Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T81386 | Target Info | |||
| Target Name | Positive transcription elongation factor b (P-TEFb) | ||||
| Synonyms |
P-TEFb
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| Target Type | Clinical trial Target | ||||
| Gene Name | CDK9-CCNT1 | ||||
| Biochemical Class | S-phase kinase-associated protein | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 4 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Cyclapolin 9
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Investigative | Compound Info | ||
| Synonyms |
Cyclapolin-9; CHEMBL476124; 7-Nitro-5-(trifluoromethyl)-2-benzothiazolecarboxamide-3-oxide; 7-Nitro-3-oxy-5-trifluoromethyl-benzothiazole-2-carboxylic acid amide; SCHEMBL5055142; CTK8I6133; AOB5979; ZINC2577648; BDBM50263697; AKOS024457436; HY-15159; CS-0003792; 7-Nitro-5-(trifluoromethyl)-2-Benzothiazolecarboxamide 3-oxide; 2-(aminocarbonyl)-7-nitro-5-(trifluoromethyl)-1,3-benzothiazol-3-ium-3-olate
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2R)-2-[[4-[(4-Chlorophenyl)methylamino]-8-propan-2-ylpyrazolo[1,5-a][1,3,5]triazin-2-yl]amino]-3-methylbutan-1-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL480442
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
3-(6-Chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(7-methoxybenzofuran-3-yl)pyrrole-2,5-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL522760; SCHEMBL3133068; BDBM50267565; 3-(6-chloro-5-fluoro-1-methylindol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)pyrrole-2,5-dione
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
2-Benzothiazolecarboxamide, 7-nitro-5-[(trifluoromethyl)thio]-, 3-oxide
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Investigative | Compound Info | ||
| Synonyms |
Cyclapolin 1; 2-Benzothiazolecarboxamide, 7-nitro-5-[(trifluoromethyl)thio]-3-oxide; SCHEMBL5062617; CHEMBL1222044; CTK2H1083; DTXSID10429521; 7-nitro-3-oxido-5-(trifluoromethylsulfanyl)-1,3-benzothiazol-3-ium-2-carboxamide
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Non Binders of This Target (in total, 5 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Fascaplysine
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Investigative | Compound Info | ||
| Synonyms |
Fascaplysin; Fascaplysin chloride; CHEMBL258765; Fascaplisine; NSC622398; NSC-622398; 12,13-dihydro-13-oxo-pyrido[1,2-a:3,4-b']diindol-5-ium, monochloride; GNF-PF-1458; Fascaplysin, Synthetic; SCHEMBL15531753; HMS3229G10; Pyrido(1,2a:3,4-b')diindol-5-ium, 12,13-dihydro-13-oxo-, chloride; CCG-206840; Fascaplysin, Synthetic - CAS 114719-57-2; J-003125; Pyrido[1,4-b']diindol-5-ium, 12,13-dihydro-13-oxo-,chloride; Pyrido[1,2-a:3,4-b']diindol-5-ium, 12,13-dihydro-13-oxo-, chloride
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| Activity |
IC50 > 250000 nM
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[4] | |||
| Compound Name |
Chembl4216945
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455464
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| Activity |
IC50 = 529300 nM
|
[5] | |||
| Compound Name |
N-(2-(1H-Indol-3-yl)ethyl)-4-chloro-N-methylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL213302; BDBM50188066
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| Activity |
IC50 > 1000000 nM
|
[4] | |||
| Compound Name |
N-(2-(1H-Indol-3-yl)ethyl)-N-methyl-[1,1'-biphenyl]-4-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CA-224; CHEMBL213805; SCHEMBL13941762; CA224; BDBM50188071; A14414; N-[2-(1H-Indol-3-yl)ethyl]-N-methyl-4-phenylbenzamide; N-Methyl-N-[2-(1H-indole-3-yl)ethyl]-4-phenylbenzamide; biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methyl-amide
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| Activity |
IC50 > 1000000 nM
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[4] | |||
| Compound Name |
N-(2-(1H-Indol-3-yl)ethyl)-4-tert-butyl-N-methylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL209467; BDBM50188064; N-Methyl-N-[2-(1H-indole-3-yl)ethyl]-4-tert-butylbenzamide
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| Activity |
IC50 > 1000000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance. Nat Chem Biol. 2006 Nov;2(11):608-17. | ||||
| REF 2 | Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue. J Med Chem. 2009 Feb 12;52(3):655-63. | ||||
| REF 3 | From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. J Med Chem. 2009 Apr 9;52(7):1853-63. | ||||
| REF 4 | Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity. J Med Chem. 2014 Nov 26;57(22):9658-72. | ||||
| REF 5 | Discovery of novel CDK inhibitors via scaffold hopping from CAN508. Bioorg Med Chem Lett. 2018 May 1;28(8):1386-1391. | ||||
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