m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03445
|
[1], [2] | |||
Histone modification
H3K27ac
HDAC1
FTO
Direct
Inhibition
m6A modification
PARP1
PARP1
FTO
Demethylation
: m6A sites
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| m6A Modification: | |||||
|---|---|---|---|---|---|
| m6A Regulator | Fat mass and obesity-associated protein (FTO) | ERASER | |||
| m6A Target | Poly [ADP-ribose] polymerase 1 (PARP1) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Epigenetic Regulator | Histone deacetylase 1 (HDAC1) | ERASER | View Details | ||
| Regulated Target | Histone H3 lysine 27 acetylation (H3K27ac) | View Details | |||
| Downstream Gene | FTO | View Details | |||
| Crosstalk Relationship | Histone modification → m6A | Inhibition | |||
| Crosstalk Mechanism | histone modification directly impacts m6A modification through modulating the level of m6A regulator | ||||
| Crosstalk Summary | HDACi reduces ferroptosis suppressor protein (FSP1) by promoting its mRNA degradation. Specifically, it is confirmed that HDACi specifically targets HDAC1 and promotes the Histone H3 lysine 27 acetylation (H3K27ac) modification of fat mass- and obesity-associated gene (FTO) and AlkB Homolog 5, RNA Demethylase (ALKBH5), which results in significant activation of FTO and ALKBH5. The activation of FTO and ALKBH5 reduces N6-methyladenosine (m6A) modification on FSP1 mRNA, leading to its degradation. Crucially, lactylation of HDAC1K412is essential for ferroptosis regulation. Both Vorinostat (SAHA) and Trichostatin A (TSA) notably diminish HDAC1K412lactylation in comparison to other HDAC1 inhibitors, exhibiting a consistent trend of increasing susceptibility to ferroptosis. Targeting FTO significantly suppresses cancer cell growth and enhances chemotherapy sensitivity, which not only mediating the balance of intracellular ROS by regulating G6PD expression, but also maintaining genome instability by regulating Poly [ADP-ribose] polymerase 1 (PARP1) expression. These findings shed light on new molecular mechanisms of CRC development and treatments mediated by m6A modification. | ||||
| Responsed Disease | Colorectal cancer | ICD-11: 2B91 | |||
| Pathway Response | Glutathione metabolism | hsa00480 | |||
In-vitro Model |
LoVo | Colon adenocarcinoma | Homo sapiens | CVCL_0399 | |
| HCT 116 | Colon carcinoma | Homo sapiens | CVCL_0291 | ||
| HCT 8 | Colon adenocarcinoma | Homo sapiens | CVCL_2478 | ||
| SW620 | Colon adenocarcinoma | Homo sapiens | CVCL_0547 | ||
| In-vivo Model | For CDX model, nude mice (female, 4-6-week-old) were subcutaneously injected with 5 × 106 HCT116 cells on the both flank. For PDX model, the patient tumors were divided into small pieces and then inoculated on both flank of nude mice. For knockdown FTO mice model, FTO mice model, two weeks after inoculation, the shFTO#3 lenti-virus injected into the tumor for three consecutive days. For combined medication mice model, intraperitoneal injection of Rhein and Olaparib was started one week after inoculation. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Histone deacetylase 1 (HDAC1) | 250 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Panobinostat | Approved | [3] | ||
| Synonyms |
Faridak; LBH 589; LBH589; LBH-589; LBH-589B; NVP-LBH589; NVP-LBH-589; Panobinostat, NVP-LBH589, LBH589; (E)-N-HYDROXY-3-(4-{[2-(2-METHYL-1H-INDOL-3-YL)-ETHYLAMINO]-METHYL}-PHENYL)-ACRYLAMIDE; (E)-N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.54 nM | |||
| External Link | ||||
| Vorinostat | Approved | [3] | ||
| Synonyms |
NHNPODA; SAHA; SHH; Zolinza; Merck brand of Vorinostat; OCTANEDIOIC ACID HYDROXYAMIDE PHENYLAMIDE; SAHA cpd; Suberanilohydroxamic acid; Suberoylanilide hydroxamic acid; Vorinostat MSD; Vorinostat [USAN]; M344; MK0683; SKI390; WIN64652; MK-0683; SAHA, Suberoylanilide hydroxamic acid; SW-064652; Zolinza (TN); Vorinostat (JAN/USAN); N1-hydroxy-N8-phenyloctanediamide; Zolinza, MK-0683, SAHA; N'-hydroxy-N-phenyloctanediamide; N-Hydroxy-N'-phenyl octanediamide; N-Hyrdroxy-N'-phenyloctanediamide; N-hydroxy-N'-phenyloctanediamide; N-hydroxy-N'-phenyl-octane-1,8-diotic acid diamide; Vorinostat (HDAC inhibitor)
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 1.3 nM | |||
| External Link | ||||
| Romidepsin | Approved | [4] | ||
| Synonyms |
Chromadax; Istodax; Antibiotic FR 901228; FK 228; FK228; FR 901228; FR901228; HDInhib_000006; Chromadax (TN); FK-228; FK-901228; FR-901228; Istodax (TN); Romidepsin (USAN); Cyclo((2Z)-2-amino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl), cyclic (35)-disulfide; L-Valine, N-((3S,4E)-3-hydroxy-7-mercapto-1-oxo-4-heptenyl)-D-valyl-D-cysteinyl-(2Z)-2-amino-2-butenoxyl-, (4-1)-lactone, cyclic (1-2)-disulfide; (1S,4S,7Z,10S,16E,21R)-7-Ethylidene-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo(8.7.6)tricos-16-ene-3,6,9,19,22-pentone; (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone; (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 0.0015 nM | |||
| External Link | ||||
| HBI-8000 | Phase 1/2 | [5] | ||
| Synonyms |
CS055; SCHEMBL5500152; GTPL8305; AKOS026750315; N-(2-amino-5-fluorophenyl)-4-{[3-(pyridin-3-yl)prop-2-enamido]methyl}benzamide
Click to Show/Hide
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| MOA | Modulator | |||
| Activity | IC50 = 167 nM | |||
| External Link | ||||
| NVP-LAQ824 | Phase 3 | [6] | ||
| Synonyms |
Dacinostat; 404951-53-7; LAQ824; LAQ-824; LAQ824 (Dacinostat); UNII-V10P524501; (E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamide; CHEMBL356066; V10P524501; (2E)-N-hydroxy-3-[4-({(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enamide; Dacinostat [INN]; (E)-N-Hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]meth yl]phenyl]prop-2-enamide; (2E)-N-hydroxy-3-(4-{[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl}phenyl)prop-2-enamide; NVP-LAQ 824; NVP-LAQ824, Dacinostat, LAQ824; LBH539
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| MOA | Inhibitor | |||
| Activity | Ki = 0.55 nM | |||
| External Link | ||||
| SNDX-275 | Phase 3 | [7] | ||
| Synonyms |
Entinostat; Histone Deacetylase Inhibitor I; IN1470; MS 275; SNDX 275; MS 27-275; Ms-275; Entinostat (USAN/INN); MS-27-275; Pyridin-3-ylmethyl 4-(2-aminophenylcarbamoyl)benzylcarbamate; Pyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate; Pyridin-3-ylmethyl {4-[(2-aminophenyl)carbamoyl]benzyl}carbamate; Pyridin-3-ylmethyl{4-[(2-aminophenyl)carbamoyl]benzyl}carbamate; Carbamic acid, [[4-[[(2-aminophenyl)amino]carbonyl]phenyl] methyl]-, 3-pyridinylmethyl ester; Carbamic acid, [[4-[[(2-aminophenyl)carbaonyl]phenyl]methyl]-, 3-pyridinylmethyl ester; Entinostat, SNDX-275, MS-27-275, MS-275; N-(2-Aminophenyl)-4-[N-(pyridin-3-yl-methoxycarbonyl)aminomethyl]benzamide; N-(2-aminophenyl)-4-(N-(pyridin-3-ylmethoxycarbonyl)aminomethyl)benzamide; Carbamic acid, ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)-, 3-pyridinylmethyl ester; 3-Pyridinylmethyl ((4-(((2-aminophenyl)amino)carbonyl)phenyl)methyl)carbamate
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| MOA | Inhibitor | |||
| Activity | Ki = 22 nM | |||
| External Link | ||||
| ITF2357 | Phase 3 | [8] | ||
| Synonyms |
Givinostat; Carbamic acid, N-(4-((hydroxyamino)carbonyl)phenyl)-, (6-((diethylamino)methyl)-2-naphthalenyl)methyl ester, hydrochloride (1:1)
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| MOA | Inhibitor | |||
| Activity | Ki = 2 nM | |||
| External Link | ||||
| Resminostat | Phase 2 | [9] | ||
| Synonyms |
864814-88-0; 4SC-201; RAS2410; Resminostat (RAS2410); UNII-1578EUB98L; (E)-3-(1-((4-((dimethylamino)methyl)phenyl)sulfonyl)-1H-pyrrol-3-yl)-N-hydroxyacrylamide; BYK408740; 1578EUB98L; Resminostat [INN]; 4SC 201; Resminostat 4SC-201; Resminostat (4SC-201); SCHEMBL295541; SCHEMBL295540; GTPL7502; EX-A542; DTXSID50235587; MolPort-027-720-936; AOB87187; BCP02538; 4SC201; ZINC13983495; s2693; AKOS030526945; SB16667; DB12392; CS-1521; API0013984; BC261895
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| MOA | Inhibitor | |||
| External Link | ||||
| Sodium butyrate | Phase 2 | [10] | ||
| Synonyms |
Butyrate sodium; Sodium butanoate; Sodium propanecarboxylate; OR8783; Butanoic acid, sodium salt; Butyric Acid, Na; Sodium butyrate (USP); Sodium n-butyrate; TPA/BA; Tetradecanoyl phorbol acetate/ sodium butyrate; Butanoic acid, sodium salt (1:1); Tetradecanoyl phorbol acetate (TPA)/ sodium butyrate (BA)
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| MOA | Inhibitor | |||
| External Link | ||||
| SB-623 | Phase 2 | [11] | ||
| Synonyms |
(E)-3-[1-(2-diethylaminoethyl)-2-phenethylbenzimidazol-5-yl]-N-hydroxyprop-2-enamide
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| MOA | Inhibitor | |||
| Activity | IC50 = 52 nM | |||
| External Link | ||||
| MGCD-0103 | Phase 2 | [3] | ||
| Synonyms |
Mocetinostat; MG 0103; MG 4230; MG 4915; MG 5026; MG0103; MG4230; MG4915; MG5206; MGCD 0103; MGCD0103; MG-0103; MG-4230; MG-4915; MG-5026; Mocetinostat, MGCD0103; N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide; N-(2-Aminophenyl)-4-((4-pyridin-3-ylpyrimidin-2-ylamino)methyl)benzamide
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| MOA | Inhibitor | |||
| Activity | Ki = 9 nM | |||
| External Link | ||||
| Phenylbutyrate | Phase 2 | [12] | ||
| Synonyms |
Benzenebutyric acid; Phenyl butanoate; Phenyl butyrate; HDInhib_000004; Butanoic acid, phenyl ester; Butyric acid, phenyl ester; FR-2080; Gamma-Phenylbutyric acid; Omega-Phenylbutanoic acid; GAMMA-PHENYL-BUTYRIC ACID; Butyric acid, 4-phenyl-(8CI); 1-Phenylbutyric acid; 4-PHENYL-BUTANOIC ACID; 4-PHENYLBUTYRIC ACID; 4-Phenylbutanoic acid; 4-phenylbutans; 4-phenylbutyrate
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| MOA | Inhibitor | |||
| Activity | IC50 = 64000 nM | |||
| External Link | ||||
| CHR-3996 | Phase 1/2 | [13] | ||
| Synonyms |
CCT-075453; CHR-2504; HDAC inhibitors, Chroma Therapeutics; Histone deacetylase inhibitors, Chroma
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| MOA | Inhibitor | |||
| Activity | IC50 = 3 nM | |||
| External Link | ||||
| SB-639 | Phase 1 | [11] | ||
| Synonyms |
CHEMBL491316; AC1OCG09; SCHEMBL13118363; BDBM50248476; US8551988, 72; N-hydroxy-3-(2-phenethyl-1-(2-(pyrrolidin-1-yl)ethyl)-1H-benzo[d]imidazol-5-yl)acrylamide; (E)-N-hydroxy-3-[2-phenethyl-1-(2-pyrrolidin-1-ylethyl)benzimidazol-5-yl]prop-2-enamide
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| MOA | Inhibitor | |||
| Activity | Ki = 11 nM | |||
| External Link | ||||
| RG-2833 | Phase 1 | [5] | ||
| Synonyms |
RG-FA; HDAC-1 inhibtors (Friedreich ataxia), RepliGen
Click to Show/Hide
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| MOA | Modulator | |||
| Activity | Ki = 32 nM | |||
| External Link | ||||
| OBP-801 | Phase 1 | [14] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 3.3 nM | |||
| External Link | ||||
| PMID29671355-Compound-42 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 10 to 100 nM | |||
| External Link | ||||
| PMID28092474-Compound-33d | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32u | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33a | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32a | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32j | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32z | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32g | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-34c | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32x | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33b | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32b | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32o | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33g | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33j | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33p | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33m | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32v | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-24 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 382 nM | |||
| External Link | ||||
| PMID28092474-Compound-34b | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33e | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32t | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32c | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33i | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32r | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32h | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-65a | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 13800 nM | |||
