Table 1. Biochemical and cellular activity of small-molecule BCL-2 family inhibitors.

For each compound listed, binding affinities (Ki) for BCL-2 family proteins were calculated in time-resolved fluorescence resonance energy transfer (TR-FRET) assays, and the effects on cell viability [median effective concentration (EC50)] were assessed in BCL-2–dependent (RS4;11) or BCL-XL–dependent (Molt-4) cancer cell lines. All values are in nanomolar units.

BCL-XL/BCL-2BCL-2–selectiveBCL-XL–selective
NavitoclaxA-874009VenetoclaxA-1211212A-1155463A-1331852
BCL-2 TR-FRET0.0440.048<0.010<0.010746
BCL-XL TR-FRET0.0550.4634814<0.010<0.010
MCL-1 TR-FRET>224>3900>444>444>444142
BCL-W TR-FRET21224585284
Molt-4 viability303134>5000>5000706
RS4;11 viability1122886>5000>5000