Table 2. Biological Activity of Alkyne 15 and Halogenated Analoguesa.
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 |
All assays were run in triplicate.
Geometric mean of over 35 assays run in triplicate.