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. 2014 Aug 26;5(10):1088–1093. doi: 10.1021/ml5001867

Table 2. Biological Activity of Alkyne 15 and Halogenated Analoguesa.

graphic file with name ml-2014-001867_0003.jpg

compound halogen position BCL-XLKi (nM) BCL-XL 1% HS Ki (nM) BCL-2 Ki (nM) H146 10% HS EC50 (μM)
15 none 0.02 0.28 60 0.60
16 2-Cl 0.04 0.41 280 0.18
17 (A-1155463) 2-F <0.01 0.10 80 0.065b
18 3-F 0.01 1.12 88 0.051
19 2-F, 5-F 0.03 0.33 90 0.126
a

All assays were run in triplicate.

b

Geometric mean of over 35 assays run in triplicate.