| External Link | ||||
| PMID28092474-Compound-32y | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33h | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-38a | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33f | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| Diaryl amine derivative 3 | Patented | [16] | ||
| Synonyms |
PMID28092474-Compound-11
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 460 nM | |||
| External Link | ||||
| PMID28092474-Compound-33c | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-39 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 3840 nM | |||
| External Link | ||||
| PMID29671355-Compound-19 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 500 to 1000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32e | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32m | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32p | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32d | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32n | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-33k | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32k | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-34a | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| Isosteric imidazolyl pyrimidine derivative 1 | Patented | [17] | ||
| Synonyms |
PMID26161698-Compound-37
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 656 nM | |||
| External Link | ||||
| PMID29671355-Compound-22 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2100 nM | |||
| External Link | ||||
| PMID29671355-Compound-26 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8750 nM | |||
| External Link | ||||
| PMID28092474-Compound-33o | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32f | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| Diaryl amine derivative 2 | Patented | [16] | ||
| Synonyms |
PMID28092474-Compound-10
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 240 nM | |||
| External Link | ||||
| PMID28092474-Compound-33l | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32i | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32q | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-18 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-57 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID29671355-Compound-27 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 187 nM | |||
| External Link | ||||
| PMID28092474-Compound-32l | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 1000 nM; IC50 <= 10000 nM | |||
| External Link | ||||
| PMID28092474-Compound-32s | Patented | [16] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-38b | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 226 nM | |||
| External Link | ||||
| PMID29671355-Compound-28 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 28 nM | |||
| External Link | ||||
| PMID29671355-Compound-59 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 3 nM | |||
| External Link | ||||
| PMID29671355-Compound-55 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID29671355-Compound-73 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1000 nM | |||
| External Link | ||||
| PMID29671355-Compound-13 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 >= 10000 nM | |||
| External Link | ||||
| PMID29671355-Compound-11 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 21 nM | |||
| External Link | ||||
| PMID29671355-Compound-9 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 94 nM | |||
| External Link | ||||
| PMID29671355-Compound-8 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 16900 nM | |||
| External Link | ||||
| PMID29671355-Compound-61 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2.6 nM | |||
| External Link | ||||
| PMID29671355-Compound-23 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 3620 nM | |||
| External Link | ||||
| PMID29671355-Compound-44 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 150 nM | |||
| External Link | ||||
| PMID29671355-Compound-56 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8700 nM | |||
| External Link | ||||
| PMID29671355-Compound-67 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2900 nM | |||
| External Link | ||||
| PMID29671355-Compound-31 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 0.3 nM | |||
| External Link | ||||
| PMID29671355-Compound-21 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2120 nM | |||
| External Link | ||||
| PMID29671355-Compound-62 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 to 500 nM | |||
| External Link | ||||
| PMID29671355-Compound-43 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 23 nM | |||
| External Link | ||||
| PMID29671355-Compound-25 | Patented | [15] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 175 nM | |||
| External Link | ||||
| AN-9 | Discontinued in Phase 2 | [10] | ||
| Synonyms |
Pivanex; Pivalyloxymethyl butyrate; AN 9; AN9; AN 9 (ion exchanger); Butanoyloxymethyl 2,2-dimethylpropanoate; Butanoicacid, (2,2-dimethyl-1-oxopropoxy)methyl ester; N-(5-amino-9,10-dioxoanthracen-1-yl)acetamide; N-(5-amino-9,10-dioxo-9,10-dihydroanthracen-1-yl)acetamide; ((2,2-Dimethylpropanoyl)oxy)methyl butanoate;1,5-BIS[3-(DIETHYLAMINO)PROPIONAMIDO]ANTHRACENE-9,10-DIONE
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| Tacedinaline | Discontinued in Phase 2 | [11] | ||
| Synonyms |
Acetyldinaline; Tacedinalina; Goe 5549; PD 123654; Ci-994; Goe-5549; PD-123654; Tacedinalina [INN-Spanish]; Tacedinaline [USAN:INN]; C.I. 994; Tacedinaline (USAN/INN); 4-(Acetylamino)-N-(2-aminophenyl)benzamide; 4-acetamido-N-(2-aminophenyl)benzamide; 4-acetamido-n-(2-aminophenyl)benzamid; 4-acetylamino-N-(2'-aminophenyl)benzamide
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | Ki = 50 nM | |||
| External Link | ||||
| Pyroxamide | Discontinued in Phase 1 | [11] | ||
| Synonyms |
POLAR HYBRID COMPOUND; Suberoyl-3-aminopyridineamide hydroxamic acid; N-Hydroxy-N'-3-pyridinyloctanediamide; N'-hydroxy-N-pyridin-3-yloctanediamide; N-hydroxy-n'-(pyridin-3-yl)octanediamide; N-Hydroxy-N'-(3-pyridyl)-1,8-octanediamide
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | Ki = 2.7 nM | |||
| External Link | ||||
| M-carboxycinnamic acid bishydroxamide | Preclinical | [11] | ||
| Synonyms |
Cbha; Histone Deacetylase Inhibitor II; HDInhib_000062; M-Carboxycinnamic Acid bis-Hydroxamide; N-hydroxy-3-[(E)-3-(hydroxyamino)-3-oxoprop-1-enyl]benzamide
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| HC-Toxin | Preclinical | [11] | ||
| Synonyms |
HC Toxin; Cyclo(aoe-pro-ala-ala); Cyclo(2-amino-8-oxo-9,10-epoxydecanoic acid-prolyl-alanyl-alanine); Cyclic(L-alanyl-D-alanyl-eta-oxo-L-alpha-aminooxiraneoctanoyl-D-prolyl); Cyclo(L-alanyl-D-alanyl-(alphaS,2S)-alpha-amino-eta-oxooxiraneoctanoyl-D-prolyl); (3S,6R,9S,12R)-6,9-dimethyl-3-[6-(oxiran-2-yl)-6-oxohexyl]-1,4,7,10-tetrazabicyclo[10.3.0]pentadecane-2,5,8,11-tetrone
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| SK-7068 | Preclinical | [11] | ||
| Synonyms |
N-[[4-[(E)-2-(hydroxycarbamoyl)ethenyl]phenyl]methyl]-4-pyrrolidin-1-yl-benzamide
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| Scriptaid | Preclinical | [11] | ||
| Synonyms |
CGK1026; IN1099; SB-556629; GNF-PF-2024; N-Hydroxy-1,3-dioxo-1H-benz(de)isoquinoline-2(3H)-hexan amide; 6-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-hexanoic acid hydroxyamide; 6-(1,3-Dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)-N-hydroxyhexanamide; 6-(1,3-dioxobenzo[de]isoquinolin-2-yl)-N-hydroxyhexanamide
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | Ki = 1.5 nM | |||
| External Link | ||||
| 4SC-202 | Preclinical | [9] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Chlamydocin | Preclinical | [11] | ||
| Synonyms |
HDInhib_000038; Cyclic(2-methylalanyl-L-phenylalanyl-D-propyl-L-alpha-amino-eta-oxooxiraneoctanoyl); (3S,9S,12R)-3-benzyl-6,6-dimethyl-9-[6-[(2S)-oxiran-2-yl]-6-oxohexyl]-1,4,7,10-tetrazabicyclo[10.3.0]pentadecane-2,5,8,11-tetrone; (3s,9s,14ar)-9-benzyl-6,6-dimethyl-3-{6-[(2s)-oxiran-2-yl]-6-oxohexyl}decahydropyrrolo[1,2-a][1,4,7,10]tetraazacyclododecine-1,4,7,10-tetrone
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| SK-7041 | Preclinical | [11] | ||
| Synonyms |
IN-2001; 4-(dimethylamino)-N-[[4-[(E)-3-(hydroxyamino)-3-oxoprop-1-enyl]phenyl]methyl]benzamide
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| Depudecin | Preclinical | [11] | ||
| Synonyms |
(1R)-1-[(2S,3S)-3-[(E)-2-[(3S)-3-[(1R)-1-hydroxyethyl]oxiran-2-yl]ethenyl]oxiran-2-yl]prop-2-en-1-ol; 139508-73-9
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| Oxamflatin | Terminated | [11] | ||
| Synonyms |
NSC729360; CHEBI:258842; I14-11718; NCGC00165855-01; (2E)-5-(3-(phenylsulfonylamino)phenyl)pent-2-ene-4-ynohydroxamic acid; (2E)-5-[3-(Phenylsulfonylamino)phenyl]pent-2-en-4-ynohydroxamic Acid; (E)-5-[3-(benzenesulfonamido)phenyl]-N-hydroxypent-2-en-4-ynamide; 151720-43-3
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| 6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide | Investigative | [18] | ||
| Synonyms |
UNII-2OJV8MB11B; EX-2; 2OJV8MB11B; CHEMBL1083439; 851365-34-9; Benzamide, N-(((6-(hydroxyamino)-6-oxohexyl)amino)carbonyl)-; Benzamide, N-[[[6-(hydroxyamino)-6-oxohexyl]amino]carbonyl]-; SCHEMBL4258321; CTK2I4390; DTXSID80234280; VQLQZMGNGMOMPU-UHFFFAOYSA-N; BDBM50319235
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | Ki = 16 nM | |||
| External Link | ||||
| N,8-dihydroxy-8-(naphthalen-2-yl)octanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL319738; SCHEMBL3382032; JWCSCYWHCCHTEF-UHFFFAOYSA-N; BDBM50114820; N-Hydroxy-8-hydroxy-8-(2-naphthyl)octanamide; 8-Hydroxy-8-naphthalen-2-yl-octanoic acid hydroxyamide
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 35 nM | |||
| External Link | ||||
| N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide | Investigative | [20] | ||
| Synonyms |
CHEMBL216292; SCHEMBL5903988
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 1130 nM | |||
| External Link | ||||
| N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL98911; SCHEMBL3378753; BDBM50114831; 8-Oxo-8-pyridin-3-yl-octanoic acid hydroxyamide
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 153 nM | |||
| External Link | ||||
| NSC-746457 | Investigative | [21] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 104 nM | |||
| External Link | ||||
| 4-Benzenesulfonylamino-N-hydroxy-benzamide | Investigative | [22] | ||
| Synonyms |
CHEMBL98345; SCHEMBL15480538; BDBM50105682; N-hydroxy-4-(phenylsulfonamido)benzamide; 4-(Phenylsulfonylamino)benzohydroximic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | EC50 = 5000 nM | |||
| External Link | ||||
| N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL320909; SCHEMBL1520961; AQLMJRZLPWGPGD-UHFFFAOYSA-N; BDBM50114827; N-Hydroxy-6-(2-naphthoyl)hexanamide; 7-Naphthalen-2-yl-7-oxo-heptanoic acid hydroxyamide
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | IC50 = 35 nM | |||
| External Link | ||||
| 4-tert-butyl-N-hydroxybenzamide | Investigative | [23] | ||
| Synonyms |
62034-73-5; CHEMBL249284; Benzamide, 4-(1,1-dimethylethyl)-N-hydroxy-; p-tert-butyl benzohydroxamic acid; Oprea1_740446; SCHEMBL5696343; 4-tert-Butylbenzhydroxamic Acid; 4-tert-Butylbenzohydroxamic acid; CTK2C8432; DTXSID80613051; BDBM50215019; 4-(tert-butyl )-benzhydroxamic acid; ZINC19478595; AKOS000181279
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 715 nM | |||
| External Link | ||||
| N-hydroxy-7-(naphthalen-2-yloxy)heptanamide | Investigative | [24] | ||
| Synonyms |
CHEMBL217083
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.9 nM | |||
| External Link | ||||
| 8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide | Investigative | [18] | ||
| Synonyms |
CHEMBL1083441; SCHEMBL4928514; WUKFQTZVXXYEAB-UHFFFAOYSA-N
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 8280 nM | |||
| External Link | ||||
| N-hydroxy-8-(naphthalen-2-yl)non-8-enamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95535; SCHEMBL3382075; BDBM50114823; 8-Naphthalen-2-yl-non-8-enoic acid hydroxyamide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 8 nM | |||
| External Link | ||||
| N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide | Investigative | [20] | ||
