Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03232
[1]
m6A modification G9a G9a YTHDF2 : m6A sites Indirect Inhibition Histone modification H3K9me2 G9a OPRM1
m6A Modification:
m6A Regulator YTH domain-containing family protein 2 (YTHDF2) READER
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 Inhibition
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
 Compound Name 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
 Compound Name BIX-01294 Preclinical [3]
Synonyms
BIX01294; BIX 01294
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MOA Inhibitor
Activity IC50 = 67 nM
External Link
 Compound Name A-366 Preclinical [4]
Synonyms
A 366; A366
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MOA Inhibitor
Activity IC50 = 3 nM
External Link
 Compound Name UNC0321 Investigative [5]
Synonyms
UNC-0321; UNC 0321
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MOA Inhibitor
Activity IC50 = 9000 nM
External Link
 Compound Name BRD9539 Investigative [6]
Synonyms
BRD-9539; BRD 9539
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MOA Inhibitor
Activity IC50 = 1500 nM
External Link
 Compound Name 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
 Compound Name 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
 Compound Name Propoxyphene Hydrochloride Approved [9]
Synonyms
Darvon; Dolene; Kesso-gesic; Prophene 65; Propoxyphene Hydrochloride 65; Darvon-n; Propoxyphene Napsylate
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MOA Modulator
External Link
 Compound Name 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
External Link
 Compound Name Anileridine Hydrochloride Approved [11]
Synonyms
Anileridine Phosphate; Leritine
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MOA Modulator
External Link
 Compound Name 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
External Link
 Compound Name Naloxegol Approved [13]
Synonyms
NKTR-118
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MOA Modulator
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name Naldemedine Tosylate Approved [20]
MOA Antagonist
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
External Link
 Compound Name 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
 Compound Name Oxycodone Approved [27]
MOA Modulator
Activity Ki = 12 nM
External Link
 Compound Name 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, &gt; W-5330; CHIR-01020
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MOA Modulator
Activity Ki = 5.48 nM
External Link
 Compound Name 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
 Compound Name Eluxadoline Approved [30]
Synonyms
MuDelta
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MOA Modulator
Activity EC50 = 1 nM
External Link
 Compound Name Levopropoxyphene Napsylate Anhydrous Approved [11]
Synonyms
Novrad
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MOA Modulator
External Link
 Compound Name 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
 Compound Name 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
 Compound Name 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
 Compound Name NKTR-181 Phase 3 [33]
MOA Agonist
External Link
 Compound Name 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
 Compound Name OPNT001 Phase 2 [35]
MOA Antagonist
External Link
 Compound Name ALKS33 Phase 2 [36]
Synonyms
Samidorphan
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MOA Inhibitor
Activity Ki = 0.052 nM
External Link
 Compound Name 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
 Compound Name 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
 Compound Name 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
 Compound Name TPM-1/Morphine Phase 2 [40]
MOA Inhibitor
External Link
 Compound Name Cyt-1010 Phase 1 [41]
MOA Agonist
External Link
 Compound Name GSK1521498 Phase 1 [42]
Synonyms
GSK-1521498; GSK-1521498B
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MOA Agonist
External Link
 Compound Name TRV734 Phase 1 [43]
MOA Agonist
External Link
 Compound Name 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
 Compound Name 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
 Compound Name MCP-201 Phase 1 [45]
MOA Agonist
External Link
 Compound Name 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
 Compound Name BCH-2687 Discontinued in Phase 2 [47]
MOA Agonist
External Link
 Compound Name Transdur-sufentanil Discontinued in Phase 2 [48]
Synonyms
Sufentanil transdermal patch
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MOA Agonist
External Link
 Compound Name ADL-5945 Discontinued in Phase 2 [49]
Synonyms
OpRA III
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MOA Antagonist
External Link
 Compound Name 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
 Compound Name 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
 Compound Name 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
 Compound Name 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
 Compound Name 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, &gt; NCGC00167144-01
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name KN-203 Discontinued in Phase 1 [55]
Synonyms
Mu-opioid recceptor agonist (urinary incontinence), Grunenthal/KeyNeurotek
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MOA Agonist
External Link
 Compound Name VP004 Discontinued in Phase 1 [56]
External Link
 Compound Name 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
 Compound Name 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, &gt; 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
 Compound Name 443C81 Terminated [59]
Synonyms
BW 443C; BW-443C81
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MOA Modulator
External Link
 Compound Name BCH-150 Terminated [60]
MOA Modulator
External Link
 Compound Name 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
 Compound Name DBO-11 Terminated [31]
Synonyms
166374-49-8; Naxifylline (USAN/INN)
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MOA Agonist
External Link
 Compound Name DBO-17 Terminated [31]
MOA Agonist
External Link
 Compound Name 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
 Compound Name SB-213698 Terminated [63]
Synonyms
TAN-67
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MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Dmt-Sar-Phe-D-2-Nal-NH Investigative [65]
Synonyms
CHEMBL254927; BDBM50232770
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MOA Inhibitor
External Link
 Compound Name NE-2 Investigative [27]
MOA Agonist
External Link
 Compound Name 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
 Compound Name AIKO-152 Investigative [27]
Synonyms
AIKO-150 + opioid analgesic (pain/opiate dependence), Aiko Biotechnology
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MOA Modulator
External Link
 Compound Name [Tyr-Pro-Phe-Phe-NH-]2 Investigative [67]
Synonyms
CHEMBL386887
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MOA Inhibitor
External Link
 Compound Name DC6S Investigative [68]
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Hfe-Phe-NH2 Investigative [69]
Synonyms
CHEMBL378466
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MOA Inhibitor
External Link
 Compound Name AIKO-151 Investigative [27]
Synonyms
Mu-opioid antagonist (oral, opiate dependence), Aiko Biotechnology
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MOA Antagonist
External Link
 Compound Name MM3A6S Investigative [68]
Synonyms
CHEMBL379928
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MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Hfe-Pro-NH2 Investigative [69]
Synonyms
CHEMBL380286
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MOA Inhibitor
