Table 1. Results of TR-FRET Based Binding Assay for ABL1 (Allosteric Site), cIAP1/2, and XIAPa.
| compd | ABL1 IC50 (nM) | cIAP1 IC50 (nM) | cIAP2 IC50 (nM) | XIAP IC50 (nM) |
|---|---|---|---|---|
| 1 (GNF-2) | 2800 (2000–4000) | n.d. | n.d. | n.d. |
| 2 (GNF-5) | 2000 (1400–2900) | n.d. | n.d. | n.d. |
| 3 (ABL001 derivative) | 35 (27–45) | n.d. | n.d. | n.d. |
| 4 (LCL-161 derivative) | n.d. | 4.8 (4.3–5.4) | 5.7 (4.3–7.5) | 67 (49–96) |
| 5 (SNIPER(ABL)-21) | 2000 (1200–3300) | 220 (180–280) | 330 (220–500) | 94 (70–130) |
| 6 (SNIPER(ABL)-62) | 360 (220–590) | 86 (78–94) | 140 (120–160) | 120 (99–140) |
| 7 (SNIPER(ABL)-64) | 340 (210–570) | >1000 | >1000 | >1000 |
a
The inhibitory activity of the test compounds at several concentrations were examined as described in Supporting Information. IC50 values and 95% confidence intervals were calculated by nonlinear regression analysis of percent inhibition data (n ≥ 3). n.d.: not determined.