. Author manuscript; available in PMC: 2014 Apr 14.

Published in final edited form as: J Med Chem. 2013 Aug 21;56(17):6803–6818. doi: 10.1021/jm400619b

Table 1.

Hsp90 Paralogue Affinity Determined for Hsp90 Inhibitors in Clinical Development Using 16a as a FP Probe^a

	Hsp90α IC₅₀ (nM)	Hsp90β IC₅₀ (nM)	Grp94 IC₅₀ (nM)	Trap-1 IC₅₀ (nM)
1	28	22	10	661
2	46	45	31	1496
3	19	17	124	90
4	43	42	30	205
5	33	38	190	1586
6	29	25	578	726
7	20	16	12	38
8	5	5	10	51
ADP	59308	42159	11447	55594
ATP	861330	893677	3241	31303

The paralogue binding affinity of Hsp90-regulatory nucleotides is also presented.