External Link
 Compound Name NCT-400 Investigative [27]
MOA Modulator
External Link
 Compound Name Tyr-Pro-D-(NMe)Phe-D-Pro-NH2 Investigative [71]
Synonyms
CHEMBL163808
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name Tyr-Pro-Phe-Phg-NH2 Investigative [69]
Synonyms
CHEMBL378111
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MOA Inhibitor
External Link
 Compound Name SL-3111 Investigative [73]
Synonyms
CHEMBL143592; SCHEMBL9881223; BDBM50068132
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-D-Phg-NH2 Investigative [69]
Synonyms
CHEMBL208990
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Tyr-Sar-Phe-D-2-Nal-NH2 Investigative [65]
Synonyms
CHEMBL254926
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name [D-Ala2]Met-enkephalinamide Investigative [75]
Synonyms
CHEMBL287480
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name YGGWL-NH2 Investigative [76]
Synonyms
CHEMBL504973
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 12.1 nM
External Link
 Compound Name KIN-4044 Investigative [27]
Synonyms
Mu opioid antagonist (NSCLC), Kinentia
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MOA Antagonist
External Link
 Compound Name Tyr-D-Ala-Gly-NMePhe Investigative [77]
Synonyms
CHEMBL583426
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MOA Inhibitor
External Link
 Compound Name M3B6S Investigative [68]
Synonyms
CHEMBL209751
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name DM3A6S Investigative [68]
Synonyms
CHEMBL437682
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-Hfe-NH2 Investigative [69]
Synonyms
CHEMBL211147
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MOA Inhibitor
External Link
 Compound Name (+/-)-TRANS-U-50488 METHANESULFONATE Investigative [78]
Synonyms
NCG-C00093883-01
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name AKUAMMINE Investigative [78]
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name YGWFL-NH2 Investigative [76]
Synonyms
CHEMBL455502
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MOA Inhibitor
Activity Ki = 112.5 nM
External Link
 Compound Name YRFB Investigative [81]
Synonyms
CHEMBL215513
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MOA Inhibitor
External Link
 Compound Name NRT-300 Investigative [27]
Synonyms
NCT-300
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MOA Modulator
External Link
 Compound Name 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
 Compound Name Tyr-Pro-Phg-Pro-NH2 Investigative [69]
Synonyms
CHEMBL425421
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MOA Inhibitor
External Link
 Compound Name C6S Investigative [68]
Synonyms
CHEMBL1417
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-D-2-Nal-NH2 Investigative [65]
Synonyms
CHEMBL375070
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MOA Inhibitor
Activity Ki > 1000 nM
External Link
 Compound Name Tyr-D-Ala-Phe-Thr[-D-Glc(OAc)4]-Tyr-Pro-Ser-NH2 Investigative [83]
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-D-Ala-Bn Investigative [84]
Synonyms
CHEMBL577748
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 8.67 nM
External Link
 Compound Name naloxonazine Investigative [85]
Synonyms
NSC 612113
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MOA Antagonist
Activity Ki = 1.445 nM
External Link
 Compound Name Tyr-Pro-Phg-Phe-NH2 Investigative [69]
Synonyms
CHEMBL211119
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MOA Inhibitor
External Link
 Compound Name KNT-5 Investigative [86]
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name Ac-L-Phe-D-trp-L-Phe-D-pro-NH2 Investigative [74]
Synonyms
CHEMBL442612
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 360 nM
External Link
 Compound Name DM3B6S Investigative [68]
Synonyms
CHEMBL213737
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-Ala-Bn Investigative [84]
Synonyms
CHEMBL577749
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MOA Inhibitor
Activity Ki = 122 nM
External Link
 Compound Name YPAA-NH2 Investigative [76]
Synonyms
CHEMBL466147
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MOA Inhibitor
Activity Ki = 705 nM
External Link
 Compound Name KIN-3031 Investigative [27]
Synonyms
Mu opioid angonist (CNS formulation, pain), Kinentia
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MOA Modulator
External Link
 Compound Name Tyr-Pro-Phe-D-Val-Bn Investigative [84]
Synonyms
CHEMBL577746
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MOA Inhibitor
Activity Ki = 4.97 nM
External Link
 Compound Name [Tyr-Pro-Phe-NH-CH2-]2 Investigative [67]
Synonyms
CHEMBL180286
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MOA Inhibitor
External Link
 Compound Name YAWF-NH2 Investigative [76]
Synonyms
CHEMBL445690
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MOA Inhibitor
Activity Ki = 3190 nM
External Link
 Compound Name Tyr-Pro-Trp-D-Val-Bn Investigative [84]
Synonyms
CHEMBL577745
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MOA Inhibitor
Activity Ki = 2.32 nM
External Link
 Compound Name 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
 Compound Name YPWA-NH2 Investigative [76]
Synonyms
CHEMBL512955
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MOA Inhibitor
Activity Ki = 72.7 nM
External Link
 Compound Name 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-
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MOA Agonist
External Link
 Compound Name 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
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MOA Inhibitor
Activity EC50 = 5600 nM
External Link
 Compound Name [Tyr-Pro-Phe-Phe-NH-CH2-]2 Investigative [67]
Synonyms
CHEMBL409336
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MOA Inhibitor
External Link
 Compound Name Ac-YGGFL-NH2 Investigative [76]
Synonyms
CHEMBL500212
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MOA Inhibitor
Activity Ki = 37.3 nM
External Link
 Compound Name Tyr-(R)-spiro-Aba-Gly-Phe-NH2 Investigative [89]
Synonyms
CHEMBL401142
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MOA Inhibitor
External Link
 Compound Name D-Phe-Cys-Tyr--Trp-Lys-Thr-Pen-Thr-NH2 Investigative [90]
Synonyms
CHEMBL274400
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name DIHYDROAKUAMMINE Investigative [78]
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name Tyr-Pro-Trp-Gly-Bn Investigative [84]
Synonyms
CHEMBL570634
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MOA Inhibitor
Activity Ki = 56.23 nM
External Link
 Compound Name 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
 Compound Name 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
 Compound Name PL017 Investigative [93]
Synonyms
3-N-Me-Phe-morphiceptin; PL-017; PL 017
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MOA Agonist
External Link
 Compound Name ADC-5510 Investigative [27]
Synonyms
ADC-02265510; ADL-5510; Centrally acting mu opoid receptor antagonists, Adolor
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MOA Antagonist
External Link
 Compound Name MM3B6S Investigative [68]
Synonyms
CHEMBL211374
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MOA Inhibitor
External Link
 Compound Name M3S Investigative [68]
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Trp-D-Ala-Bn Investigative [84]
Synonyms
CHEMBL577747
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MOA Inhibitor
Activity Ki = 4.56 nM
External Link
 Compound Name 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]-
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MOA Inhibitor
Activity Ki = 0.41 nM
External Link
 Compound Name KRP-110 Investigative [27]
Synonyms
IDDBCP262221
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MOA Modulator
