Target Validation Information
TTD ID	T18477
Target Name	Heat shock protein 90 alpha (HSP90A)
Type of Target	Successful
Drug Potency against Target	Alvespimycin hydrochloride	Drug Info	IC50 = 68 nM	[5]
	Ganetespib	Drug Info	IC50 < 36 nM
	Geldanamycin	Drug Info	IC50 = 281 nM	[6]
	Retaspimycin	Drug Info	IC50 = 80000 nM	[10]
	Tanespimycin	Drug Info	IC50 = 33 nM	[7]
	CCT-018159	Drug Info	IC50 = 3000 nM	[8]
		Drug Info	IC50 = 15 nM	[2]
	17-desmethoxy-17-aminogeldanamycin	Drug Info	IC50 = 12 nM	[3]
	GNF-PF-67	Drug Info	IC50 < 1875 nM	[4]
	GNF-PF-67	Drug Info	IC50 < 1875 nM	[4]
	RHEIN	Drug Info	IC50 = 3339.3 nM	[4]
	RHEIN	Drug Info	IC50 = 3339.3 nM	[4]
	SNX-2112	Drug Info	IC50 = 22 nM	[3]
	VER-49009	Drug Info	IC50 = 140 nM	[1]
	VER-49009	Drug Info	IC50 = 25 nM	[1]
	ZEARALANONE	Drug Info	IC50 = 2197.6 nM	[4]
	ZEARALANONE	Drug Info	IC50 = 2197.6 nM	[4]
Action against Disease Model	Retaspimycin	Drug Info	IPI-504 induces cytotoxicity in MM cells in a dose-dependent manner with an EC50 of growth inhibition of about 300 nM after 72 h incubation	[9]
References
REF 1	Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. J Med Chem. 2005 Jun 30;48(13):4212-5.
REF 2	Discovery and development of heat shock protein 90 inhibitors. Bioorg Med Chem. 2009 Mar 15;17(6):2225-35.
REF 3	Heat shock protein 90: inhibitors in clinical trials. J Med Chem. 2010 Jan 14;53(1):3-17.
REF 4	In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
REF 5	Stage 1 testing and pharmacodynamic evaluation of the HSP90 inhibitor alvespimycin (17-DMAG, KOS-1022) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jul;51(1):34-41.
REF 6	A fluorescence polarization assay for inhibitors of Hsp90. Anal Biochem. 2006 Mar 15;350(2):202-13.
REF 7	Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site. Curr Top Med Chem. 2006;6(11):1173-82.
REF 8	Discovery and development of pyrazole-scaffold Hsp90 inhibitors. Curr Top Med Chem. 2006;6(11):1193-203.
REF 9	IPI-504, a novel and soluble HSP-90 inhibitor, blocks the unfolded protein response in multiple myeloma cells. Cancer Chemother Pharmacol. 2008 May;61(6):923-32.
REF 10	Recent advances in the research of HIV-1 RNase H inhibitors. Mini Rev Med Chem. 2008 Oct;8(12):1243-51.

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