S)-3-[(2S)-2-[(2S)-2-(2-{2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]acetamido}acetamido)-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 610 nM | |||
| External Link | ||||
| N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea | Investigative | [104] | ||
| Synonyms |
CHEMBL569724; BDBM50303601
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 17 nM | |||
| External Link | ||||
| 1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL234543
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| MOA | Inhibitor | |||
| Activity | Ki = 3433 nM | |||
| External Link | ||||
| RTI-5989-31 | Investigative | [166] | ||
| Synonyms |
SCHEMBL6288083
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| MOA | Inhibitor | |||
| Activity | Ki = 3.1 nM | |||
| External Link | ||||
| 6-(4-((benzylamino)methyl)phenoxy)nicotinamide | Investigative | [72] | ||
| Synonyms |
CHEMBL238316; SCHEMBL3700197; LUBVSQAMVPXMBJ-UHFFFAOYSA-N; BDBM50219916
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| MOA | Inhibitor | |||
| Activity | Ki = 2.43 nM | |||
| External Link | ||||
| [Leu5]enkephalin | Investigative | [167] | ||
| Synonyms |
[Leu5]-Enkephalin; 58822-25-6; Enkephalin; Enkephalin L; [Leu 5]enkephalin; UNII-RI01R707R6; [5-Leucine]Enkephalin; Tyr-Gly-Gly-Phe-Leu-OH; CHEMBL8234; H-Tyr-Gly-Gly-Phe-Leu-OH; CHEBI:89656; RI01R707R6; Enkephalins; L-Leucine, N-(N-(N-(N-L-tyrosylglycyl)glycyl)-L-phenylalanyl)-; Leucyl-enkephalin
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 11.4 nM | |||
| External Link | ||||
| C[L-Phe-D-pro-L-mTyr-D-trp] | Investigative | [74] | ||
| Synonyms |
CHEMBL509201
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| MOA | Inhibitor | |||
| Activity | Ki = 40 nM | |||
| External Link | ||||
| 3-Methylfentanyl | Investigative | [168] | ||
| Synonyms |
Mefentanyl; 3-MF; 42045-86-3; N-(3-Methyl-1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide; F 7209; DEA No. 9813; Propanamide, N-(3-methyl-1-(2-phenylethyl)-4-piperidinyl)-N-phenyl-; CHEBI:61092; N-(3-Methyl-1-(2-phenylethyl)-4-piperidyl)-N-phenylpropanamide; N-[3-methyl-1-(2-phenylethyl)piperidin-4-yl]-N-phenylpropanamide; 3-methyl-fentanyl; C23H30N2O; 3-Methylfentanil; AC1L1WAM; Epitope ID:153511; AC1Q5I8R; SCHEMBL2337401; HSDB 8379; CTK1D6517; MLQRZXNZHAOCHQ-UHFFFAOYSA-N; DB01571; LS-119344; R-26800
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| MOA | Agonist | |||
| External Link | ||||
| ENDOMORPHIN 2 | Investigative | [91] | ||
| Synonyms |
Endomorphin-2; 141801-26-5; H-Tyr-Pro-Phe-Phe-NH2; UNII-3PH5M0466G; CHEMBL333357; 3PH5M0466G; L-Phenylalaninamide,L-tyrosyl-L-prolyl-L-phenylalanyl-; (S)-N-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-1-oxo-3-phenylpropan-2-yl)-1-((S)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide; (2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamide
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | EC50 = 0.04 nM | |||
| External Link | ||||
| 4-phenyl-1-(1-phenylbutyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL230145
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| MOA | Inhibitor | |||
| Activity | Ki = 341 nM | |||
| External Link | ||||
| Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 1; CHEMBL218763; BDBM21131; (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-3-phenylpropanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL389665
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| MOA | Inhibitor | |||
| Activity | Ki = 2147 nM | |||
| External Link | ||||
| 4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol | Investigative | [169] | ||
| Synonyms |
CHEMBL495074; SCHEMBL471335; BDBM50252834
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 7; CHEMBL382051; BDBM21137; (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-3-phenylpropanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-ethoxy-4-phenylpiperidine | Investigative | [148] | ||
| Synonyms |
CHEMBL229016
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| MOA | Inhibitor | |||
| Activity | Ki = 377 nM | |||
| External Link | ||||
| 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide | Investigative | [170] | ||
| Synonyms |
CHEMBL1257578; CHEMBL1223815; SCHEMBL15031381; BDBM50325848; BDBM50327244; AZ-MTAB, > ZINC101363709
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 721 nM | |||
| External Link | ||||
| 1-benzhydryl-4-butylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL397761; SCHEMBL13597038
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 272 nM | |||
| External Link | ||||
| 4-phenyl-1-(1-phenylheptyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL231607
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| MOA | Inhibitor | |||
| Activity | Ki = 144 nM | |||
| External Link | ||||
| Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 14; CHEMBL383458; BDBM21144; (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL233494
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|
|||
| MOA | Inhibitor | |||
| Activity | Ki = 2988 nM | |||
| External Link | ||||
| 1-benzhydryl-4-phenylpiperidin-4-ol | Investigative | [171] | ||
| Synonyms |
CHEMBL228690