External Link
 Compound Name 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
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MOA Inhibitor
External Link
 Compound Name KRP-100 Investigative [27]
Synonyms
Mu opioid receptor antagonist, Kyorin
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MOA Antagonist
External Link
 Compound Name [Tyr-Pro-Phe-NH-]2 Investigative [67]
Synonyms
CHEMBL179946
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MOA Inhibitor
External Link
 Compound Name H-Aba-ser-Gly-Phe-Leu-Thr-OH Investigative [37]
Synonyms
CHEMBL246479
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MOA Inhibitor
Activity Ki = 640 nM
External Link
 Compound Name Tyr-(R)-Aba-Gly-Phe-NH2 Investigative [89]
Synonyms
CHEMBL250448
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Lys-NH-Ph Investigative [94]
Synonyms
SCHEMBL8224099
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MOA Inhibitor
External Link
 Compound Name 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
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-D-Asp-N(Me)-Ph Investigative [96]
Synonyms
CHEMBL502302
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid Investigative [96]
Synonyms
CHEMBL444197
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) Investigative [97]
Synonyms
CHEMBL208916
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-D-Phe-Pro-NH2 Investigative [71]
Synonyms
CHEMBL162564
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MOA Inhibitor
External Link
 Compound Name H-mCpa-ala-Gly-Phe-leu-OH Investigative [37]
Synonyms
CHEMBL246682
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MOA Inhibitor
Activity Ki = 560 nM
External Link
 Compound Name H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 Investigative [98]
Synonyms
CHEMBL371856
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MOA Inhibitor
External Link
 Compound Name H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH Investigative [98]
Synonyms
CHEMBL370701
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MOA Inhibitor
External Link
 Compound Name H-Aba-ala-Gly-Phe-Met-OH Investigative [37]
Synonyms
CHEMBL246572
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MOA Inhibitor
Activity Ki = 100 nM
External Link
 Compound Name Tyr-D-Ala-Gly-Phe-Met-NH2 Investigative [62]
Synonyms
Tyr-DAla-Gly-Phe-Met-NH2
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-3,5Dmp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL413892
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH2-CH2-NH2 Investigative [100]
Synonyms
CHEMBL241010
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MOA Inhibitor
External Link
 Compound Name Ac-RYYRIK-GGG-K-(NH2)-YRFB-GGGGG Investigative [81]
Synonyms
CHEMBL441930
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-Phe-OCH2CH3 Investigative [101]
Synonyms
CHEMBL505502
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name (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
 Compound Name H-Tyr-c[D-Orn-Aic-Glu]-NH2 Investigative [102]
Synonyms
CHEMBL106849
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MOA Inhibitor
External Link
 Compound Name 3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone Investigative [103]
Synonyms
CHEMBL200890
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MOA Inhibitor
External Link
 Compound Name 2-Benzylaminomethyl-3-hydroxymorphinan Investigative [104]
Synonyms
CHEMBL578173
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MOA Inhibitor
Activity Ki = 190 nM
External Link
 Compound Name PTI-601 Investigative [27]
MOA Modulator
External Link
 Compound Name M6S Investigative [68]
MOA Inhibitor
External Link
 Compound Name Antanal 1 Investigative [105]
Synonyms
CHEMBL507442
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MOA Inhibitor
External Link
 Compound Name KETOCYCLAZOCINE Investigative [106]
MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-D-Asp-NH-Ph Investigative [96]
Synonyms
CHEMBL498799
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name H-Dmt-Tic-Asp-NH-Bzl Investigative [96]
Synonyms
CHEMBL450566
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MOA Inhibitor
External Link
 Compound Name 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
MOA Agonist
External Link
 Compound Name H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H Investigative [100]
Synonyms
CHEMBL392469
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-L-Phe-Pro-NH2 Investigative [71]
MOA Inhibitor
External Link
 Compound Name Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 Investigative [83]
MOA Inhibitor
External Link
 Compound Name Dmt-Pro-Trp-D-2-Nal-NH2 Investigative [110]
Synonyms
CHEMBL218433
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name 6-(2-phenethylisoindolin-5-yloxy)nicotinamide Investigative [58]
Synonyms
CHEMBL235154; SCHEMBL3696847
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 658.8 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 14.3 nM
External Link
 Compound Name Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 Investigative [71]
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Gly-N(Me)-Ph Investigative [96]
Synonyms
CHEMBL500937
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H Investigative [113]
Synonyms
CHEMBL375359
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH Investigative [111]
Synonyms
CHEMBL375094
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name CTAP Investigative [93]
MOA Antagonist
External Link
 Compound Name 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
 Compound Name MCL-457 Investigative [115]
Synonyms
CHEMBL242967; BDBM50210558
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MOA Inhibitor
Activity Ki = 160 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 128.82 nM
External Link
 Compound Name 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
 Compound Name 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
 Compound Name Tyr-Pro-Dmt-Phe-NH2 Investigative [99]
Synonyms
CHEMBL228512
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MOA Inhibitor
External Link
 Compound Name H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 Investigative [102]
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name H-Aba-Gly-Gly-Phe-Leu-OH Investigative [37]
Synonyms
CHEMBL247759
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MOA Inhibitor
Activity Ki = 1200 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) Investigative [90]
Synonyms
CHEMBL413950
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MOA Inhibitor
External Link
 Compound Name N-isobutylnoroxymorphone Investigative [120]
Synonyms
CHEMBL490418; 17-Isobutyl-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one; SCHEMBL3835355; OEQLILQNMUXCHV-XFWGSAIBSA-N
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H Investigative [121]
Synonyms
CHEMBL372130
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MOA Inhibitor
External Link
 Compound Name 1,10-bis-(Dmt-Tic-amino)decane Investigative [103]
Synonyms
CHEMBL373192
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH2-Bta Investigative [122]
Synonyms
CHEMBL258704
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-D-Phg-Phe-NH2 Investigative [69]
Synonyms
CHEMBL210247
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MOA Inhibitor
External Link
 Compound Name KNT-63 Investigative [26]
Synonyms
CHEMBL593980
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MOA Inhibitor
External Link
 Compound Name SB-0304 Investigative [123]
Synonyms
CHEMBL409225
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MOA Inhibitor
Activity EC50 = 5.17 nM
External Link
 Compound Name 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
