BI-2545
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Human ENPP2: IC50 = 2.2 nM (LPA measurement) |
| Selectivity within target family: > 30-fold | NA |
| Selectivity outside target family | At 10 µM (CEREP): 4/48 off targets >50% (HTR2A, Ca2+ channel, Na+ channel, SLC6A2); Shows weak activity on the PDSP scan with the closest hit on GABA/PBR (Ki = 2555.91 nM) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Whole blood assay: human ENPP2 (IC50 = 29 nM); rat ENPP2 (IC50 = 96 nM) |
| Control compound (100 times less potent than the probe) | BI-3017: human ENPP2 IC50 = 8900 nM (LPA measurement); Clean PDSP scan |