Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T58449 | ||||
Target Name | Cyclin-dependent kinase 7 (CDK7) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | Flavopiridol | Drug Info | IC50 = 110~300 nM | [3] | |
R-roscovitine | Drug Info | Ki = 540 nM | [4] | ||
R547 | Drug Info | IC50 = 1~3 nM | [3] | ||
SNS-032 | Drug Info | Ki = 62 nM | [2] | ||
ZK 304709 | Drug Info | IC50 = 85 nM | [3] | ||
2,5-dichloro-N-p-tolylthiophene-3-sulfonamide | Drug Info | IC50 = 800 nM | |||
PF-228 | Drug Info | IC50 = 197 nM | [1] | ||
Action against Disease Model | ZK 304709 | Drug Info | Blocked growth of h uMan t uMour cell lines at IC50 = 317 nM, by inducing a dose-dependent G1-S arrest followed by apoptosis. Superior efficacy over standard chemotherapy in h uMan t uMour xenografts and orthotopic mouse models of h uMan pancreatic cancer. | [3] | |
References | |||||
REF 1 | Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52. | ||||
REF 2 | 2-Amino-4-methylpyridine as a potent inhibitor of inducible NO synthase activity in vitro and in vivo. Br J Pharmacol. 1996 Nov;119(6):1101-8. | ||||
REF 3 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
REF 4 | A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem. 2010 Dec 23;53(24):8508-22. | ||||
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