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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