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 207 nM | |||
| External Link | ||||
| 1-benzhydryl-4-p-tolylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL393985
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|
|||
| MOA | Inhibitor | |||
| Activity | Ki = 940 nM | |||
| External Link | ||||
| Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 11; CHEMBL206974; BDBM21141; (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | Ki = 20 nM | |||
| External Link | ||||
| Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 9; CHEMBL208479; BDBM21139; (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL232067; BDBM50210228
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| MOA | Inhibitor | |||
| Activity | Ki = 1057 nM | |||
| External Link | ||||
| 1-benzhydryl-4-hexylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL234773
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| MOA | Inhibitor | |||
| Activity | Ki = 8899 nM | |||
| External Link | ||||
| 1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL231664
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 3364 nM | |||
| External Link | ||||
| 1-benzhydryl-4-cyclohexylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL394695
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| MOA | Inhibitor | |||
| Activity | Ki = 407 nM | |||
| External Link | ||||
| 1-benzhydryl-4-o-tolylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL232273
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| MOA | Inhibitor | |||
| Activity | Ki = 74 nM | |||
| External Link | ||||
| Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 13; CHEMBL379405; BDBM21143; (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-3-phenylpropanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL388123
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 246 nM | |||
| External Link | ||||
| 1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL395838
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| MOA | Inhibitor | |||
| Activity | Ki = 705 nM | |||
| External Link | ||||
| 1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL397945
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| MOA | Inhibitor | |||
| Activity | Ki = 24 nM | |||
| External Link | ||||
| Dihydromorphine | Investigative | [172] | ||
| Synonyms |
Paramorphan; 7,8-DIHYDROMORPHINE; 6-alpha-Hydromorphol; 509-60-4; Dihydromorfin [Czech]; UNII-C3S5FRP6JW; Hydromorphine; Paramorfan; Morphine, dihydro-; EINECS 208-100-8; C3S5FRP6JW; NSC 117865; Dihydromorfin; CHEBI:4575; DEA No. 9145; Morphinan-3,6alpha-diol, 4,5alpha-epoxy-17-methyl-; Morphinan-3,6-alpha-diol, 4,5-alpha-epoxy-17-methyl-; (4R,4aR,7S,7aR,12bS)-3-methyl-2,4,4a,5,6,7,7a,13-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol; 7,8-Dihydromorphin; 1421-28-9; dihydromorphin
Click to Show/Hide
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| MOA | Agonist | |||
| External Link | ||||
| 1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL233323
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| MOA | Inhibitor | |||
| Activity | Ki = 1734 nM | |||
| External Link | ||||
| O-DESMETHYL TRAMADOL | Investigative | [106] | ||
| Synonyms |
O-Desmethyltramadol; CHEMBL1400; (-)-O-Desmethyl Tramadol; 80456-81-1; 2-[(Dimethylamino)methyl]-1-(3-hydroxyphenyl)cyclohexanol; CHEMBL201556; O-Demethyl tramadol; tramadol M1 metabolite; Mono-O-demethyltramadol; 144830-15-9; 3-{(1R,2R)-2-[(dimethylamino)methyl]-1-hydroxycyclohexyl}phenol; 3-((1R,2R)-2-((dimethylamino)methyl)-1-hydroxycyclohexyl)phenol; (+)-O-Desmethyltramadol; SCHEMBL2517055; CTK8E8372; UWJUQVWARXYRCG-HIFRSBDPSA-N; ZINC2509756; BDBM50176258; BDBM50176263; Phenol, 3-(2-((dimethylamino)me
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 8.6 nM | |||
| External Link | ||||
| Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 12; CHEMBL408083; BDBM21142; (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL401234
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 11050 nM | |||
| External Link | ||||
| 4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL390279
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 147 nM | |||
| External Link | ||||
| 1-benzhydryl-4-m-tolylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL437380
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 273 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Investigative | [126] | ||
| Synonyms |
CHEMBL375412
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL232476
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| MOA | Inhibitor | |||
| Activity | Ki = 589 nM | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Investigative | [126] | ||
| Synonyms |
CHEMBL405192
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-phenyl-1-(1-phenylhexyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL230253
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| MOA | Inhibitor | |||
| Activity | Ki = 37 nM | |||
| External Link | ||||
| 4-phenyl-1-(1-phenylpentyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL390882
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| MOA | Inhibitor | |||
| Activity | Ki = 29 nM | |||
| External Link | ||||