| Synonyms |
CHEMBL216509; SCHEMBL5903774; BDBM50198477
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 243 nM | |||
| External Link | ||||
| N-hydroxy-5-phenylthiophene-2-carboxamide | Investigative | [20] | ||
| Synonyms |
CHEMBL217573; SCHEMBL5903684
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 900 nM | |||
| External Link | ||||
| Azithromycin-N-benzyltriazolyldecahydroxamic Acid | Investigative | [25] | ||
| Synonyms |
CHEMBL496761; SCHEMBL14328159; BDBM27184; triazole-linked azithromycin-based compound, 16h
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide | Investigative | [24] | ||
| Synonyms |
CHEMBL265479
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| MOA | Inhibitor | |||
| Activity | IC50 = 18.8 nM | |||
| External Link | ||||
| 8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95313; SCHEMBL1520838; BDBM50114816; 8-Biphenyl-4-yl-8-oxo-octanoic acid hydroxyamide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide | Investigative | [20] | ||
| Synonyms |
CHEMBL217816; SCHEMBL5903934
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 1260 nM | |||
| External Link | ||||
| Gymnochrome E | Investigative | [26] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 10900 nM | |||
| External Link | ||||
| N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide | Investigative | [19] | ||
| Synonyms |
CHEMBL451182; SCHEMBL3382916; SCHEMBL3382922; PGGPUSMJSOKMEA-XBXARRHUSA-N; ZINC13474418; BDBM50114829; (E)-N-Hydroxy-8-(2-naphthyl)-7-octenamide; 8-Naphthalen-2-yl-oct-7-enoic acid hydroxyamide; (E)-8-Naphthalen-2-yl-oct-7-enoic acid hydroxyamide
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 6 nM | |||
| External Link | ||||
| N-hydroxybenzo[b]thiophene-2-carboxamide | Investigative | [27] | ||
| Synonyms |
CHEMBL245946; 211172-97-3; Benzo[b]thiophene-2-carboxamide, N-hydroxy-; SCHEMBL999904; CTK0J7987; DTXSID40470925; BDBM50216024; benzothiophene-2-carbohydroxamic acid
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 670 nM | |||
| External Link | ||||
| 7-(1H-indol-5-yloxy)-N-hydroxyheptanamide | Investigative | [24] | ||
| Synonyms |
CHEMBL426516
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 3.6 nM | |||
| External Link | ||||
| 8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL319070; SCHEMBL3382402; RFYYZRFJBNAHCG-UHFFFAOYSA-N; BDBM50114817; n-hydroxy-7-(4-bromobenzoyl)heptanamide; 8-(4-Bromo-phenyl)-8-oxo-octanoic acid hydroxyamide
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 45 nM | |||
| External Link | ||||
| N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95990; SCHEMBL1521117; NIGGAQZXTHMKPL-UHFFFAOYSA-N; BDBM50114822; N-Hydroxy-6-(4-methoxybenzoyl)hexanamide; 7-(4-Methoxy-phenyl)-7-oxo-heptanoic acid hydroxyamide
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 450 nM | |||
| External Link | ||||
| N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95885; SCHEMBL3382183; BDBM50114815; 8-(2-Methoxy-phenyl)-8-oxo-octanoic acid hydroxyamide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 95 nM | |||
| External Link | ||||
| N-hydroxy-6-oxo-6-phenylhexanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95152; SCHEMBL1521154; BDBM50114819; 6-Oxo-6-phenyl-hexanoic acid hydroxyamide
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 1500 nM | |||
| External Link | ||||
| N-hydroxy-8-(naphthalen-2-yl)octanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95747; SCHEMBL3378763; KWFDCRKEDDNSLQ-UHFFFAOYSA-N; N-Hydroxy-8-(2-naphthyl)octanamide; BDBM50114833; ZINC13474419; 8-Naphthalen-2-yl-octanoic acid hydroxyamide
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| MOA | Inhibitor | |||
| Activity | IC50 = 25 nM | |||
| External Link | ||||
| ADS-102550 | Investigative | [20] | ||
| Synonyms |
CHEMBL217716; SCHEMBL5903759; BDBM50198218
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 29 nM | |||
| External Link | ||||
| N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95835; SCHEMBL3383312; LIOTZVIDBXLBAC-UHFFFAOYSA-N; n-hydroxy-7-(p-anisoyl)heptanamide; BDBM50114826; 8-(4-Methoxy-phenyl)-8-oxo-octanoic acid hydroxyamide
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 15 nM | |||
| External Link | ||||
| N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide | Investigative | [28] | ||
| Synonyms |
CHEMBL238569; SCHEMBL1064835
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| MOA | Inhibitor | |||
| Activity | IC50 = 1000 nM | |||
| External Link | ||||
| N-hydroxy-2,2'-bithiophene-5-carboxamide | Investigative | [20] | ||
| Synonyms |
CHEMBL217750; SCHEMBL5903723; BDBM50198479
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 2500 nM | |||
| External Link | ||||
| ADS-100380 | Investigative | [20] | ||
| Synonyms |
CHEMBL216885; SCHEMBL5904027; BDBM50198221
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 750 nM | |||
| External Link | ||||
| N-hydroxy-7-oxo-7-phenylheptanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL95916; SCHEMBL1521257; BDBM50114832; 7-Oxo-7-phenyl-heptanoic acid hydroxyamide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 500 nM | |||
| External Link | ||||
| 7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide | Investigative | [18] | ||
| Synonyms |
CHEMBL1083440; SCHEMBL4922807
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 145 nM | |||
| External Link | ||||
| SK-683 | Investigative | [29] | ||
| Synonyms |
CHEMBL116620; SCHEMBL8089576; BDBM50148757
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 1 nM | |||
| External Link | ||||
| N-hydroxy-9-oxo-9-phenylnonanamide | Investigative | [19] | ||
| Synonyms |
CHEMBL99810; SCHEMBL1521077; BDBM50114824; 9-Oxo-9-phenyl-nonanoic acid hydroxyamide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 135 nM | |||
| External Link | ||||
| N-Hydroxy-N'-(4-methylphenyl)octanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1092762; BDBM50314138
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 76 nM | |||
| External Link | ||||
| N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093043; BDBM50314143
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-(2-aminophenyl)quinoxaline-6-carboxamide | Investigative | [31] | ||
| Synonyms |
benzamide-type inhibitor, 20; CHEMBL236060; BDBM19424
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 2000 nM | |||
| External Link | ||||
| 7-Biphenyl-4-yl-heptanoic acid hydroxyamide | Investigative | [32] | ||
| Synonyms |
CHEMBL125098; BDBM50222335; 7-(4-Biphenylyl)heptanehydroximic acid
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-(2-Ethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093040; BDBM50314142
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid | Investigative | [33] | ||
| Synonyms |
CHEMBL115049; 436150-72-0; SCHEMBL7368556; CTK1D2674; DTXSID40658342; BDBM50221807; 8-[([1,1'-Biphenyl]-4-yl)oxy]-2-oxooctanoic acid; Octanoic acid, 8-([1,1'-biphenyl]-4-yloxy)-2-oxo-
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 1,1,1-Trifluoro-8-phenoxy-octan-2-one | Investigative | [34] | ||
| Synonyms |
CHEMBL114796; BDBM50217940
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|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-(Biphenyl-4-yloxy)-heptanoic acid hydroxyamide | Investigative | [33] | ||
| Synonyms |
CHEMBL114184; SCHEMBL3383144
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1092032; BDBM50314141
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-Phenoxy-heptanoic acid hydroxyamide | Investigative | [32] | ||
| Synonyms |
CHEMBL124322; N-hydroxy-7-phenoxyheptanamide; 7-Phenoxyheptanehydroximic acid
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one | Investigative | [34] | ||
| Synonyms |
CHEMBL117916; SCHEMBL7366611; BDBM50217945
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| MOA | Inhibitor | |||
| External Link | ||||
| 6-(9H-carbazol-9-yl)-N-hydroxyhexanamide | Investigative | [35] | ||
| Synonyms |
CHEMBL1290142; A1-02262; SCHEMBL1004139; SOMDVJCUFVPZKM-UHFFFAOYSA-N; BDBM50331109; 9H-Carbazole-9-hexanamide, N-hydroxy-; 6-Carbazol-9-ylhexanoic acid hydroxyamide; US8748451, 1
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 3074 nM | |||
| External Link | ||||
| Desclasinose Azithromycinarylalkyl Hydroxamate | Investigative | [25] | ||
| Synonyms |
CHEMBL454025; SCHEMBL14329692; BDBM27176; Desclasinose Azithromycinarylalkyl Hydroxamate, 10
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| MOA | Inhibitor | |||
| External Link | ||||
| N-(4-Ethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093042; BDBM50314139
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093713; BDBM50314133
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide | Investigative | [36] | ||
| Synonyms |
CHEMBL473270
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | IC50 = 9 nM | |||
| External Link | ||||
| N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093357; BDBM50314144
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|
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| MOA | Inhibitor | |||
| External Link | ||||
| Azithromycin-N-benzyltriazolyloctahydroxamic Acid | Investigative | [25] | ||
| Synonyms |
SCHEMBL8976909; CHEMBL455342; BDBM27181; triazole-linked azithromycin-based compound, 16e
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| N-(4-hydroxybiphenyl-3-yl)benzamide | Investigative | [37] | ||
| Synonyms |
CHEMBL269935; SCHEMBL5724398; BDBM50232005
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | IC50 = 58 nM | |||
| External Link | ||||
| AZUMAMIDE E | Investigative | [38] | ||
| Synonyms |
CHEMBL402363
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|
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| MOA | Inhibitor | |||
| Activity | IC50 = 50 nM | |||
| External Link | ||||
| Azithromycin-N-benzyltriazolylnonahydroxamic Acid | Investigative | [25] | ||
| Synonyms |
CHEMBL509089; SCHEMBL14329756; BDBM27183; triazole-linked azithromycin-based compound, 16g
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-N'-(3-methylphenyl)octanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1089339; BDBM50314136
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | IC50 = 57 nM | |||
| External Link | ||||
| 8-Phenyl-octanoic acid hydroxyamide | Investigative | [32] | ||
| Synonyms |
CHEMBL123624; N-Hydroxy-8-phenyloctanamide; SCHEMBL5807174
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| Azithromycin-N-benzyltriazolylhexahydroxamic Acid | Investigative | [25] | ||
| Synonyms |
CHEMBL446811; SCHEMBL14328156; CHEMBL3735805; BDBM27177; triazole-linked azithromycin-based compound, 16a
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| N-(3-Ethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093041; BDBM50314134
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093359; BDBM50314135
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-N'-(4-methoxyphenyl)octanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1091487; BDBM50314137
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|
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| MOA | Inhibitor | |||
| Activity | IC50 = 71 nM | |||
| External Link | ||||
| AZUMAMIDE B | Investigative | [38] | ||
| Synonyms |
CHEMBL402727
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|
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| MOA | Inhibitor | |||
| Activity | IC50 = 1830 nM | |||
| External Link | ||||
| 8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one | Investigative | [34] | ||
| Synonyms |
CHEMBL116023; SCHEMBL7368359; BDBM50218558
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| Azithromycinarylalkylhydroxamic Acid | Investigative | [25] | ||
| Synonyms |
CHEMBL510806; SCHEMBL14329660; BDBM27175; Azithromycinarylalkylhydroxamic Acid, 8
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-N'-(2-methylphenyl)octanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1076794; BDBM50314140
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| MOA | Inhibitor | |||
| Activity | IC50 = 576 nM | |||
| External Link | ||||
| nexturastat A | Investigative | [39] | ||
| Synonyms |
S7473
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 360 nM | |||
| External Link | ||||
| AZUMAMIDE C | Investigative | [38] | ||
| Synonyms |
CHEMBL257972
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|
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| MOA | Inhibitor | |||
| Activity | Ki = 20 nM | |||
| External Link | ||||
