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. Author manuscript; available in PMC: 2010 Jul 23.
Published in final edited form as: J Med Chem. 2009 Jul 23;52(14):4511–4523. doi: 10.1021/jm900472s

Table 3.

Cross-activity of selected 5, 5′ substituted compound 2 derivatives against Bcl-XL, Bcl-2, Mcl-1 and Bfl-1.

Compound IC50 (μM) FPA Kd (μM) ITC
IC50 Bcl-XL Bcl-2 Mcl-1 Bfl-1 Bcl-XL
2 3.7 4.3 2.6 >10 1.7
12e 3.5 0.48 0.83 5.0 0.41
8m 1.1 0.71 0.78 2.0 0.85
8n 0.80 0.15 0.30 0.55 ND
8p 6.3 4.4 3.2 NDa* ND
8q 0.93 0.67 0.59 1.3 0.12
8j 0.8 0.70 1.1 ND ND
8k 0.27 0.49 0.23 0.40 0.11
8r 0.76 0.32 0.28 0.73 0.11
8s 0.85 0.70 0.35 0.67 ND
a*

ND = Not determined