Target Validation Information
Target ID T66719
Target Name Heat shock protein HSP90
Target Type
Clinical Trial
Drug Potency against Target SNX-2112 Drug Info IC50 = 22 nM [530621]
Geldanamycin Drug Info IC50 = 281 nM [552578]
ZEARALANONE Drug Info IC50 = 2197.6 nM [531262]
RHEIN Drug Info IC50 = 3339.3 nM [531262]
17-desmethoxy-17-aminogeldanamycin Drug Info IC50 = 12 nM [530621]
GNF-PF-67 Drug Info IC50 < 1875 nM [531262]
17-allylamino-17-desmethoxy-geldanamycin Drug Info IC50 = 15 nM [529815]
CCT-018159 Drug Info IC50 = 3000 nM [552620]
VER-49009 Drug Info IC50 = 140 nM [527601]
References
Ref 530621J Med Chem. 2010 Jan 14;53(1):3-17.Heat shock protein 90: inhibitors in clinical trials.
Ref 552578A fluorescence polarization assay for inhibitors of Hsp90. Anal Biochem. 2006 Mar 15;350(2):202-13. Epub 2006 Jan 23.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 530621J Med Chem. 2010 Jan 14;53(1):3-17.Heat shock protein 90: inhibitors in clinical trials.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 529815Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. Epub 2008 Nov 6.Discovery and development of heat shock protein 90 inhibitors.
Ref 552620Discovery and development of pyrazole-scaffold Hsp90 inhibitors. Curr Top Med Chem. 2006;6(11):1193-203.
Ref 527601J Med Chem. 2005 Jun 30;48(13):4212-5.Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.

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