| N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide | Investigative | [30] | ||
| Synonyms |
CHEMBL1093358; BDBM50314145
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| MOA | Inhibitor | |||
| External Link | ||||
| N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide | Investigative | [40] | ||
| Synonyms |
CHEMBL511212; BDBM50258645
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| MOA | Inhibitor | |||
| Activity | IC50 = 3 nM | |||
| External Link | ||||
| LARGAZOLE | Investigative | [41] | ||
| Synonyms |
CHEMBL1173445; (+)-Largazole; SCHEMBL71330; ZINC56861395
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|
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| MOA | Inhibitor | |||
| Activity | IC50 = 10.09 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL393260
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| MOA | Inhibitor | |||
| Activity | IC50 = 36 nM | |||
| External Link | ||||
| 7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide | Investigative | [43] | ||
| Synonyms |
CHEMBL419758; NCH-31; JMC505425 Compound 7; BDBM19131; 7-mercapto-N-(4-phenyl-2-thiazolyl)heptanamide; N-(4-phenyl-1,3-thiazol-2-yl)-7-sulfanylheptanamide
Click to Show/Hide
|
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| MOA | Inhibitor | |||
| Activity | IC50 = 48 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL390991
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 2.7 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL394261
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| MOA | Inhibitor | |||
| Activity | IC50 = 2 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL391384
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 5.3 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL393261
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| MOA | Inhibitor | |||
| Activity | IC50 = 170 nM | |||
| External Link | ||||
| N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide | Investigative | [40] | ||
| Synonyms |
CHEMBL512644; SCHEMBL8226957
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| MOA | Inhibitor | |||
| Activity | IC50 = 33 nM | |||
| External Link | ||||
| N-(2-aminophenyl)nicotinamide | Investigative | [37] | ||
| Synonyms |
N-(2-Amino-phenyl)-nicotinamide; 436089-31-5; N-(2-aminophenyl)pyridine-3-carboxamide; CHEMBL236678; AC1LMN6K; SCHEMBL18086514; CTK4I7538; DTXSID50360661; CHEBI:125506; ZINC873967; BDBM50220259; 3463AE; AKOS000129725; RTR-042156; MCULE-7933541910; N-(2-aminophenyl)-3-pyridylcarboxamide; ZB014940; ACM436089315; ST086607; ASN 01337807; KB-298440; TR-042156; BC4148434; SR-01000329900; SR-01000329900-1; BRD-K20880473-001-04-6
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 2600 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL241555
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 3.2 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL428737
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 88 nM | |||
| External Link | ||||
| N-(4-aminobiphenyl-3-yl)nicotinamide | Investigative | [37] | ||
| Synonyms |
CHEMBL255805; BDBM50232035
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 48 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) | Investigative | [42] | ||
| Synonyms |
CHEMBL238587
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| MOA | Inhibitor | |||
| Activity | IC50 = 4.7 nM | |||
| External Link | ||||
| N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide | Investigative | [37] | ||
| Synonyms |
CHEMBL256440; SCHEMBL1066609
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 65 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL238596; BDBM50222727
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 94 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL393961
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 6.4 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL391383
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| MOA | Inhibitor | |||
| Activity | IC50 = 6.2 nM | |||
| External Link | ||||
| N-(2-aminophenyl)-4-methoxybenzamide | Investigative | [31] | ||
| Synonyms |
AC1LFX2W; Cambridge id 5129152; Oprea1_722128; benzamide-type inhibitor, 22; CHEMBL236061; SCHEMBL5226034; BDBM19426; CTK7A1998; MolPort-001-019-504; BDYVCYUXCNZYRW-UHFFFAOYSA-N; ZINC281656; STK156256; AKOS000130378; MCULE-9183453747; N-(2-Amino-phenyl)4-methoxy-benzamide; N-(2-amino-phenyl)-4-methoxy-benzamide; NCGC00240897-01; N1-(4-methoxybenzoyl)-1,2-benzenediamine; N1-(4-methoxy-benzoyl)-1,2-benzenediamine; ST50908739; N-(2-aminophenyl)(4-methoxyphenyl)carboxamide; SR-01000196394
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 2000 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL393464
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 3.7 nM | |||
| External Link | ||||
| Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) | Investigative | [42] | ||
| Synonyms |
CHEMBL238829; BDBM50222732
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 3.9 nM | |||
| External Link | ||||
| 4-Phenylbutyrohydroxamic acid | Investigative | [44] | ||
| Synonyms |
N-Hydroxy-4-phenylbutanamide; 32153-46-1; NSC131300; UNII-QX182FOM5S; QX182FOM5S; 4-phenylbutanehydroxamic acid; CHEMBL55895; Benzenebutanamide, N-hydroxy-; NSC 131300; AC1Q7DIW; AC1L5RDX; Phenylbutyrylhydroxamic Acid; AC1Q5QD1; N-Hydroxy-4-phenyl-butyramide; 4-Phenylbutyryl hydroxamic acid; SCHEMBL1350853; CTK4G8310; DTXSID60185943; MolPort-011-492-164; UPHXPXYRKPCXHK-UHFFFAOYSA-N; ZINC4962622; STL301752; BDBM50015142; AKOS009266186; MCULE-9765156954; NSC-131300; NE28489; BCB03_000829; EN300-68596
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | Ki = 295 nM | |||
| External Link | ||||
| 8-Oxo-8-phenyl-octanoic acid hydroxyamide | Investigative | [45] | ||
| Synonyms |
CHEMBL95959; SCHEMBL3383197; N-hydroxy-8-oxo-8-phenyloctanamide
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 65 nM | |||
| External Link | ||||
| ST-3050 | Investigative | [46] | ||
| Synonyms |
CHEMBL472631; SCHEMBL3445133; SCHEMBL3445139; BDBM50278222
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|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 3060 nM | |||
| External Link | ||||
| Octanedioic acid bis-hydroxyamide | Investigative | [47] | ||
| Synonyms |
Suberohydroxamic acid
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 19 nM | |||
| External Link | ||||
| ST-2986 | Investigative | [46] | ||
| Synonyms |
CHEMBL471041; SCHEMBL3444455; BDBM50278219
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 5480 nM | |||
| External Link | ||||
| 9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide | Investigative | [34] | ||
| Synonyms |
9,9,9-Trifluoro-8-Oxo-N-Phenylnonanamide; CHEMBL113537; 2gh6; SCHEMBL2702892; KRCXZGYVOZSCSF-UHFFFAOYSA-N; BDBM50121062; DB07553
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| Activity | IC50 = 7800 nM | |||
| External Link | ||||
| 7-Mercapto-heptanoic acid phenylamide | Investigative | [48] | ||
| Synonyms |
Thiol-SAHA (t-SAHA); CHEMBL325676; SCHEMBL14821761; BDBM152692
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| Activity | IC50 = 218 nM | |||
| External Link | ||||
| 6-benzenesulfinylhexanoic acid hydroxamide | Investigative | [49] | ||
| Synonyms |
6-(benzenesulfinyl)hexanoic acid hydroxyamide; 875737-03-4
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-(2-Mercapto-ethyl)-N'-phenyl-succinamide | Investigative | [50] | ||
| Synonyms |
CHEMBL193959
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|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-Mercapto-heptanoic acid biphenyl-4-ylamide | Investigative | [48] | ||
| Synonyms |
CHEMBL112311
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-phenylacetylamino-benzamide | Investigative | [51] | ||
| Synonyms |
CHEMBL356824; 656261-23-3; SCHEMBL675578; CTK1J6158; DTXSID40458440; ZINC13533297; AKOS030583151; Benzeneacetamide, N-[4-[(hydroxyamino)carbonyl]phenyl]-
Click to Show/Hide
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|||
| MOA | Inhibitor | |||
| External Link | ||||
| 6-(2-Bromo-acetylamino)-hexanoic acid phenylamide | Investigative | [48] | ||
| Synonyms |
CHEMBL344920; 651767-99-6; SCHEMBL3736839; CTK1J8444; DTXSID50432973; HWYLREOMBVUGJQ-UHFFFAOYSA-N; BDBM50222416; ZINC13587789; AKOS030603042; N-Phenyl-6-(bromoacetylamino)hexanamide; Hexanamide, 6-[(bromoacetyl)amino]-N-phenyl-
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide | Investigative | [52] | ||
| Synonyms |
CHEMBL143674; SCHEMBL673760
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|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one | Investigative | [53] | ||
| Synonyms |
CHEMBL126355; BDBM50222394
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| Octanedioic acid hydroxyamide pyridin-4-ylamide | Investigative | [54] | ||
| Synonyms |
SCHEMBL8082656; CHEMBL165162; ZINC13472304
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-(6-Mercapto-hexyl)-benzamide | Investigative | [48] | ||
| Synonyms |
CHEMBL112364; BDBM50223650
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|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide | Investigative | [54] | ||
| Synonyms |
CHEMBL167455
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide | Investigative | [51] | ||
| Synonyms |
SCHEMBL675474
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 6-benzenesulfonylhexanoic acid hydroxamide | Investigative | [49] | ||
| Synonyms |
CHEMBL203207
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one | Investigative | [34] | ||
| Synonyms |
SCHEMBL7373122; CHEMBL116578
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester | Investigative | [48] | ||
| Synonyms |
CHEMBL111806; SCHEMBL14812153
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|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 4-Butyrylamino-N-hydroxy-benzamide | Investigative | [52] | ||
| Synonyms |
CHEMBL142254; 656261-22-2; Benzamide, N-hydroxy-4-[(1-oxobutyl)amino]-; SCHEMBL675234; CTK1J6159; DTXSID90461262
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one | Investigative | [53] | ||
| Synonyms |
CHEMBL127328
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-Mercapto-heptanoic acid biphenyl-3-ylamide | Investigative | [48] | ||
| Synonyms |
CHEMBL320323
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione | Investigative | [55] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide | Investigative | [51] | ||
| Synonyms |
SCHEMBL676079
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide | Investigative | [48] | ||
| Synonyms |
CHEMBL324126
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-Mercapto-heptanoic acid pyridin-3-ylamide | Investigative | [48] | ||
| Synonyms |
CHEMBL332246; Heptanamide, 7-mercapto-N-3-pyridinyl-; BDBM50223653
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 6-Phenoxy-hexane-1-thiol | Investigative | [48] | ||
| Synonyms |
CHEMBL109796; 6-phenoxyhexane-1-thiol; 1-Hexanethiol, 6-phenoxy-; SCHEMBL5679745; MolPort-020-180-823; BDBM50223652; AKOS018584222; MCULE-9521857089
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 4-Benzoylamino-N-hydroxy-benzamide | Investigative | [51] | ||
| Synonyms |
SCHEMBL673678; CHEMBL191227
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide | Investigative | [45] | ||
| Synonyms |
CHEMBL143734; NSC718168; AC1L8L82; SCHEMBL13039735; ZINC5579677; BDBM50082664; NSC-718168; NCI60_040737; 6-(4-Chlorobenzoylamino)hexanehydroxamic acid
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one | Investigative | [34] | ||
| Synonyms |
CHEMBL112148; SCHEMBL7364383; BDBM50218532
Click to Show/Hide
|
|||
| MOA | Inhibitor | |||
| External Link | ||||
| 7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one | Investigative | [53] | ||
| Synonyms |
CHEMBL127351; SCHEMBL7365180; HWZHDGRMABBYOV-UHFFFAOYSA-N; BDBM50222367; 7-((1,1'-biphenyl)-3-yloxy)-1-(1 ,3-oxazol-2-yl)-1-heptanone
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| MOA | Inhibitor | |||
| External Link | ||||
| 6-Mercapto-hexanoic acid phenylamide | Investigative | [48] | ||
| Synonyms |
CHEMBL109654; Hexanamide, 6-mercapto-N-phenyl-; SCHEMBL14254925; BDBM50027600
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| MOA | Inhibitor | |||
| Activity | IC50 = 791 nM | |||
| External Link | ||||
| Cyclostellettamine derivative | Investigative | [56] | ||
| Synonyms |
CHEMBL88332
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| MOA | Inhibitor | |||