 Compound Name Tyr-Pro-L-(NMe)Phe-Pro-NH2 Investigative [71]
MOA Inhibitor
External Link
 Compound Name 3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone Investigative [103]
Synonyms
CHEMBL381874
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name Ac-RYYRIK-K-(NH2)-YRFB Investigative [81]
Synonyms
CHEMBL412939
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph Investigative [94]
Synonyms
SCHEMBL8222648
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MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity IC50 = 894 nM
External Link
 Compound Name H-Dmt-Aba-Gly-NH-CH2-Bid Investigative [95]
Synonyms
CHEMBL211543
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MOA Inhibitor
Activity Ki = 19.9 nM
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 0.11 nM
External Link
 Compound Name 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
 Compound Name 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
 Compound Name H-mCpa-ser-Gly-Phe-Leu-Thr-OH Investigative [37]
Synonyms
CHEMBL393867
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MOA Inhibitor
Activity Ki = 1100 nM
External Link
 Compound Name H-Dmt-Tic-Lys(Z)-NH-Ph Investigative [94]
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-Phe-N(CH3)2 Investigative [101]
Synonyms
CHEMBL505975
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Mmp-Phe-NH Investigative [99]
Synonyms
CHEMBL413676
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 Investigative [90]
Synonyms
CHEMBL384284
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MOA Inhibitor
External Link
 Compound Name Dynorphin(1-8) Investigative [114]
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name KNT-62 Investigative [26]
Synonyms
CHEMBL594654
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MOA Inhibitor
External Link
 Compound Name DM6S Investigative [68]
Synonyms
CHEMBL385448
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid Investigative [94]
Synonyms
CHEMBL386309; SCHEMBL8228625
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MOA Inhibitor
External Link
 Compound Name (-)-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
MOA Inhibitor
External Link
 Compound Name 1,4-bis-(Dmt-Tic-amino)butane Investigative [103]
Synonyms
CHEMBL370197
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name Ac-RYYRIK-GGG-K-(NH2)-YAFGYPS-GG Investigative [81]
Synonyms
CHEMBL414736
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH Investigative [111]
Synonyms
CHEMBL219482
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MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 0.16 nM
External Link
 Compound Name H-Dmt-Tic-Lys(Ac)-NH-Ph Investigative [94]
Synonyms
SCHEMBL8228366
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MOA Inhibitor
External Link
 Compound Name DSLET Investigative [27]
Synonyms
DSTLE; Dislet; [D-Ser2, Leu5, Thr6]-enkephalin
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MOA Agonist
External Link
 Compound Name H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 Investigative [111]
Synonyms
CHEMBL415426
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name 1-benzhydryl-4-cyclopropylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL398039
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 18365 nM
External Link
 Compound Name Tyr-Pro-Tmp-Phe-NH Investigative [99]
Synonyms
CHEMBL389023
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MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 0.16 nM
External Link
 Compound Name Tyr-Pro-Imp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL434559
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MOA Inhibitor
External Link
 Compound Name AMINOFENTANYL Investigative [128]
Synonyms
CHEMBL385168; BDBM50191054
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MOA Inhibitor
External Link
 Compound Name M3Pr6S Investigative [68]
Synonyms
CHEMBL385048; 3-Propionylmorphine 6-sulfate
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 Investigative [83]
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-Phe-NHCH3 Investigative [101]
Synonyms
CHEMBL453689
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MOA Inhibitor
External Link
 Compound Name Dmt-Pro-Phe-D-1-Nal-NH2 Investigative [110]
Synonyms
CHEMBL385583
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 Investigative [83]
MOA Inhibitor
External Link
 Compound Name 3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone Investigative [103]
Synonyms
CHEMBL198800
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MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MR-1029 Investigative [129]
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Dmp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL266122
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MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name Tyr-Pro-D-Phe-D-Pro-NH2 Investigative [71]
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH2-ImidPh Investigative [122]
Synonyms
CHEMBL259917
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 Investigative [97]
Synonyms
CHEMBL411335
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name Dmt-Pro-Phe-D-2-Nal-NH2 Investigative [110]
MOA Inhibitor
External Link
 Compound Name 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, &gt; 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
MOA Antagonist
External Link
 Compound Name H-Dmt-Tic-NH-CH2-Indn Investigative [122]
Synonyms
CHEMBL260127
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MOA Inhibitor
External Link
 Compound Name Antanal 2 Investigative [105]
Synonyms
CHEMBL454035
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-Phe-OC(CH3)3 Investigative [101]
Synonyms
CHEMBL500195
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 1.585 nM
External Link
 Compound Name Tyr-Pro-Phe-Phe-OCH3 Investigative [101]
Synonyms
CHEMBL361922; Tyr-Pro-Phe-Phe-OMe
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid Investigative [94]
Synonyms
SCHEMBL8230993; CHEMBL377960
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 Investigative [111]
Synonyms
CHEMBL269314
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MOA Inhibitor
External Link
 Compound Name MR-1526 Investigative [129]
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Asp-N(Me)-Ph Investigative [96]
Synonyms
CHEMBL448360
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MOA Inhibitor
External Link
 Compound Name 2-(2-methylquinolin-4-ylamino)-N-phenylacetamide Investigative [131]
Synonyms
CHEMBL594511
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 Investigative [111]
Synonyms
CHEMBL218781
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Glu-NH-(CH2)5-NH2 Investigative [132]
Synonyms
CHEMBL225479
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MOA Inhibitor
External Link
 Compound Name C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] Investigative [74]
Synonyms
CHEMBL507127
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 170 nM
External Link
 Compound Name Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 Investigative [71]
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH2-Indl Investigative [122]
Synonyms
CHEMBL408975
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Asp-NH-Ph Investigative [96]
Synonyms
CHEMBL501202
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MOA Inhibitor
External Link
 Compound Name H-Aba-ala-Gly-Phe-leu-OH Investigative [37]
Synonyms
CHEMBL247064
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1200 nM
External Link
 Compound Name H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Investigative [117]
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) Investigative [96]