| 1-benzhydryl-4-methoxy-4-phenylpiperidine | Investigative | [148] | ||
| Synonyms |
CHEMBL228965
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| MOA | Inhibitor | |||
| Activity | Ki = 412 nM | |||
| External Link | ||||
| 1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL232066
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| MOA | Inhibitor | |||
| Activity | Ki = 771 nM | |||
| External Link | ||||
| Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Investigative | [126] | ||
| Synonyms |
CHEMBL374325
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 2; CHEMBL382349; BDBM21132; (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL228687
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| MOA | Inhibitor | |||
| Activity | Ki = 451 nM | |||
| External Link | ||||
| 1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL233493
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| MOA | Inhibitor | |||
| Activity | Ki = 983 nM | |||
| External Link | ||||
| Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 10; CHEMBL218327; BDBM21140; H-Tyr-DPhe-Gly-DTrp-NMeNle-Asp-Phe-NH(2); (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-3-phenylpropanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Investigative | [64] | ||
| Synonyms |
CCK-Opioid Peptide, 8; CHEMBL262172; BDBM21138; (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Investigative | [113] | ||
| Synonyms |
CHEMBL386212
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL392753
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| MOA | Inhibitor | |||
| Activity | Ki = 936 nM | |||
| External Link | ||||
| 1-benzhydryl-4-phenyl-4-propoxypiperidine | Investigative | [148] | ||
| Synonyms |
CHEMBL229017
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| MOA | Inhibitor | |||
| Activity | Ki = 1649 nM | |||
| External Link | ||||
| 4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol | Investigative | [148] | ||
| Synonyms |
CHEMBL228793
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| MOA | Inhibitor | |||
| Activity | Ki = 3728 nM | |||
| External Link | ||||
| 1-benzhydryl-4-(furan-2-yl)piperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL231874
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| MOA | Inhibitor | |||
| Activity | Ki = 4554 nM | |||
| External Link | ||||
| 1-benzhydryl-4-benzylpiperidin-4-ol | Investigative | [127] | ||
| Synonyms |
CHEMBL231661
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| MOA | Inhibitor | |||
| Activity | Ki = 10390 nM | |||
| External Link | ||||
| ICI-199441 | Investigative | [173] | ||
| Synonyms |
115199-84-3; ICI-199,441 HYDROCHLORIDE; ICI 199,441 hydrochloride; Ici 199441; Ici 199,441; AC1MIZCX; N-(2-(N-Methyl-3,4-dichlorophenylacetamido)-2-phenylethyl)pyrrolidine; SCHEMBL7647023; CTK8E9897; MolPort-023-275-929; AKOS024458644; (S)-3,4-Dichloro-N-methyl-N-(1-phenyl-2-(1-pyrrolidinyl)ethyl)benzeneacetamide monohydrochloride; RT-013313; B6448; J-003264; Benzeneacetamide, 3,4-dichloro-N-methyl-N-(1-phenyl-2-(1-pyrrolidinyl)ethyl)-, monohydrochloride, (S)-
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| MOA | Inhibitor | |||
| Activity | Ki = 53 nM | |||
| External Link | ||||
| FALCARINDIOL | Investigative | [174] | ||
| Synonyms |
55297-87-5; 1,9-Heptadecadiene-4,6-diyne-3,8-diol; Heptadeca-1,9-diene-4,6-diyne-3,8-diol; AC1L1FO2; SCHEMBL16680213; CTK1C6414; 225110-25-8; AKOS030230026; AN-40378; 4CN-1774
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide | Investigative | [175] | ||
| Synonyms |
CHEMBL550063; SCHEMBL10266987; BDBM50297313
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| MOA | Inhibitor | |||
| Activity | Ki = 2700 nM | |||
| External Link | ||||
| SOMATOSTATIN | Investigative | [90] | ||
| Synonyms |
51110-01-1; Somiaton; Panhibin; Aminopan; Somatostatin acetate; SRIF; Somatotropin release-inhibiting factor; Somatotropin release-inhibiting hormone; Growth hormone release-inhibiting factor; CCRIS 7071; EINECS 256-969-7; Growth hormone release-inhibiting hormone; AY 24910; Growth hormone release inhibiting factor; Somatostatin 1-14; Ala-Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys; NCGC00181005-01; 61950-59-2; [D-Trp8]-SOMATOSTATIN; SCHEMBL3046327
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| MOA | Inhibitor | |||
| External Link | ||||
| (+/-)-nantenine | Investigative | [176] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 7265 nM | |||
| External Link | ||||
| 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Investigative | [177] | ||
| Synonyms |
AC-42; CHEMBL1242950; AC42; GTPL289; SCHEMBL4504348; ANTKBACNWQHQJE-UHFFFAOYSA-N; ZINC2022527; BDBM50326219; AKOS030284249; NCGC00485453-01; gamma-(4-Butylpiperidino)-2'-methylbutyrophenone; L019209; 4-(4-butylpiperdin-1-yl)-1-(2-methylphenyl)butan-1-one; 4-(4-butylpiperidin-1-yl)-1-(2-methylphenyl)butan-1-one
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| MOA | Inhibitor | |||
| Activity | Ki >= 1000 nM | |||
| External Link | ||||
| 8E43: Pain disorders | 1 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| FMX104 | Phase 2 | [178] | ||
| External Link | ||||
References
: m6A sites