| External Link | ||||
| N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide | Investigative | [45] | ||
| Synonyms |
CHEMBL139999; SCHEMBL1232700; BDBM50082661; ZINC13472309
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| MOA | Inhibitor | |||
| External Link | ||||
| 5-Mercapto-pentanoic acid phenylamide | Investigative | [48] | ||
| Synonyms |
N-Phenyl-5-mercaptovaleramide; CHEMBL114344; Pentanamide, 5-mercapto-N-phenyl-
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| MOA | Inhibitor | |||
| External Link | ||||
| Octanedioic acid hydroxyamide pyridin-2-ylamide | Investigative | [54] | ||
| Synonyms |
SCHEMBL8090513; CHEMBL164872; ZINC13472303
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| MOA | Inhibitor | |||
| External Link | ||||
| N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide | Investigative | [50] | ||
| Synonyms |
CHEMBL193979
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-(methylsulfonylthio)ethyl 2-propylpentanoate | Investigative | [55] | ||
| Synonyms |
CHEMBL271677; SCHEMBL4156413
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| MOA | Inhibitor | |||
| External Link | ||||
| (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one | Investigative | [53] | ||
| Synonyms |
CHEMBL126465; SCHEMBL7368197; SCHEMBL7368201
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide | Investigative | [51] | ||
| Synonyms |
SCHEMBL676080
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide | Investigative | [57] | ||
| Synonyms |
N-hydroxy-4-(3-phenylpropanamido)benzamide
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide | Investigative | [51] | ||
| Synonyms |
SCHEMBL7311087
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| MOA | Inhibitor | |||
| External Link | ||||
| 8-Oxo-8-phenyl-octanoic acid | Investigative | [54] | ||
| Synonyms |
8-Oxo-8-phenyloctanoic acid; 7-Benzoylheptanoic acid; 24314-23-6; Benzeneoctanoic acid, h-oxo-; 7-BENZOYL HEPTANOIC ACID; AC1L6TSB; SCHEMBL3381106; 8-keto-8-phenyl-caprylic acid; CHEMBL162423; 8-Oxo-8-phenyloctanoic acid #; CTK4F3363; DTXSID40305602; UMCSRRHQLAVYRS-UHFFFAOYSA-N; ZINC2168376; 7009f; NSC171230; AKOS016022495; NSC-171230; MCULE-7202530747; ACM24314236; ST50825837
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide | Investigative | [51] | ||
| Synonyms |
CHEMBL143336; 656261-24-4; SCHEMBL674421; CTK1J6157; DTXSID30433908; ZINC13533300; AKOS030583673; n-hydroxy-4-(4-phenylbutyryl-amino)benzamide; Benzenebutanamide, N-[4-[(hydroxyamino)carbonyl]phenyl]-
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| 6-phenylsulfanylhexanoic acid hydroxamide | Investigative | [49] | ||
| Synonyms |
Hexanamide, N-hydroxy-6-(phenylthio)-; CHEMBL203028; SCHEMBL7317658
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| MOA | Inhibitor | |||
| External Link | ||||
| ST-2987 | Investigative | [46] | ||
| Synonyms |
CHEMBL471042; SCHEMBL3444989; SCHEMBL3444984; BDBM50278220
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| MOA | Inhibitor | |||
| Activity | IC50 = 790 nM | |||
| External Link | ||||
| 7-Mercapto-heptanoic acid quinolin-3-ylamide | Investigative | [48] | ||
| Synonyms |
CHEMBL112234
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| MOA | Inhibitor | |||
| External Link | ||||
| 5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide | Investigative | [58] | ||
| Synonyms |
CHEMBL84288
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| MOA | Inhibitor | |||
| External Link | ||||
| 8-Mercapto-octanoic acid phenylamide | Investigative | [48] | ||
| Synonyms |
8-mercapto-N-phenyloctanamide; CHEMBL326433; ZINC13609343
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| MOA | Inhibitor | |||
| Activity | IC50 = 294 nM | |||
| External Link | ||||
| N-(6-Hydroxycarbamoyl-hexyl)-benzamide | Investigative | [54] | ||
| Synonyms |
CHEMBL57107; 174664-71-2; SCHEMBL573254; CTK0A7470; DTXSID00433435; BDBM50220823; ZINC13490043; 7-(Benzoylamino)heptanehydroxamic acid; AKOS030580013; Benzamide, N-[7-(hydroxyamino)-7-oxoheptyl]-
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| MOA | Inhibitor | |||
| External Link | ||||
| 7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one | Investigative | [34] | ||
| Synonyms |
CHEMBL326529; SCHEMBL7365237; BDBM50217957
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| MOA | Inhibitor | |||
| External Link | ||||
| 7-Mercapto-heptanoic acid benzothiazol-2-ylamide | Investigative | [48] | ||
| Synonyms |
CHEMBL178779
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| MOA | Inhibitor | |||
| External Link | ||||
| N-Hydroxy-4-(pentanoylamino-methyl)-benzamide | Investigative | [52] | ||
| Synonyms |
CHEMBL143102
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| MOA | Inhibitor | |||
| External Link | ||||
| PSAMMAPLIN A | Investigative | [45] | ||
| Synonyms |
110659-91-1; Bisprasin; NSC614495; AC1O46WI; SCHEMBL364511; ZINC150352860; NSC-614495; B723735K022; J-002461; Benzenepropanamide, N,N'-(dithiodi-2,1-ethanediyl)bis(3-bromo-4-hydroxy-alpha-(hydroxyimino)-
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| Poly [ADP-ribose] polymerase 1 (PARP1) | 131 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Nicotinamide | Approved | [59] | ||
| Synonyms |
Aminicotin; Amixicotyn; Amnicotin; Benicot; Dipegyl; Endobion; Enduramide; Hansamid; Mediatric; Niacevit; Niacinamide; Niacotinamide; Niamide; Nicamina; Nicamindon; Nicasir; Nicobion; Nicofort; Nicogen; Nicomidol; Nicosylamide; Nicota; Nicotamide; Nicotilamide; Nicotililamido; Nicotinamid; Nicotinamida; Nicotinamidum; Nicotinsaeureamid; Nicotinsaureamid; Nicotol; Nicotylamide; Nicotylamidum; Nicovit; Nicovitina; Nicovitol; Nicozymin; Nikasan; Nikazan; Nikotinamid; Nikotinsaeureamid; Niocinamide; Niozymin; Papulex; Pelmin; Pelmine; Savacotyl; Amid kyseliny nikotinove; Amid kyseliny nikotinove [Czech]; Amide PP; Astra Brand of Niacinamide; Austrovit PP; Delonin amide; Factor pp; Inovitan PP; Jenapharm Brand of Niacinamide; Merck Brand of Niacinamide; Niacinamide Astra Brand; Niacinamide Jenapharm Brand; Niacinamide Merck Brand; Niacinamide Pharmagenix Brand; Niacinamide [USAN]; Niavit PP; Nicotine acid amide; Nicotine amide; Nicotinic acid amide; Nicotinic amide; Nicotinsaureamid Jenapharm; Nicotinsaureamid [German]; Nikotinsaeureamid [German]; Pelonin amide; Pharmagenix Brand of Niacinamide; Vitamin B; Vitamin PP; Witamina PP; Nicosan 2; Vitamin H1; B 3, Vitamin; B3, Vitamin; Beta-Pyridinecarboxamide; Jenapharm, Nicotinsaureamid; Nandervit-N; Niacin-Vitamin B3; Niacinamide (USP); Nicotinamida [INN-Spanish]; Nicotinamide (Niacinamide); Nicotinamidum [INN-Latin]; Niko-tamin; PP-Faktor; Vi-Nicotyl; Vitamin B (VAN); M-(Aminocarbonyl)pyridine; Niacinamide, Nicotinic acid amide, Nicotinamide; Nicotinamide (JP15/INN); Nicotinamide, niacin, vitamin B3; Nicotinamide-carbonyl-14C; Pyridine-3-carboxamide; Pyridine-3-carboxylic acid amide; 3 Pyridinecarboxamide; 3-Carbamoylpyridine; 3-Pyridinecarboxamide; 3-Pyridinecarboxylic acid amide
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| MOA | Binder | |||
| Activity | IC50 = 210000 nM | |||
| External Link | ||||
| KU-0058948 | Approved | [60] | ||
| Synonyms |
CHEMBL380648; 4-[3-(1,4-diazepan-1-ylcarbonyl)-4-fluorobenzyl]phthalazin-1(2H)-one; 4-(3-(1,4-diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one; Homopiperazine analogue, 14; SCHEMBL864319; BDBM27533; HGEPGGJUGUMFHT-UHFFFAOYSA-N; ZINC3821234; DB08058; NCGC00386677-01; KU-58948; FT-0670691; TL80090044; 4-[3-([1,4]diazepane-1-carbonyl)-4 -fluorobenzyl]-2H-phthalazin-1-one; 4-[3-([1,4]diazepane-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one
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| MOA | Inhibitor | |||
| Activity | IC50 = 7 nM | |||
| External Link | ||||
| Niraparib Tosylate | Approved | [61] | ||
| Synonyms |
1038915-73-9; MK-4827 (tosylate); MK-4827 tosylate; UNII-75KE12AY9U; MK-4827(Niraparib) tosylate; 75KE12AY9U; MK-4827-tosylate; MK 4827 tosylate; Niraparib(MK-4827) tosylate; KS-00000TSH; MolPort-044-556-849; s7625; HY-10619B; AKOS030632785; CS-2283; AC-30383; KB-335358; AX8326059
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| MOA | Modulator | |||
| External Link | ||||
| Nicaraven | Phase 3 | [62] | ||
| Synonyms |
AVS; Antevan; Antevas
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| MOA | Modulator | |||
| External Link | ||||
| CC-486 | Phase 3 | [63] | ||
| Synonyms |
AG-14361; AG14361; 328543-09-5; UNII-48N0U0K50I; AG 14361; CHEMBL65892; 48N0U0K50I; Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-; AG-014361; 1-(4-((dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one; Imidazo(4,5,1-jk)(1,4)benzodiazepin-7(4H)-one, 2-(4-((dimethylamino)methyl)phenyl)-5,6-dihydro-; 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one; SMR000486393; MLS006011157; MLS001065917; Nucleoside analogue
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| MOA | Inhibitor | |||
| Activity | Ki = 5.8 nM | |||
| External Link | ||||
| AG140699 | Phase 2 | [64] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AZD5305 | Phase 2 | [65] | ||
| Synonyms |
16MZ1V3RBT; 2589531-76-8; 2-Pyridinecarboxamide, 5-(4-((7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3-yl)methyl)-1-piperazinyl)-N-methyl-; 2-Pyridinecarboxamide, 5-[4-[(7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methyl-; 5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)-N-methylpicolinamide; 5-[4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methylpicolinamide; 5-[4-[(7-ethyl-6-oxo-5H-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl]-N-methylpyridine-2-carboxamide; 5-{4-[(7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3- yl)methyl]piperazin-1-yl}-N-methylpyridine-2- carboxamide; AC-37130; Azd 5305; AZD 5305 [WHO-DD]; AZD5305; AZD-5305; AZD-5305 [WHO-DD]; CHEMBL5095220; CS-0163534; E80364; EX-A5234; example 4 [WO2021013735]; GTPL11526; HY-132167; MS-26971; NSC834196; NSC-834196; Saruparib; saruparib [INN]; SCHEMBL22912701; SY295016; UNII-16MZ1V3RBT
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| MOA | Inhibitor | |||
| External Link | ||||
| PMID27841036-Compound-37 | Phase 2 | [66] | ||
| Synonyms |
2X-121
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| MOA | Inhibitor | |||
| Activity | IC50 = 2 nM | |||
| External Link | ||||
| Stenoparib | Phase 2 | [67] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AMXI 5001 | Phase 1/2 | [68] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| NMS-03305293 | Phase 1 | [69] | ||
| Synonyms |
NMS-P293
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-6
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| MOA | Inhibitor | |||
| Activity | IC50 = 230 nM | |||
| External Link | ||||
| Benzimidazole carboxamide derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-I
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| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
| External Link | ||||
| PMID27841036-Compound-33 | Patented | [66] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 4 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-9
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| MOA | Inhibitor | |||
| Activity | IC50 = 44 nM | |||
| External Link | ||||
| Phthalazine ketone derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-16
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| MOA | Inhibitor | |||
| Activity | IC50 = 6000 nM | |||
| External Link | ||||
| Quinazolinedione derivative 3 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-13
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| MOA | Inhibitor | |||
| Activity | IC50 = 140 nM | |||
| External Link | ||||
| 4-Carboxamido-isoindolinone derivative 2 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-3
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| MOA | Inhibitor | |||
| Activity | IC50 = 11 nM | |||
| External Link | ||||
| 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 3 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-8
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| MOA | Inhibitor | |||
| Activity | IC50 = 15 nM; Kd < 10 nM | |||
| External Link | ||||
| 7-azaindole derivative 8 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-10
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| MOA | Inhibitor | |||
| Activity | IC50 < 100 nM | |||
| External Link | ||||