Synonyms
CHEMBL499099; BDBM50272228
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name Tyr-(S)-Aba-Gly-Phe-NH2 Investigative [89]
Synonyms
CHEMBL399796
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Lys-NH-CH2-Ph Investigative [94]
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid Investigative [94]
Synonyms
CHEMBL212172
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH Investigative [111]
Synonyms
CHEMBL375095
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH Investigative [111]
Synonyms
CHEMBL376453
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MOA Inhibitor
External Link
 Compound Name H-Apa-ala-Gly-Phe-leu-OH Investigative [37]
Synonyms
CHEMBL247363
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MOA Inhibitor
Activity Ki = 1400 nM
External Link
 Compound Name 1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane Investigative [103]
Synonyms
CHEMBL370399
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Lys(Z)-NH-CH2-Ph Investigative [94]
MOA Inhibitor
External Link
 Compound Name 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
 Compound Name 1,6-bis-(Dmt-Tic-amino)hexane Investigative [103]
Synonyms
CHEMBL197185
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MOA Inhibitor
External Link
 Compound Name ZYKLOPHIN Investigative [133]
Synonyms
GTPL9193; CHEMBL574568
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MOA Inhibitor
External Link
 Compound Name M3P6S Investigative [68]
Synonyms
CHEMBL213228
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MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-(CH2)6-NH-Phe-H Investigative [121]
Synonyms
CHEMBL198909
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name Tyr-Pro-Phe-Phe-OCH2OH Investigative [101]
Synonyms
CHEMBL522293
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MOA Inhibitor
External Link
 Compound Name 3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone Investigative [103]
Synonyms
CHEMBL373668
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH2-Imid Investigative [122]
Synonyms
CHEMBL407957
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Phe-Phe-NHNH2 Investigative [101]
Synonyms
CHEMBL180777
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MOA Inhibitor
External Link
 Compound Name [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
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MOA Inhibitor
Activity IC50 = 250 nM
External Link
 Compound Name H-Dmt-Tic-NH-CH2-Boa Investigative [122]
Synonyms
CHEMBL258458
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-Glu-NH2 Investigative [132]
MOA Inhibitor
External Link
 Compound Name M3A6S Investigative [68]
Synonyms
CHEMBL214040; 3-Acetylmorphine 6-sulfate; 3-O-acetylmorphine-6-sulfate
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid Investigative [94]
Synonyms
CHEMBL378082
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MOA Inhibitor
External Link
 Compound Name M3IBu6S Investigative [68]
Synonyms
CHEMBL211576
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-NH-(CH2)6-NH-Tic-H Investigative [121]
Synonyms
CHEMBL380590
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MOA Inhibitor
External Link
 Compound Name H-Cdp-ser-Gly-Phe-Leu-Thr-OH Investigative [37]
Synonyms
CHEMBL247760
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MOA Inhibitor
Activity Ki = 19 nM
External Link
 Compound Name D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) Investigative [90]
Synonyms
CHEMBL437283
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MOA Inhibitor
External Link
 Compound Name Tyr-(S)-spiro-Aba-Gly-Phe-NH2 Investigative [89]
Synonyms
CHEMBL401143
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Aba-Gly-NH-Ph Investigative [95]
Synonyms
CHEMBL377392
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MOA Inhibitor
Activity Ki = 1.48 nM
External Link
 Compound Name Ac-RYYRIK-K-(NH2)-YAFGYPS Investigative [81]
Synonyms
CHEMBL404792
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-Emp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL375274
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MOA Inhibitor
External Link
 Compound Name Tyr-Pro-L-Phe-D-Pro-NH2 Investigative [71]
MOA Inhibitor
External Link
 Compound Name H-Tyr-Pro-Ala-Phe-NH2 Investigative [76]
Synonyms
YPAF-NH2
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MOA Inhibitor
Activity Ki = 225.9 nM
External Link
 Compound Name Oxymorphone semicarbazone hydrochloride Investigative [114]
Synonyms
CHEMBL1202432; Oxymorphone Semicarbazone HCl
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MOA Inhibitor
External Link
 Compound Name H-Tyr-Tic-Cha-Phe-OH Investigative [111]
Synonyms
CHEMBL197937
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MOA Inhibitor
External Link
 Compound Name H-Tyr-Pro-Dap(6DMN)-Phe-NH2 Investigative [97]
Synonyms
CHEMBL207661
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MOA Inhibitor
External Link
 Compound Name H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 Investigative [111]
Synonyms
CHEMBL218782
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MOA Inhibitor
External Link
 Compound Name 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
 Compound Name (-)-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
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MOA Inhibitor
External Link
 Compound Name 5-(4-((phenethylamino)methyl)phenoxy)picolinamide Investigative [72]
Synonyms
CHEMBL236376; SCHEMBL3771658
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MOA Inhibitor
Activity Ki = 0.44 nM
External Link
 Compound Name MCL-117 Investigative [136]
Synonyms
CHEMBL1790045; (-)3-hydroxy-N-propargylmorphinan; BDBM50366764
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MOA Inhibitor
Activity Ki = 0.003 nM
External Link
 Compound Name 17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine Investigative [104]
Synonyms
CHEMBL568757
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MOA Inhibitor
Activity Ki = 0.08 nM
External Link
 Compound Name 1-benzhydryl-4-isopropylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL233721
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MOA Inhibitor
Activity Ki = 13230 nM
External Link
 Compound Name 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
 Compound Name BUTORPHAN Investigative [137]
Synonyms
CHEMBL301160; MCL-101; SCHEMBL11805323; ZINC3982790; 3-Hydroxy-N-cyclobutylmethylmorphinan; BDBM50135808; 3-hydroxy-n-cyclobutylmethyl morphinan
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.12 nM
External Link
 Compound Name 1-benzhydryl-4-tert-butylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL234771
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MOA Inhibitor
Activity Ki = 3599 nM
External Link
 Compound Name 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
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MOA Inhibitor
Activity Ki = 0.31 nM
External Link
 Compound Name quadazocine Investigative [27]
Synonyms
(-)-WIN 44,441; (-)-quadazocine
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MOA Antagonist
External Link
 Compound Name 17-methyl-4'-methyldihydromorphinone Investigative [139]
Synonyms
CHEMBL607018
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MOA Inhibitor
External Link
 Compound Name MCL-443 Investigative [140]
Synonyms
CHEMBL394624
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MOA Inhibitor
Activity Ki = 0.7 nM
External Link
 Compound Name H-Cpa-Gly-Gly-Phe-Met-OH Investigative [37]
Synonyms
CHEMBL391580
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MOA Inhibitor
Activity Ki = 28 nM
External Link
 Compound Name MCL-450 Investigative [141]
