Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T31309 | ||||
Target Name | Apoptosis regulator Bcl-2 (BCL-2) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | ABT-263 | Drug Info | Ki = 0.5 nM | [6] | |
MCI-186 | Drug Info | IC50 = 270 nM | [5] | ||
2,3,4-trihydroxy-5-isopropyl-N-phenyl-benzamide | Drug Info | IC50 = 7000 nM | [2] | ||
4,5-dibenzylbenzene-1,2-diol | Drug Info | IC50 = 4700 nM | [4] | ||
5,10-Dioxy-2-phenyl-benzo[g]pteridin-4-ylamine | Drug Info | IC50 = 1600 nM | [1] | ||
ABT-737 | Drug Info | Ki < 1 nM | [3] | ||
N-phenyl-2,3,4-trihydroxy-5-benzyl-benzamide | Drug Info | IC50 = 5000 nM | [2] | ||
QEDIIRNIARHLAQVGDSMDR | Drug Info | Ki = 11 nM | [2] | ||
TW-37 | Drug Info | IC50 = 200 nM | [2] | ||
References | |||||
REF 1 | Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening. J Med Chem. 2001 Dec 6;44(25):4313-24. | ||||
REF 2 | Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. J Med Chem. 2006 Oct 19;49(21):6139-42. | ||||
REF 3 | Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J Med Chem. 2007 Feb 22;50(4):641-62. | ||||
REF 4 | Vaccinia virus virulence factor N1L is a novel promising target for antiviral therapeutic intervention. J Med Chem. 2010 May 27;53(10):3899-906. | ||||
REF 5 | A newly synthesized poly(ADP-ribose) polymerase inhibitor, DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: pharmacological ... J Pharmacol Exp Ther. 2005 Feb;312(2):472-81. | ||||
REF 6 | BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. | ||||
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