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. Author manuscript; available in PMC: 2022 May 3.
Published in final edited form as: Angew Chem Int Ed Engl. 2021 Mar 26;60(19):10547–10551. doi: 10.1002/anie.202015422

Table 2:

Installation of substituted thiophenols and evaluation of binding affinity IC50 determined using fluorescence polarization (FP) assay. Compounds were incubated with Hsp90α/β and FITC-GDA in triplicates and ± SD was measured.

graphic file with name nihms-1679691-t0007.jpg
Compound IC50 Hsp90α (μM)(a) IC50Hsp90β (μM)(a) Fold Selectivity
12a 0.71 ± 0.03 >50 >70
12b 0.52 ± 0.01 27.7±3.07 ~53
12c 0.53 ± 0.07 11.6±1.07 ~22
12d 0.84 ± 0.13 >50 >63
12e 0.72 ± 0.08 37.5±3.8 ~51
12f 3.03±0.26 >50 >16
12g 0.9±0.02 >50 >16
12h 0.46±0.05 22.28±2.8 ~48