Synonyms
CHEMBL373984; BDBM50194274
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MOA Inhibitor
Activity Ki = 0.69 nM
External Link
 Compound Name Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Investigative [142]
Synonyms
CHEMBL373489
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MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 105 nM
External Link
 Compound Name MCL-458 Investigative [115]
Synonyms
CHEMBL390912; BDBM50210556
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MOA Inhibitor
Activity Ki = 5.8 nM
External Link
 Compound Name 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
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.21 nM
External Link
 Compound Name MCL-139 Investigative [136]
Synonyms
CHEMBL203251
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MOA Inhibitor
Activity Ki = 0.16 nM
External Link
 Compound Name Dmt-Pro-Dmt-Phe-NH2 Investigative [99]
Synonyms
CHEMBL388800
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MOA Inhibitor
External Link
 Compound Name MCL-429 Investigative [140]
Synonyms
CHEMBL397035
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MOA Inhibitor
Activity Ki = 0.11 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Antagonist
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 0.1 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.062 nM
External Link
 Compound Name MCL-145 Investigative [136]
MOA Inhibitor
Activity Ki = 0.2 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.94 nM
External Link
 Compound Name 3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole Investigative [145]
Synonyms
CHEMBL210770; SCHEMBL14280723; NRIVFQIOYWIUPX-UHFFFAOYSA-N; BDBM50185792
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 230 nM
External Link
 Compound Name Dmt-Pro-3,5Dmp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL389949
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MOA Inhibitor
External Link
 Compound Name [3H]diprenorphine Investigative [85]
Synonyms
[15,16-3H]diprenorphine
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MOA Antagonist
External Link
 Compound Name 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
 Compound Name MCL-153 Investigative [147]
MOA Inhibitor
Activity Ki = 29 nM
External Link
 Compound Name 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
 Compound Name Dmt-Pro-Mmp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL389948
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MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.16 nM
External Link
 Compound Name MCL-433 Investigative [140]
Synonyms
CHEMBL245049
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MOA Inhibitor
Activity Ki = 1.4 nM
External Link
 Compound Name 4-phenyl-1-(1-phenylpropyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL433814; SCHEMBL9520650
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2298 nM
External Link
 Compound Name NRP290 Investigative [27]
MOA Agonist
External Link
 Compound Name M6G thiosaccharide analogue Investigative [149]
MOA Inhibitor
External Link
 Compound Name MCL-434 Investigative [140]
Synonyms
CHEMBL241824
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 5.3 nM
External Link
 Compound Name 4-phenyl-1-(1-phenylethyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL230249
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MOA Inhibitor
Activity Ki = 6265 nM
External Link
 Compound Name MCL-446 Investigative [115]
Synonyms
CHEMBL428038; BDBM50210549
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 12 nM
External Link
 Compound Name H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 Investigative [150]
Synonyms
CHEMBL220333
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MOA Inhibitor
External Link
 Compound Name MCL-435 Investigative [140]
Synonyms
CHEMBL242046
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1.2 nM
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity EC50 = 2.65 nM
External Link
 Compound Name 6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Investigative [153]
Synonyms
CHEMBL171118
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MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MCL-182 Investigative [115]
Synonyms
CHEMBL49143; 3-aminobutorphan; 3-Amino-N-cyclobutylmethylmorphinan
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3.7 nM
External Link
 Compound Name TQ-1017 Investigative [154]
MOA Agonist
External Link
 Compound Name MCL-447 Investigative [115]
Synonyms
CHEMBL394573; BDBM50210555
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3.2 nM
External Link
 Compound Name 17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Investigative [104]
Synonyms
CHEMBL568989
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.34 nM
External Link
 Compound Name 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
 Compound Name MCL-183 Investigative [115]
Synonyms
CHEMBL390866; SCHEMBL14419223
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MOA Inhibitor
Activity Ki = 7.1 nM
External Link
 Compound Name Deprotected cogener of M6G Investigative [149]
Synonyms
CHEMBL362202
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MOA Inhibitor
Activity Ki = 3.5 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.09 nM
External Link
 Compound Name MCL-428 Investigative [140]
Synonyms
CHEMBL242048
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.12 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MCL-448 Investigative [115]
Synonyms
CHEMBL242968; BDBM50210550
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1.4 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name [Dcp1]Dyn A(1-11)-NH2 Investigative [142]
Synonyms
CHEMBL412997
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name SN-23 Investigative [63]
Synonyms
CHEMBL564538
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MOA Inhibitor
External Link
 Compound Name 6-desoxonaltrexone Investigative [36]
Synonyms
CHEMBL511816; SCHEMBL3825815; XBPQMXFKKJADMC-WOUAJJJCSA-N; BDBM50278385; 3,14-Dihydroxy-17-cyclopropylmethyl-4,5alpha-epoxymorphinan
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.24 nM
External Link
 Compound Name 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
 Compound Name 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
 Compound Name Dmt-Pro-Imp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL228516
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MOA Inhibitor
External Link
 Compound Name 14-O-phenylpropylnaltrexone Investigative [156]
Synonyms
CHEMBL514774; SCHEMBL3167650; BDBM50249017
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.34 nM
External Link
 Compound Name 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))
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.46 nM
External Link
 Compound Name MCL-432 Investigative [140]
Synonyms
CHEMBL242047
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MOA Inhibitor
Activity Ki = 3.7 nM
External Link
 Compound Name 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
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1.6 nM
External Link
 Compound Name Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl Investigative [159]
Synonyms
CHEMBL448998
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MOA Inhibitor
External Link
 Compound Name MCL-147 Investigative [115]
Synonyms
CHEMBL242756; SCHEMBL14419222; Aminothiazolo-N-Cyclopropylmorphinan
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1.5 nM
External Link
 Compound Name 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
 Compound Name dynorphin B Investigative [27]
Synonyms
rimorphin
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MOA Agonist
External Link
