BI-113823
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Radioligand binding assay (displacement of kallidin) at 10 µM: hBDKRB1 (Ki = 5.3 nM), rat (Ki = 13.3 nM), rabbit (Ki = 15.3 nM) |
| Selectivity within target family: > 30-fold | Radioligand binding assay at 10 µM: hBDKRB2 Ki > 10 µM |
| Selectivity outside target family | Eurofins SafteyScreen (69 targets) at 10 µM: Closest off-targets are SIGMAR1 (70 % inh.), TMEM97 (55 % inh.) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Cellular assay (Measurement of intracellular calcium in HEK-cells expressing hBDKRB1): IC50 = 7 nM |
| Control compound (100 times less potent than the probe) | BI-5832: Radioligand binding assay at 10 µM: hBDKRB1 (Ki = 431 nM); Cellular assay: IC50 = 699 nM; Eurofins SafteyScreen (44 targets) at 10 µM: clean except for OPRK1 (58 % inh.) |