| 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 5 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-IV
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| MOA | Inhibitor | |||
| External Link | ||||
| Phthalazine ketone derivative 3 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-18
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| MOA | Inhibitor | |||
| Activity | IC50 = 9000 nM | |||
| External Link | ||||
| Dihydropyrido phthalazinone derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-21
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| MOA | Inhibitor | |||
| Activity | IC50 < 800 nM | |||
| External Link | ||||
| Phthalazine ketone derivative 2 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-17
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| MOA | Inhibitor | |||
| Activity | IC50 = 8000 nM | |||
| External Link | ||||
| Tricyclic indole compound 13 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-XVI
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 to 270 nM | |||
| External Link | ||||
| 3-phenyl isoquinolin-1(2H) derivative 2 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-VII
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-Carboxamido-isoindolinone derivative 5 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-III
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| MOA | Inhibitor | |||
| External Link | ||||
| Quinazolinedione derivative 2 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-12
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.37 nM | |||
| External Link | ||||
| Quinazolinedione derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-11
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.21 nM | |||
| External Link | ||||
| Dihydropyrido phthalazinone derivative 2 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-22
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| MOA | Inhibitor | |||
| Activity | IC50 < 800 nM | |||
| External Link | ||||
| 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 2 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-7
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| MOA | Inhibitor | |||
| Activity | IC50 = 26 nM; Kd < 10 nM | |||
| External Link | ||||
| Phthalazine derivative 3 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-19
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| Tetra-hydro-quinoline derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-VIII
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| MOA | Inhibitor | |||
| Activity | IC50 = 1 to 500 nM | |||
| External Link | ||||
| 4-Carboxamido-isoindolinone derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-2
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| MOA | Inhibitor | |||
| Activity | IC50 = 20 nM | |||
| External Link | ||||
| 4-Carboxamido-isoindolinone derivative 3 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-4
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| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| 4-Carboxamido-isoindolinone derivative 4 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-5
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| MOA | Inhibitor | |||
| Activity | IC50 = 20 nM | |||
| External Link | ||||
| Dihydrodiazepinocarbazolone derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-26
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| MOA | Inhibitor | |||
| Activity | IC50 = 2.9 nM | |||
| External Link | ||||
| Tetra-cyclic pyridophthalazinone derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-25
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| MOA | Inhibitor | |||
| Activity | IC50 = 5.1 nM | |||
| External Link | ||||
| 3-phenyl isoquinolin-1(2H) derivative 1 | Patented | [66] | ||
| Synonyms |
PMID27841036-Compound-20
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| MOA | Inhibitor | |||
| Activity | IC50 < 10 nM | |||
| External Link | ||||
| CPH-102 | Preclinical | [70] | ||
| Synonyms |
IABP; INH2BP, Crimson Pharmaceutical; INH2BP, Octamer; PARP inhibitors, Crimson Pharmaceutical; PARP inhibitors, Octamer; CPH-101, Crimson Pharma
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| MOA | Inhibitor | |||
| External Link | ||||
| PJ34 | Preclinical | [71] | ||
| Synonyms |
344458-19-1; pj-34; N~2~,N~2~-DIMETHYL-N~1~-(6-OXO-5,6-DIHYDROPHENANTHRIDIN-2-YL)GLYCINAMIDE; CHEMBL372303; P34; 2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide; Acetamide, N-(5,6-dihydro-6-oxo-2-phenanthridinyl)-2-(dimethylamino)-; UYJZZVDLGDDTCL-UHFFFAOYSA-N; PJ34(free base); 1xk9; SCHEMBL422317; ZINC8960; AC1L1J45; BDBM27497; CTK1B7701; MolPort-035-395-737; Ibrutinib (PCI32765 pound(c); HMS3651B06; BCP07990; HY-13688A; 2662AH; AKOS030229047; SB19292; DB08348; CS-1463; NCGC00370866-10; DA-42692; BC600341
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| MOA | Inhibitor | |||
| Activity | IC50 = 10.9 nM | |||
| External Link | ||||
| NU1025 | Terminated | [72] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 48 nM | |||
| External Link | ||||
| 3-Ethynylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL501330; 8-Quinolinecarboxamide, 3-ethynyl-; BDBM50255268
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| MOA | Inhibitor | |||
| Activity | IC50 = 2300 nM | |||
| External Link | ||||
| 2-(4-Amino-phenyl)-8-hydroxy-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 289 nM | |||
| External Link | ||||
| N-(4-Phenylthiazol-2-yl)isonicotinamide | Investigative | [75] | ||
| Synonyms |
N-(4-phenyl-1,3-thiazol-2-yl)pyridine-4-carboxamide; CHEMBL482012; 5245-66-9; BAS 03572091; AC1Q5OBS; AC1LG7OX; CBMicro_015073; n-(4-phenyl-1,3-thiazol-2-yl)isonicotinamide; Cambridge id 5245669; Oprea1_303023; Oprea1_553111; SCHEMBL17107144; CTK4J5937; DTXSID30355050; MolPort-001-992-732; ZINC290573; STK483947; BDBM50255300; AKOS000569765; MCULE-9247268363; BIM-0015234.P001; N-(4-Phenyl-thiazol-2-yl)-isonicotinamide; ST50017829; N~4~-(4-phenyl-1,3-thiazol-2-yl)isonicotinamide; Z27772062
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| MOA | Inhibitor | |||
| Activity | IC50 = 753 nM | |||
| External Link | ||||
| 5-Chloro-2-methyl-3H-quinazolin-4-one | Investigative | [76] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1200 nM | |||
| External Link | ||||
| BZ3 | Investigative | [77] | ||
| Synonyms |
5-METHOXYINDOLE; 1006-94-6; 5-Methoxy-1H-indole; 1H-Indole, 5-methoxy-; Femedol; 5-Methoxy indole; Indole, 5-methoxy-; Methoxy-5 indole; Indol-5-yl methyl ether; UNII-DQM3AS43PQ; Methoxy-5 indole [French]; 5-Methoxyindole, 99%; EINECS 213-745-3; DQM3AS43PQ; NSC 521752; CHEMBL280311; DWAQDRSOVMLGRQ-UHFFFAOYSA-N; MFCD00005674; 916979-77-6; 5Methoxyindole; 5-methoxyindol; 5-methoxy-indole; 3img; 3imc; PubChem7432; 1,3-dihydro-5-methyl-2H-Indol-2-one; ACMC-1BMAQ; 5-(methyloxy)-1H-indole; AC1Q4F1F; AC1L22NW; SCHEMBL74720; KSC177G3N; WLN: T
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-(3'-Methoxyphenyl) Benzimidazole-4-Carboxamide | Investigative | [72] | ||
| Synonyms |
2-(3-methoxyphenyl)-1H-benzimidazole-4-carboxamide; CHEMBL134022; BZC; 1efy; AC1L1BMO; SCHEMBL4321727; CTK7A9229; NVVWVYYHTKCIAE-UHFFFAOYSA-N; ZINC11565446; BDBM50093373; DB04010; 2-(3'-Methoxyphenyl)-1-H-benzimidazole-4-carboxamide; 2-(3-methoxyphenyl)-1H-1,3-benzodiazole-4-carboxamide; 2-(3''-METHOXYPHENYL) BENZIMIDAZOLE-4-CARBOXAMIDE; 2-(3-Methoxy-phenyl)-1H-benzoimidazole-4-carboxylic acid amide
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| MOA | Inhibitor | |||
| Activity | Ki = 6 nM | |||
| External Link | ||||
| CEP-6800 | Investigative | [78] | ||
| Synonyms |
UNII-0X7U7SRK9H; 0X7U7SRK9H; CHEMBL247374; 609848-02-4; SCHEMBL12256417; BDBM50197585; 1H-Cyclopenta(a)pyrrolo(3,4-C)carbazole-1,3(2H)-dione, 10-(aminomethyl)-4,5,6,7-tetrahydro-; 8-aminomethyl-1,2,3,11-tetrahydro-5,11-diaza-benzo[a]trindene-4,6-dione
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| MOA | Inhibitor | |||
| Activity | IC50 = 18 nM | |||
| External Link | ||||
| ANG-2864 | Investigative | [70] | ||
| Synonyms |
PARP inhibitor (ischemia/cancer), Angion Biomedica
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-Methoxybenzamide | Investigative | [79] | ||
| Synonyms |
5813-86-5; m-Methoxybenzamide; m-Anisamide; 3-Methoxy-benzamide; Benzamide, 3-methoxy-; UNII-M8502TLK98; EINECS 227-379-7; NSC 28589; NSC 209527; BRN 2206857; CHEMBL123978; VKPLPDIMEREJJF-UHFFFAOYSA-N; M8502TLK98; 3MB; 3pax; 5-methoxybenzamide; 3-methoxy-benzamid; ACMC-1ASRE; AC1Q5DMC; M-METHOXY BENZAMIDE; bmse000775; 3-Methoxybenzamide, 97%; Oprea1_695428; MLS001066418; 4-10-00-00326 (Beilstein Handbook Reference); cid_98487; SCHEMBL283787; AC1L407F; KS-00000VVU; CTK1H2082; VKPLPDIMEREJJF-UHFFFAOYSA-; DTXSID00206848
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| MOA | Inhibitor | |||
| Activity | IC50 = 17000 nM | |||
| External Link | ||||
| 2-Benzyl-2H-indazole-7-carboxamide | Investigative | [80] | ||
| Synonyms |
CHEMBL1094951; SCHEMBL2268172
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| MOA | Inhibitor | |||
| Activity | IC50 = 130 nM | |||
| External Link | ||||
| 5-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione | Investigative | [81] | ||
| Synonyms |
CHEMBL201723
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| MOA | Inhibitor | |||
| Activity | IC50 = 5000 nM | |||
| External Link | ||||
| 4-amino-1,8-naphthalimide | Investigative | [72] | ||
| Synonyms |
1742-95-6; 4-Aminonaphthalimide; 6-AMINO-BENZO[DE]ISOQUINOLINE-1,3-DIONE; 6-Amino-1H-benzo[de]isoquinoline-1,3(2H)-dione; 4-Aminonaphthalene-1,8-dicarboximide; Naphthalimide, 4-amino-; DFP 1; 1H-Benz[de]isoquinoline-1,3(2H)-dione, 6-amino-; EINECS 217-110-1; BRN 0177185; 6-aminobenzo[de]isoquinoline-1,3-dione; PARP Inhibitor V, 4-ANI; CHEMBL338790; CHEBI:40071; SSMIFVHARFVINF-UHFFFAOYSA-N; 6-Amino-1H-benz(de)isoquinoline-1,3(2H)-dione; 4-AMINO-1,8 NAPHTHALIMIDE
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| MOA | Inhibitor | |||
| Activity | IC50 = 26 nM | |||
| External Link | ||||
| Pyrrolo[3,4-e]indole-1,3(2H,6H)-dione | Investigative | [81] | ||
| Synonyms |
CHEMBL373066; pyrroloisoindoledione
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| MOA | Inhibitor | |||
| Activity | IC50 = 750 nM | |||
| External Link | ||||
| 8-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one | Investigative | [82] | ||
| Synonyms |
SCHEMBL4662780; CHEMBL363363; BDBM27514; LQEYAIKMIJUZNT-UHFFFAOYSA-N; indeno[1,2-c]isoquinolinone, 2a; ZINC13652898; 5,6-Dihydro-5-oxo-8-amino-indeno[1,2-c]isoquinoline
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| MOA | Inhibitor | |||
| Activity | IC50 = 300 nM | |||
| External Link | ||||
| EB-47 | Investigative | [64] | ||
| Synonyms |
EB 47; 366454-36-6; 5'-Deoxy-5'-[4-[2-[(2,3-dihydro-1-oxo-1H-isoindol-4-yl)amino]-2-oxoethyl]-1-piperazinyl]-5'-oxoadenosine Dihydrochloride; DTXSID40692822; ZINC98052573; NCGC00370771-01; KB-76747; FT-0667818; 4-[1-(6-Amino-9H-purin-9-yl)-1-deoxy-; A-D-ribofuranuronoyl]-N-(2,3-dihydro-1-oxo-1H-isoindol-4-yl)-1-piperazineacetamide Dihydrochloride; 2-{4-[(2R,3R,4S,5S)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxyoxolane-2-carbonyl]piperazin-1-yl}-N-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)acetamide (non-preferred name)
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| MOA | Inhibitor | |||
| External Link | ||||
| BZ6 | Investigative | [77] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 2-(4-methoxyphenyl)quinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL481591; 655222-47-2; CTK1J6622; DTXSID70649086; BDBM50255383; AKOS030560276; 8-Quinolinecarboxamide, 2-(4-methoxyphenyl)-
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| MOA | Inhibitor | |||
| Activity | IC50 = 1100 nM | |||
| External Link | ||||
| 9-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one | Investigative | [82] | ||
| Synonyms |
CHEMBL194155; SCHEMBL4078284; BDBM27515; BIBLEFNXUYTZIB-UHFFFAOYSA-N; indeno[1,2-c]isoquinolinone, 2b; ZINC13652899; 5,6-Dihydro-5-oxo-9-amino-indeno[1,2-c]isoquinoline
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| MOA | Inhibitor | |||
| Activity | EC50 = 95 nM | |||
| External Link | ||||
| (E)-N-(4-Phenylthiazol-2-yl) cinnamamide | Investigative | [75] | ||
| Synonyms |