 Compound Name H-Cdp-Gly-Gly-Phe-Leu-OH Investigative [37]
Synonyms
CHEMBL246739
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MOA Inhibitor
Activity Ki = 9.8 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 Investigative [150]
Synonyms
CHEMBL220219
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Investigative [58]
Synonyms
CHEMBL238361; SCHEMBL3702187
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.07 nM
External Link
 Compound Name C[L-mTyr-D-pro-L-Phe-D-trp] Investigative [74]
Synonyms
CHEMBL510506
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 37 nM
External Link
 Compound Name 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
 Compound Name 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
 Compound Name 1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL393675
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 11430 nM
External Link
 Compound Name MCL-445 Investigative [115]
Synonyms
CHEMBL243195; BDBM50210553
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 22 nM
External Link
 Compound Name MCL-449 Investigative [140]
Synonyms
CHEMBL427862
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MOA Inhibitor
Activity Ki = 0.29 nM
External Link
 Compound Name N-(17-Methylmorphinan-3-yl)-N'-phenylurea Investigative [104]
Synonyms
CHEMBL568829; BDBM50303599
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 11 nM
External Link
 Compound Name MCL-431 Investigative [140]
Synonyms
CHEMBL241823
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MOA Inhibitor
Activity Ki = 4.8 nM
External Link
 Compound Name Dmt-Pro-Tmp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL228503
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MOA Inhibitor
External Link
 Compound Name Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Investigative [142]
Synonyms
CHEMBL386043
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 9.5 nM
External Link
 Compound Name MCL-149 Investigative [115]
Synonyms
CHEMBL299220; 3-aminocyclorphan; SCHEMBL13383188; 3-Amino-N-cyclopropylmethylmorphinan; ZINC13532322
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1.3 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.14 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 12 nM
External Link
 Compound Name ELAEOCARPENINE Investigative [161]
MOA Inhibitor
Activity Ki = 18000 nM
External Link
 Compound Name 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, &gt; NCGC00163196-01; NCGC00163196-02; 27-L-Tyrosine-31-L-glutamic acid-beta-endorphin (sheep); beta-Endorphin (sheep), 27-L-tyrosine-31-L-glutamic acid-
    Click to Show/Hide
MOA Antagonist
External Link
 Compound Name MCL-451 Investigative [141]
Synonyms
CHEMBL384915; H-Dmt-Tic-beta-Ala-OH
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1100 nM
External Link
 Compound Name 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)
    Click to Show/Hide
MOA Agonist
External Link
 Compound Name 6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Investigative [58]
Synonyms
CHEMBL237066; 6-[4-(2-benzylamino-ethyl)-phenoxy]-nicotinamide; SCHEMBL3698270; FCDWJNPFPYAKET-UHFFFAOYSA-N; BDBM50219925
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2.25 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Antagonist
Activity Ki = 0.07 nM
External Link
 Compound Name H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl Investigative [151]
Synonyms
CHEMBL272665; BDBM21011; C-terminal modified bifunctional peptide, 4
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 2-Hydroxymethyl-3-hydroxymorphinan Investigative [104]
Synonyms
CHEMBL570449
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 15 nM
External Link
 Compound Name N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Investigative [104]
Synonyms
CHEMBL571560; MCL-630
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1.7 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 66 nM
External Link
 Compound Name H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl Investigative [151]
Synonyms
CHEMBL271619; BDBM21010; C-terminal modified bifunctional peptide, 3
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 12 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 0.001 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.25 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 2.35 nM
External Link
 Compound Name H-Cdp-ala-Gly-Phe-leu-OH Investigative [37]
Synonyms
CHEMBL247758
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 9.8 nM
External Link
 Compound Name 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
 Compound Name Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Investigative [136]
Synonyms
CHEMBL372823
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 14 nM
External Link
 Compound Name ethylketocyclazocine Investigative [27]
Synonyms
CHEMBL71301; AC1L28LJ; GTPL1602; BDBM50017232; L024009
    Click to Show/Hide
MOA Agonist
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 0.71 nM
External Link
 Compound Name Dmt-Pro-Emp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL374818
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MOA Inhibitor
External Link
 Compound Name 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
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MOA Inhibitor
External Link
 Compound Name SN-28 Investigative [165]
Synonyms
CHEMBL552308; SCHEMBL16248949
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MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 0.2 nM
External Link
 Compound Name H-Cpa-Gly-Gly-Phe-Met-NH2 Investigative [37]
Synonyms
CHEMBL246956
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 18 nM
External Link
 Compound Name SN-11 Investigative [63]
Synonyms
CHEMBL559518
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MOA Inhibitor
External Link
 Compound Name Benzyl derivative of M6G Investigative [149]
Synonyms
CHEMBL366917
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.5 nM
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 5.62 nM
External Link
 Compound Name 17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Investigative [104]
Synonyms
CHEMBL570225
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MOA Inhibitor
Activity Ki = 1.7 nM
External Link
 Compound Name MCL-444 Investigative [140]
Synonyms
CHEMBL263096
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MOA Inhibitor
Activity Ki = 0.3 nM
External Link
 Compound Name H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Investigative [150]
Synonyms
CHEMBL220327
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MOA Inhibitor
External Link
 Compound Name Dmt-Pro-Dmp-Phe-NH2 Investigative [99]
Synonyms
CHEMBL228409
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MOA Inhibitor
External Link
 Compound Name H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Investigative [150]
Synonyms
CHEMBL373572
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
Activity Ki = 610 nM
External Link
 Compound Name 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
 Compound Name 1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL234543
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MOA Inhibitor
Activity Ki = 3433 nM
External Link
 Compound Name RTI-5989-31 Investigative [166]
Synonyms
SCHEMBL6288083
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MOA Inhibitor
Activity Ki = 3.1 nM
External Link
 Compound Name 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
 Compound Name [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
MOA Inhibitor
Activity Ki = 11.4 nM
External Link
 Compound Name 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
 Compound Name 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
