Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T44458 | ||||
Target Name | Cell division protein kinase 9 | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | AT7519 | Drug Info | IC50 < 10 nM | [537564] | |
3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol | Drug Info | IC50 = 1500 nM | [528490] | ||
P276-00 | Drug Info | IC50 = 20 nM | [537564] | ||
MERIOLIN 7 | Drug Info | IC50 = 5300 nM | [529275] | ||
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | Drug Info | IC50 = 350 nM | [528490] | ||
SCH 727965 | Drug Info | Ki = 4 nM | [553063] | ||
R-roscovitine | Drug Info | IC50 = 230 nM | [537564] | ||
SNS-032 | Drug Info | IC50 = 1 nM | [552961] | ||
MERIOLIN 2 | Drug Info | IC50 = 18 nM | [529275] | ||
MERIOLIN 6 | Drug Info | IC50 = 5.6 nM | [529275] | ||
MERIOLIN 4 | Drug Info | IC50 = 7 nM | [529275] | ||
MERIOLIN 1 | Drug Info | IC50 = 26 nM | [529275] | ||
MERIOLIN 8 | Drug Info | IC50 = 1200 nM | [529275] | ||
Flavopiridol | Drug Info | IC50 = 3 nM | [537564] | ||
4-(phenyldiazenyl)-1H-pyrazole-3,5-diamine | Drug Info | IC50 = 15000 nM | [528490] | ||
ZK 304709 | Drug Info | IC50 = 4 nM | [552961] | ||
MERIOLIN 3 | Drug Info | IC50 = 6 nM | [529275] | ||
MERIOLIN 5 | Drug Info | IC50 = 5.6 nM | [529275] | ||
Action against Disease Model | SCH 727965 | Induced apoptosis in t uMour cell lines and growth inhibition or regression in xenograft models. | [537564] | Drug Info | |
The Effect of Target Knockout, Knockdown or Genetic Variations | (A) TBP is specifically enriched at the TSS and is not affected by CDK9 knockdown, whereas CDK9 is significantly enriched both at the TSS and at 0.5 kb and these levels decreaseon knockdown. (B) CDK9 knockdown similarly decreases RNAPII and P-Ser 5-RNAPII levels at the TSS without affecting elongation to the 3'-end cleavage site. By contrast, P-Ser 2 is markedly decreased to near-background levels both at the TSS and at 0.5 kb. (C) The H2B-ubiquitinating complex (PAF1, RNF20 and RNF40) is enriched at 0.5 kb of the HIST1H2BD gene together with H2Bub1, and their levels decrease following CDK9 knockdown. (D) ChIP analysis of SLBP and the U7 snRNP component LSM11 shows decreased recruitment to the 3'-cleavage site. (E) CDK9 knockdown increases RNAPII read-through past the normal 3'-end cleavage site of the HIST1H2BD and HIST1H2AC genes. | [537564] | |||
References | |||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
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 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. | ||||
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 553063 | Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53. doi: 10.1158/1535-7163.MCT-10-0324. Epub 2010 Jul 27. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
Ref 552961 | End of the line for cannabinoid receptor 1 as an anti-obesity target? An opinion. Nat Rev Drug Discov. 2009 Jul;8(7):594. doi: 10.1038/nrd2775-c1. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
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 552961 | End of the line for cannabinoid receptor 1 as an anti-obesity target? An opinion. Nat Rev Drug Discov. 2009 Jul;8(7):594. doi: 10.1038/nrd2775-c1. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. | ||||
Ref 529275 | J Med Chem. 2008 Feb 28;51(4):737-51. Epub 2008 Jan 31.Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolincomplex. |
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