CHEMBL452100; 2-Cinnamamido-4-phenylthiazole; (2E)-3-phenyl-N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide; 1107621-03-3; AC1LEPJR; ZINC60264; WOJRHCOBUKJCAJ-VAWYXSNFSA-N; MolPort-019-760-060; MolPort-001-931-977; HMS1397P15; STK173781; BDBM50255301; N-(4-phenylthiazol-2-yl)cinnamamide; AKOS000523355; MCULE-8934603681; BAS 00417267; ST4016450; 3-Phenyl-N-(4-phenyl-thiazol-2-yl)-acrylamide; AG-690/11629440; 3-phenyl-N-(4-phenyl-1,3-thiazol-2-yl)acrylamide; F0298-0058; A0793/0037152
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| MOA | Inhibitor | |||
| Activity | IC50 = 224 nM | |||
| External Link | ||||
| ANG-2684 | Investigative | [70] | ||
| Synonyms |
ANG-3038; PARP-1 inhibitors (acute pancreatitis/stroke); PARP-1 inhibitors (acute pancreatitis/stroke), Angion Biomedica
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione | Investigative | [81] | ||
| Synonyms |
CHEMBL380940; SCHEMBL5828673
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| MOA | Inhibitor | |||
| Activity | IC50 = 2000 nM | |||
| External Link | ||||
| 2,3-dihydro-1H-benzo[de]isoquinolin-1-one | Investigative | [83] | ||
| Synonyms |
CHEMBL594596; 2,3-dihydro-benzo[de]isoquinolin-1-one; SCHEMBL832168; ZINC24216; BDBM50306285; FCH1866210
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| MOA | Inhibitor | |||
| Activity | IC50 = 540 nM | |||
| External Link | ||||
| 5-amino-3,4-dihydroisoquinolin-1(2H)-one | Investigative | [83] | ||
| Synonyms |
129075-53-2; CHEMBL594759; SCHEMBL7581623; RTPKPVYTPRJRBY-UHFFFAOYSA-N; ZINC45353622; BDBM50306284; AKOS023598631; AB53700; FCH1123505; KS-9128; CM10348; AJ-110485; 5-amino-3,4-dihydro-1(2H)-isoquinolinone; EN300-254419
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| MOA | Inhibitor | |||
| Activity | IC50 = 410 nM | |||
| External Link | ||||
| KR-33889 | Investigative | [70] | ||
| Synonyms |
KR-34285; PARP-1 inhibitors (myocardial infarction), KRICT
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-(5-Morpholin-4-yl-pentyl)-2H-phthalazin-1-one | Investigative | [84] | ||
| Synonyms |
CHEMBL194684
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| MOA | Inhibitor | |||
| Activity | IC50 = 119 nM | |||
| External Link | ||||
| AG-014376 | Investigative | [85] | ||
| Synonyms |
CHEMBL361489; SCHEMBL7159231; BDBM50154730; 6-(4-Dimethylaminomethyl-phenyl)-3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-one
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| MOA | Inhibitor | |||
| Activity | Ki = 6.4 nM | |||
| External Link | ||||
| 3-Hydroxy-benzamide | Investigative | [74] | ||
| Synonyms |
3-hydroxybenzamide; 618-49-5; benzamide, 3-hydroxy-; CHEMBL419424; 3-Hydroxy benzamide; NSC379289; 3-hydroxybenzenecarboxamide; AC1Q4ZB3; AC1L7W2U; ACMC-1B71B; Oprea1_435073; SCHEMBL161861; 3-Hydroxybenzamide, AldrichCPR; CTK2F7291; DTXSID90321635; NGMMGKYJUWYIIG-UHFFFAOYSA-N; MolPort-001-791-593; ZINC1590754; KM0548; BDBM50068769; 9282AB; ANW-33964; 3-HYDROXY-BENZOIC ACID,AMIDE; SBB079277; AKOS000207073; VZ26952; NSC-379289; MB00281; MCULE-9599926365; NCGC00323509-01; KB-32185; CJ-25437; AJ-27681; CJ-05592; SC-47787
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| MOA | Inhibitor | |||
| Activity | IC50 = 9100 nM | |||
| External Link | ||||
| 8-Methoxy-2-phenyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 10000 nM | |||
| External Link | ||||
| Quinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
8-Quinolinecarboxamide; 55706-61-1; CCRIS 6967; CHEMBL502330; HPQRQAOVNXWEEQ-UHFFFAOYSA-N; 8-Carbamoylquinoline; 8-Quinolinecarboxamide #; AC1L44SC; SCHEMBL460456; CTK5A4047; quinoline-8-carboxylic acid amide; DTXSID00204243; MolPort-005-722-305; ZINC6095019; BDBM50255266; AKOS008969900; NE38855; MCULE-7978956907; LS-188644; KB-259682
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| MOA | Inhibitor | |||
| Activity | IC50 = 1900 nM | |||
| External Link | ||||
| 9-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one | Investigative | [82] | ||
| Synonyms |
CHEMBL190895; BDBM27513; indeno[1,2-c]isoquinolinone, 1e; 9-Fluoro-5,6-dihydro-11H-indeno[1,2-c]isoquinoline-5-one
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| MOA | Inhibitor | |||
| Activity | EC50 = 180 nM | |||
| External Link | ||||
| 8-Methyl-2-(4-nitro-phenyl)-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 104 nM | |||
| External Link | ||||
| 2H-Isoquinolin-1-one | Investigative | [74] | ||
| Synonyms |
1-Hydroxyisoquinoline; 491-30-5; Isoquinolin-1(2H)-one; isoquinolin-1-ol; 1-Isoquinolinol; Isocarbostyril; 1(2H)-ISOQUINOLINONE; Isoquinolin-1-one; 489453-23-8; 1(2H)-Isoquinolone; 1,2-dihydroisoquinolin-1-one; 1-hydroxyisoquinolin; isoquinolinol; 87602-67-3; 1(2H)-ISOQUINILONE; Isocarbostyril, 98%; UNII-95EG3HGG1P; 95EG3HGG1P; Isoquinolinone; CHEMBL339695; CHEBI:18350; VDBNYAPERZTOOF-UHFFFAOYSA-N; 1-isoquinolone; oxidoisoquinolinium; EINECS 207-732-1; Isocarbostyril(1-hydroxyisoquinoline); NSC 27273
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| MOA | Inhibitor | |||
| Activity | IC50 = 9 nM | |||
| External Link | ||||
| KU-58684 | Investigative | [75] | ||
| Synonyms |
SCHEMBL863338; 623578-11-0
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| MOA | Inhibitor | |||
| External Link | ||||
| 2,8-Dimethyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 490 nM | |||
| External Link | ||||
| 5-aminoisoquinolin-1(2H)-one | Investigative | [73] | ||
| Synonyms |
93117-08-9; 5-amino-2H-isoquinolin-1-one; 5-AMINOISOQUINOLIN-1-OL; 5-amino-1,2-dihydroisoquinolin-1-one; 5-AIQ; CHEMBL446240; 5-Amino-2H-isoquinoin-1-one; 5-AMINO-1(2H)-ISOQUINOLINONE; 5-aminoisoquinolinone; 4pnq; 32X; AC1Q6DVG; AC1L1CUR; 5-Amino-1-isoquinolinol; SCHEMBL215327; 5-Amino-1-hydroxyisoquinoline; BDBM27503; 5-amino-isoquinolin-1(2h)-one; 5-amino isoquinolin-1(2h)-one; CTK5H2122; DTXSID90274354; 1(2H)-Isoquinolinone,5-amino-; MolPort-008-423-043; MolPort-004-803-197
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| MOA | Inhibitor | |||
| Activity | IC50 = 940 nM | |||
| External Link | ||||
| INO-1002 | Investigative | [70] | ||
| Synonyms |
PARP inhibitors, Inotek; PARP inhibitor (erectile dysfunction), Inotek; PARP inhibitor (prostate nerve damage), Inotek; Poly (ADP ribose) polymerase inhibitor (erectile dysfunction), Inotek; Poly (ADP ribose) polymerase inhibitor (prostate nerve damage), Inotek
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-(4-aminophenyl)quinoxaline-5-carboxamide | Investigative | [75] | ||
| Synonyms |
CHEMBL443077; quinoxaline analogue, 3f; SCHEMBL7112515
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| MOA | Inhibitor | |||
| Activity | IC50 = 87 nM | |||
| External Link | ||||
| 2-phenylpyrazolo-[1,5-a]pyridine-7-carboxamide | Investigative | [80] | ||
| Synonyms |
2-phenylpyrazolo[1,5-a]pyridine-7-carboxamide; 1196713-16-2; ZINC64337832; DA-47424
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-benzylphthalazin-1(2H)-one | Investigative | [75] | ||
| Synonyms |
4-Benzyl-1(2H)-phthalazinone; 32003-14-8; 4-Benzyl-2H-phthalazin-1-one; 4-benzyl-1,2-dihydrophthalazin-1-one; CHEMBL66761; JUCCMEHWBGPJKS-UHFFFAOYSA-N; benzylphthalazinone; phthalazinone, 1; 4-benzyl-phthalazone; AC1LDDNC; SMR000135223; AC1Q6GZZ; ChemDiv2_000142; Cambridge id 5241846; Oprea1_151142; Oprea1_623913; CBDivE_015258; MLS000530246; SCHEMBL863462; CTK4G8063; BDBM27660; DTXSID30346948; MolPort-001-796-654; HMS2379K10; HMS1369G10; 4-benzyl-2-hydrophthalazin-1-one; 4-Benzyl-1(2H)-phthalazinone #
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| MOA | Inhibitor | |||
| Activity | IC50 = 770 nM | |||
| External Link | ||||
| 3-Methylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL504998; 8-Quinolinecarboxamide, 3-methyl-; BDBM50255267
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| MOA | Inhibitor | |||
| Activity | IC50 = 3400 nM | |||
| External Link | ||||
| 2-(4-Chlorophenyl)-5-Quinoxalinecarboxamide | Investigative | [79] | ||
| Synonyms |
3-(4-CHLOROPHENYL)QUINOXALINE-5-CARBOXAMIDE; 4tju; 1wok; AC1LCVX7; quinoxaline analogue, 3b; SCHEMBL424209; 3-(4-chloro-phenyl)-quinoxaline-5-carboxylic acid amide; CTK8F4675; BDBM27720; ZINC1489510; DB03509; 489457-67-2
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-(4-Methoxy-phenyl)-8-methyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 891 nM | |||
| External Link | ||||
| HYDAMTIQ | Investigative | [70] | ||
| Synonyms |
PARP-1 inhibitor (brain ischemia), University of Perugia
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| MOA | Inhibitor | |||
| External Link | ||||
| 8-Nitro-6H,11H-indeno[1,2-c]isoquinolin-5-one | Investigative | [82] | ||
| Synonyms |
SCHEMBL4661629; CHEMBL370673; BDBM27510; SWBDUXDIPMGDNO-UHFFFAOYSA-N; indeno[1,2-c]isoquinolinone, 1b; ZINC13652894; 5,6-dihydro-5-oxo-8-nitro-indeno[1,2-c]isoquinoline; 8-Nitro-5,6-dihydro-11H-indeno[1,2-c]isoquinoline-5-one
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| MOA | Inhibitor | |||
| Activity | IC50 = 500 nM | |||
| External Link | ||||
| PD-128763 | Investigative | [79] | ||
| Synonyms |
5-Methyl-3,4-dihydroisoquinolin-1(2H)-one; 129075-56-5; 3,4-Dihydro-5-methyl-1(2H)-isoquinolinone; 3,4-DIHYDRO-5-METHYL-ISOQUINOLINONE; 1(2H)-Isoquinolinone, 3,4-dihydro-5-methyl-; CHEBI:41928; PD128763; CHEMBL125200; 5-methyl-3,4-dihydro-2H-isoquinolin-1-one; 3,4-dihydro-5-methylisoquinolinone; 1(2H)-Isoquinolinone,3,4-dihydro-5-methyl-; 5-methyl-1,2,3,4-tetrahydroisoquinolin-1-one; DHQ; PD 128763; dihydroisoquinolinone, 1; AC1L3WIO; ACMC-1C7L4; SCHEMBL831538; AMBZ0075; KS-00000QFP; CTK4B6146; BDBM27682
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| MOA | Inhibitor | |||
| Activity | Ki = 70 nM | |||
| External Link | ||||
| 8-Methyl-2-phenyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 795 nM | |||
| External Link | ||||
| TI3 | Investigative | [77] | ||
| Synonyms |
RB106; CHEMBL419499; [(2S)-2-SULFANYL-3-PHENYLPROPANOYL]-GLY-(5-PHENYLPROLINE); 1qf2; AC1L9LL2; BDBM50051785; DB02669; N-[(S)-2-Mercapto-3-phenylpropionyl]-Gly-[(5R)-5-phenyl-L-Pro-]-OH; N-[(2S)-3-phenyl-2-sulfanylpropanoyl]glycyl-(5R)-5-phenyl-L-proline; (2S,5R)-5-phenyl-1-[2-[[(2S)-3-phenyl-2-sulfanylpropanoyl]amino]acetyl]pyrrolidine-2-carboxylic acid; (2S,5R)-1-[2-((S)-2-Mercapto-3-phenyl-propionylamino)-acetyl]-5-phenyl-pyrrolidine-2-carboxylic acid
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-aminobenzo[c][1,5]naphthyridin-6(5H)-one | Investigative | [75] | ||
| Synonyms |
CHEMBL106154; Benzo[c]-1,5-naphthyridin-6(5H)-one, 3-amino-; SCHEMBL12750402; BDBM50130580; 433726-73-9
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| MOA | Inhibitor | |||
| Activity | IC50 = 180 nM | |||
| External Link | ||||
| S-111 | Investigative | [70] | ||
| Synonyms |
PARP1 inhibitor (cancer), Sentinel Oncology
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| MOA | Inhibitor | |||
| External Link | ||||
| Thieno-phenanthridin-6-one | Investigative | [64] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 3-Morpholin-4-ylmethyl-5H-phenanthridin-6-one | Investigative | [84] | ||
| Synonyms |
CHEMBL194535
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| MOA | Inhibitor | |||
| Activity | IC50 = 23 nM | |||
| External Link | ||||
| 1,2,3,4,4a,5-hexahydrophenanthridin-6(10bH)-one | Investigative | [75] | ||
| Synonyms |
CHEMBL84044; 7403-93-2; NSC403412; AC1L83AN; SCHEMBL6645911; DTXSID70323238; BDBM50131013; NSC-403412; 2,3,4,4a,5,10b-hexahydro-1H-phenanthridin-6-one; 1,3,4,4a,5,10b-Hexahydro-2H-phenanthridin-6-one
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| MOA | Inhibitor | |||
| Activity | IC50 = 7500 nM | |||
| External Link | ||||
| 8-Hydroxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 105 nM | |||
| External Link | ||||
| 2-(4-Amino-phenyl)-8-methyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 504 nM | |||
| External Link | ||||
| 4-(4-Morpholin-4-yl-butyl)-2H-phthalazin-1-one | Investigative | [84] | ||
| Synonyms |
CHEMBL373210
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| MOA | Inhibitor | |||
| Activity | IC50 = 950 nM | |||
| External Link | ||||
| 2-phenyl-2H-benzo[d][1,2,3]triazole-4-carboxamide | Investigative | [80] | ||
| Synonyms |
CHEMBL1096560; SCHEMBL2265205
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| MOA | Inhibitor | |||
| Activity | IC50 = 71 nM | |||
| External Link | ||||
| 2-phenyl-2H-indazole-7-carboxamide | Investigative | [80] | ||
| Synonyms |
CHEMBL594298; SCHEMBL1422404; BDBM50306166
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| MOA | Inhibitor | |||
| Activity | IC50 = 24 nM | |||
| External Link | ||||
