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 530823J 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 530823J 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 525924J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
Ref 530823J 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 528490J 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 526504J 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 528490J 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 528490J 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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