    Click to Show/Hide
MOA Agonist
External Link
 Compound Name 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
MOA Inhibitor
Activity EC50 = 0.04 nM
External Link
 Compound Name 4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL230145
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MOA Inhibitor
Activity Ki = 341 nM
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name 1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Investigative [148]
Synonyms
CHEMBL389665
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MOA Inhibitor
Activity Ki = 2147 nM
External Link
 Compound Name 4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol Investigative [169]
Synonyms
CHEMBL495074; SCHEMBL471335; BDBM50252834
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name 1-benzhydryl-4-ethoxy-4-phenylpiperidine Investigative [148]
Synonyms
CHEMBL229016
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MOA Inhibitor
Activity Ki = 377 nM
External Link
 Compound Name 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Investigative [170]
Synonyms
CHEMBL1257578; CHEMBL1223815; SCHEMBL15031381; BDBM50325848; BDBM50327244; AZ-MTAB, &gt; ZINC101363709
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 721 nM
External Link
 Compound Name 1-benzhydryl-4-butylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL397761; SCHEMBL13597038
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MOA Inhibitor
Activity Ki = 272 nM
External Link
 Compound Name 4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL231607
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 144 nM
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name 1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL233494
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2988 nM
External Link
 Compound Name 1-benzhydryl-4-phenylpiperidin-4-ol Investigative [171]
Synonyms
CHEMBL228690
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 207 nM
External Link
 Compound Name 1-benzhydryl-4-p-tolylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL393985
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 940 nM
External Link
 Compound Name 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
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name 1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL232067; BDBM50210228
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1057 nM
External Link
 Compound Name 1-benzhydryl-4-hexylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL234773
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 8899 nM
External Link
 Compound Name 1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL231664
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3364 nM
External Link
 Compound Name 1-benzhydryl-4-cyclohexylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL394695
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 407 nM
External Link
 Compound Name 1-benzhydryl-4-o-tolylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL232273
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 74 nM
External Link
 Compound Name 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
MOA Inhibitor
External Link
 Compound Name 4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL388123
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 246 nM
External Link
 Compound Name 1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL395838
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 705 nM
External Link
 Compound Name 1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Investigative [148]
Synonyms
CHEMBL397945
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 24 nM
External Link
 Compound Name 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
MOA Agonist
External Link
 Compound Name 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
 Compound Name 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
MOA Inhibitor
Activity Ki = 8.6 nM
External Link
 Compound Name 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
 Compound Name 1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL401234
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 11050 nM
External Link
 Compound Name 4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL390279
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 147 nM
External Link
 Compound Name 1-benzhydryl-4-m-tolylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL437380
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 273 nM
External Link
 Compound Name H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Investigative [126]
Synonyms
CHEMBL375412
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL232476
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MOA Inhibitor
Activity Ki = 589 nM
External Link
 Compound Name 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
 Compound Name 4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL230253
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 37 nM
External Link
 Compound Name 4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL390882
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 29 nM
External Link
 Compound Name 1-benzhydryl-4-methoxy-4-phenylpiperidine Investigative [148]
Synonyms
CHEMBL228965
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 412 nM
External Link
 Compound Name 1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL232066
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 771 nM
External Link
 Compound Name Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Investigative [126]
Synonyms
CHEMBL374325
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Investigative [148]
Synonyms
CHEMBL228687
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 451 nM
External Link
 Compound Name 1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL233493
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 983 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Investigative [113]
Synonyms
CHEMBL386212
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL392753
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 936 nM
External Link
 Compound Name 1-benzhydryl-4-phenyl-4-propoxypiperidine Investigative [148]
Synonyms
CHEMBL229017
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1649 nM
External Link
 Compound Name 4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Investigative [148]
Synonyms
CHEMBL228793
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3728 nM
External Link
 Compound Name 1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Investigative [127]
Synonyms
CHEMBL231874
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 4554 nM
External Link
 Compound Name 1-benzhydryl-4-benzylpiperidin-4-ol Investigative [127]
Synonyms
CHEMBL231661
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 10390 nM
External Link
 Compound Name 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)-
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 53 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Investigative [175]
Synonyms
CHEMBL550063; SCHEMBL10266987; BDBM50297313
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2700 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (+/-)-nantenine Investigative [176]
MOA Inhibitor
Activity Ki = 7265 nM
External Link
 Compound Name 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
    Click to Show/Hide
MOA Inhibitor
Activity Ki >= 1000 nM
External Link
8E43: Pain disorders 1 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name FMX104 Phase 2 [178]
External Link
References
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Ref 178 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)