| Carba-Nicotinamide-Adenine-Dinucleotide | Investigative | [79] | ||
| Synonyms |
Carba-NAD; Carbanicotinamide adenine dinucleotide; 112345-60-5; AC1L4TS7; AC1Q5J0L; SCHEMBL16445201; 5'-o-{[({[(1r,2r,3s,4r)-4-(3-carbamoylpyridinium-1-yl)-2,3-dihydroxycyclopentyl]methoxy}phosphinato)oxy](hydroxy)phosphoryl}adenosine; [[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(1R,2R,3S,4R)-4-(3-carbamoylpyridin-1-ium-1-yl)-2,3-dihydroxycyclopentyl]methyl phosphate; Adenosine 5'-(trihydrogen diphosphate), 5'-((4-(3-(aminocarbonyl)pyridinio)-2,3-dihydroxycyclopentyl)m
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-aminobenzamide | Investigative | [71] | ||
| Synonyms |
3544-24-9; m-Aminobenzamide; Benzamide, 3-amino-; 3-Amino-benzamide; Benzamide, m-amino-; meta-aminobenzamide; 3-ABA; 3-Aminobenzimide; 3-amino benzamide; aniline-3-carboxamide; 3-aminobenzoic acid amide; UNII-8J365YF1YH; CCRIS 3925; EINECS 222-586-9; NSC 36962; BRN 2802373; PARP Inhibitor I, 3-ABA; 3-H2NC6H4CONH2; CHEMBL81977; 3-AB; 8J365YF1YH; CHEBI:64042; GSCPDZHWVNUUFI-UHFFFAOYSA-N; MFCD00007989; 3-Aminobenzamide, 98%; SR-01000075657; HSDB 7581; 3-azanylbenzamide; m-amino benzamide; 4pml; 3-Aminobenzaminde
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| MOA | Inhibitor | |||
| Activity | Ki = 3100 nM | |||
| External Link | ||||
| 3-Ethenylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL481793; 8-Quinolinecarboxamide, 3-ethenyl-; BDBM50255270
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| MOA | Inhibitor | |||
| Activity | IC50 = 5800 nM | |||
| External Link | ||||
| 3-Phenylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL450259; BDBM50255264
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| MOA | Inhibitor | |||
| Activity | IC50 = 15000 nM | |||
| External Link | ||||
| 3-(4-methoxyphenyl)quinoxaline-5-carboxamide | Investigative | [75] | ||
| Synonyms |
CHEMBL519443; quinoxaline analogue, 3e; SCHEMBL7045177
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| MOA | Inhibitor | |||
| Activity | IC50 = 71 nM | |||
| External Link | ||||
| TI4 | Investigative | [77] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Benzo[c][1,5]naphthyridin-6(5H)-one | Investigative | [75] | ||
| Synonyms |
CHEMBL320031; Benzo[c]-1,5-naphthyridin-6(5H)-one; SCHEMBL12750384; BDBM50130585; 5H-Benzo[c][1,5]naphthyridin-6-one; Benzo[c][1,5]naphthyridine-6(5H)-one
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| MOA | Inhibitor | |||
| Activity | IC50 = 116 nM | |||
| External Link | ||||
| 3-(4-cyanophenyl)quinoxaline-5-carboxamide | Investigative | [75] | ||
| Synonyms |
CHEMBL481603; quinoxaline analogue, 3c; SCHEMBL7108289
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| MOA | Inhibitor | |||
| Activity | IC50 = 101 nM | |||
| External Link | ||||
| 1,7,8,9-tetrahydro-1,5-diaza-trindene-4,6-dione | Investigative | [81] | ||
| Synonyms |
CHEMBL201907; SCHEMBL2086780; ZINC28569089
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| MOA | Inhibitor | |||
| Activity | IC50 = 40 nM | |||
| External Link | ||||
| 8-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one | Investigative | [82] | ||
| Synonyms |
CHEMBL370045; BDBM27512; indeno[1,2-c]isoquinolinone, 1d; ZINC13652896; 8-Fluoro-5,6-dihydro-11H-indeno[1,2-c]isoquinoline-5-one
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| MOA | Inhibitor | |||
| Activity | EC50 = 225 nM | |||
| External Link | ||||
| 8-Hydroxy-2-phenyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1034 nM | |||
| External Link | ||||
| 8-Methoxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 10000 nM | |||
| External Link | ||||
| 2-(4-Chlorophenyl)-2H-indazole-7-carboxamide | Investigative | [80] | ||
| Synonyms |
CHEMBL1099295; SCHEMBL2264064
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| MOA | Inhibitor | |||
| Activity | IC50 = 24 nM | |||
| External Link | ||||
| BPI-704001 | Investigative | [70] | ||
| Synonyms |
BPI-705001; BPI-715001; PARP-1 inhibitors (cancer); PARP-1 inhibitors (cancer), Beta Pharma
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| MOA | Inhibitor | |||
| External Link | ||||
| Pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione | Investigative | [81] | ||
| Synonyms |
CHEMBL370869; SCHEMBL5381581
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| MOA | Inhibitor | |||
| Activity | IC50 = 10000 nM | |||
| External Link | ||||
| 2-Methylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL471966; 8-Quinolinecarboxamide, 2-methyl-; SCHEMBL422282; BDBM50255329; AKOS022882220
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| MOA | Inhibitor | |||
| Activity | IC50 = 500 nM | |||
| External Link | ||||
| 8-Methoxy-2-methyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 3-Prop-1-ynylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL504903; ZINC40829471
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| MOA | Inhibitor | |||
| Activity | IC50 = 2200 nM | |||
| External Link | ||||
| 2-(2-Chlorophenyl)-2H-indazole-7-carboxamide | Investigative | [80] | ||
| Synonyms |
CHEMBL1094952; SCHEMBL2265265
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| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| 2-(3-Piperidin-1-yl-propyl)-3H-quinazolin-4-one | Investigative | [76] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1100 nM | |||
| External Link | ||||
| 3-Ethylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL453989; 8-Quinolinecarboxamide, 3-ethyl-; BDBM50255269
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| MOA | Inhibitor | |||
| Activity | IC50 = 3700 nM | |||
| External Link | ||||
| A-620223 | Investigative | [70] | ||
| Synonyms |
A-866111; A-966492; ABT-472; ABT-999; PARP inhibitor, Abbott; PARP inhibitors, Abbott; Poly (ADP)ribose polymer inhibitor, Abbott; Poly (ADP)ribose inhibitors (cancer), Abbott
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| MOA | Inhibitor | |||
| Activity | EC50 = 3 nM | |||
| External Link | ||||
| DR2313 | Investigative | [64] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 2-(4-Azido-phenyl)-8-methoxy-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| 2-(3-Chlorophenyl)-2H-indazole-7-carboxamide | Investigative | [80] | ||
| Synonyms |
CHEMBL1094953; SCHEMBL2265628
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| MOA | Inhibitor | |||
| Activity | IC50 = 14 nM | |||
| External Link | ||||
| 2-(4-Hydroxy-phenyl)-8-methyl-3H-quinazolin-4-one | Investigative | [74] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1200 nM | |||
| External Link | ||||
| 2-ethylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL526128; 8-Quinolinecarboxamide, 2-ethyl-; BDBM50255330
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| MOA | Inhibitor | |||
| Activity | IC50 = 800 nM | |||
| External Link | ||||
| 2-phenylquinoline-8-carboxamide | Investigative | [73] | ||
| Synonyms |
CHEMBL480429; SCHEMBL6442515; ZINC3939668
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| MOA | Inhibitor | |||
| Activity | IC50 = 900 nM | |||
| External Link | ||||
| BZ5 | Investigative | [77] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| ME0328 | Investigative | [86] | ||
| Synonyms |
ME-0328; compound 5b [PMID 24188023]
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| MOA | Inhibitor | |||
| Activity | IC50 = 6300 nM | |||
| External Link | ||||
| [2(R,S)-2-Sulfanylheptanoyl]-Phe-Ala | Investigative | [77] | ||
| Synonyms |
TI1; AC1NRDCJ; 1qf1; DB02597; N-[(2S)-2-sulfanylheptanoyl]-L-phenylalanyl-L-alanine; N-[N-[(S)-2-Mercaptoheptanoyl]-L-phenylalanyl]-L-alanine; (2S)-2-[[(2S)-3-phenyl-2-[[(2S)-2-sulfanylheptanoyl]amino]propanoyl]amino]propanoic acid; (2S)-2-[(2S)-3-phenyl-2-[(2S)-2-sulfanylheptanamido]propanamido]propanoic
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| MOA | Inhibitor | |||
| External Link | ||||
| S-070 | Investigative | [70] | ||
| Synonyms |
S-158; Targeted synergy program (solid tumor), Sentinel Oncology; Chk1/PARP-1 inhibitors (cancer); Chk1/PARP-1 inhibitors (cancer), Sentinel Oncology
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| MOA | Inhibitor | |||
| External Link | ||||
| 2B91: Colorectal cancer | 25 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Retifanlimab | Approved | [87] | ||
| Synonyms |
INCMGA0012; Retifanlimab
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| External Link | ||||
| Aflibercept | Approved | [88] | ||
| Synonyms |
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
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| External Link | ||||
| Regorafenib | Approved | [89] | ||
| Synonyms |
755037-03-7; BAY 73-4506; Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY73-4506; Regorafenib (BAY 73-4506); UNII-24T2A1DOYB; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY-73-4506; 24T2A1DOYB; CHEMBL1946170; CHEBI:68647; Stivarga (TN); BAY73-4506 hydrochloride; Regorafenib [USAN:INN]
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| External Link | ||||
| Bevacizumab | Approved | [90] | ||
| Synonyms |
Bevacizumab (ophthalmic slow-release tissue tablet)
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| External Link | ||||
| SYM-004 | Phase 3 | [90] | ||
| Synonyms |
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
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| External Link | ||||
| Bevacizumab + Erlotinib | Phase 3 | [91] | ||
| External Link | ||||
| CPI-613 | Phase 3 | [90] | ||
| Synonyms |
95809-78-2; 6,8-bis(benzylthio)octanoic acid; CPI 613; MLS006010202; SCHEMBL1062218; 6,8-Bis(benzylsulfanyl)octanoic acid; Octanoic acid, 6,8-bis((phenylmethyl)thio)-; Octanoic acid, 6,8-bis[(phenylMethyl)thio]-; 6,8-Bis[(phenylmethyl)thio]octanoic acid; CPI613; CHEMBL3186849; QCR-193; AOB1058; MolPort-023-219-128; HMS3656L06; C22H28O2S2; BCP04663; EX-A2043; s2776; AKOS025142095; BCP9000552; DB12109; RL06062; CS-0961; NCGC00344764-01; SMR004701300; AS-16613; BC261916; AK174899; HY-15453; BCP0726000030; KB-293127; AB0035874
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| External Link | ||||
| Bevacizumab | Approved | [88] | ||
| External Link | ||||
| AlloStim | Phase 2/3 | [92] | ||
| Synonyms |
AlloStim (TN)
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| External Link | ||||
| Sibrotuzumab | Phase 2 | [93] | ||
| External Link | ||||
| CV301 | Phase 2 | [94] | ||
| External Link | ||||
| Efatutazone | Phase 2 | [95] | ||
| Synonyms |
Inolitazone; 223132-37-4; 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-Thiazolidinedione; Efatutazone [INN]; RS5444; CS-7017; SCHEMBL3246054; CHEMBL3545280; JCYNMRJCUYVDBC-UHFFFAOYSA-N; Efatutazone;CS-7017;RS5444; BCP07478; AKOS030526729; DB11894; CS-0778; KB-77905; DA-07988; HY-14792; QC-10456; 4CA-1384; FT-0737589; 5-[4-[6-(4-amino-3 ,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]benzyl]thiazolidine-2,4-dione
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| External Link | ||||
| LOR-2040 | Phase 2 | [96] | ||
| External Link | ||||
| RG7221 | Phase 2 | [97] | ||
| External Link | ||||
| PEG-SN38 | Phase 2 | [98] | ||
| Synonyms |
EZN-2208
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| External Link | ||||
| MEGF0444A | Phase 2 | [99] | ||
| External Link | ||||
| Encapsulated cell therapy | Phase 1/2 | [100] | ||
| External Link | ||||
| AB928 | Phase 1/2 | [101] | ||
| External Link | ||||
| MGD007 | Phase 1 | [97] | ||
| External Link | ||||
| BNC-101 | Phase 1 | [102] | ||
| External Link | ||||
| Navicixizumab | Phase 1 | [90] | ||
| External Link | ||||
| RG7160 | Discontinued in Phase 2 | [103] | ||
| External Link | ||||
| Nimesulide | Terminated | [104] | ||
| Synonyms |
51803-78-2; N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide; Mesulid; Flogovital; Sulidene; Nimed; R-805; 4-NITRO-2-PHENOXYMETHANESULFONANILIDE; Nisulid; Nimesulidum [INN-Latin]; Nimesulida [INN-Spanish]; R 805; UNII-V4TKW1454M; 4-Nitro-2-phenoxy-methanesulfonanilide; 4'-Nitro-2'-phenoxymethanesulfonanilide; Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)-; EINECS 257-431-4; 4'-Nitro-2'-phenoxymethansulfonanilid; BRN 2421175; CHEMBL56367; MLS000069680; V4TKW1454M; Methanesulfonanilide, 4'-nitro-2'-phenoxy-; CHEBI:44445; Dulanermin
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| External Link | ||||
| Saracatinib | Phase 2 | [105] | ||
| External Link | ||||
| G3139 + Irinotecan | Investigative | [106] | ||
| External Link | ||||
References
: m6A sites