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. Author manuscript; available in PMC: 2011 May 27.
Published in final edited form as: J Med Chem. 2010 May 27;53(10):4166–4176. doi: 10.1021/jm1001265

Table 2.

Cross-activity of Diastereoisomers of 4 against Bcl-XL, Bcl-2, Mcl-1 and Bfl-1 in Fluorescence Polarization displacement assays and binding to Bcl-xL as measured via Isothermal Titration Calorimetry.

Compound IC50 (μM) FPA Kd (μM) ITC
IC50 Bcl-XL Bcl-2 Bfl-1 Mcl-1 Bcl-XL
11 0.31 ± 0.05 0.32 ± 0.05 0.62 ± 0.04 0.20 ± 0.02 0.1
12 0.68 ± 0.09 1.14 ± 0.09 0.59 ± 0.07 0.18 ± 0.02 2.4
13 0.44 ± 0.02 0.43 ± 0.01 0.75 ± 0.07 0.24 ± 0.02 0.4
14 0.65 ± 0.06 0.43 ± 0.03 0.77 ± 0.05 0.24 ± 0.02 2.0
4 0.39 ± 0.02 0.66 ± 0.02 0.42 ± 0.09 0.33 ± 0.02 ND

ND = Not determined