| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T10052 | ||||
| Target Name | G1/S-specific cyclin E1 | ||||
| Target Type | Discontinued |
||||
| Drug Potency against Target | (2'Z,3'E)-5-Nitro-5'-methoxy-indirubin-3'-oxime | Drug Info | IC50 = 2950 nM | [530823] | |
| (2'Z,3'E)-5-Fluoro-5'-methoxy-indirubin-3'-oxime | Drug Info | IC50 = 4120 nM | [530823] | ||
| PD-0183812 | Drug Info | IC50 = 165 nM | [525924] | ||
| 5-nitroindirubin-3'-oxime | Drug Info | IC50 = 7.35 nM | [530823] | ||
| 3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol | Drug Info | IC50 = 6000 nM | [528490] | ||
| 4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol | Drug Info | IC50 = 400 nM | [526504] | ||
| 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | Drug Info | IC50 = 3500 nM | [528490] | ||
| 2-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol | Drug Info | IC50 = 2500 nM | [528490] | ||
| References | |||||
| Ref 530823 | J Med Chem. 2010 May 13;53(9):3696-706.5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. | ||||
| Ref 530823 | J Med Chem. 2010 May 13;53(9):3696-706.5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. | ||||
| Ref 525924 | J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. | ||||
| Ref 530823 | J Med Chem. 2010 May 13;53(9):3696-706.5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. | ||||
| Ref 528490 | J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. | ||||
| Ref 526504 | J Med Chem. 2003 Jan 16;46(2):222-36.Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. | ||||
| Ref 528490 | J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. | ||||
| Ref 528490 | J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. | ||||
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