Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T20973 | ||||
Target Name | Cyclin-dependent kinase 5 (CDK5) | ||||
Type of Target |
Patented-recorded |
||||
Drug Potency against Target | AT7519 | Drug Info | IC50 = 13 nM | [5] | |
R-roscovitine | Drug Info | IC50 = 270 nM | [5] | ||
SCH 727965 | Drug Info | IC50 < 5 nM | [5] | ||
1-phenyl-3-(2-(pyridin-4-yl)thiazol-4-yl)urea | Drug Info | IC50 = 2990 nM | [2] | ||
3-(2-phenylthiazol-4-yl)quinolin-2(1H)-one | Drug Info | IC50 = 1400 nM | [4] | ||
AZAKENPAULLONE | Drug Info | IC50 = 4200 nM | [1] | ||
KENPAULLONE | Drug Info | IC50 = 850 nM | [1] | ||
MANZAMINE A | Drug Info | IC50 = 1500 nM | [3] | ||
Thieno analogue of kenpaullone | Drug Info | IC50 = 4000 nM | [1] | ||
References | |||||
REF 1 | 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6. | ||||
REF 2 | Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. Bioorg Med Chem. 2007 Oct 15;15(20):6574-95. | ||||
REF 3 | Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for ... J Nat Prod. 2007 Sep;70(9):1397-405. | ||||
REF 4 | Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5384-9. | ||||
REF 5 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
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