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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