BAY-386
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) | Surpasses criterion: Binding assay (platelet membranes) IC50 = 56 nM |
| Selectivity within target family: > 30-fold | Surpasses criterion: F2RL3 (PAR4): Functional cellular assay (HEK cells) IC50 > 10 µM ( > 1,000 fold selectivity) Eurofins-Cerep cellular and nuclear receptor functional assay screen (25) at 10 µM: Closest off-target: CNR1 (80.7 % Inhibition of control agonist response) CNR1 functional test (GTPγS binding): IC50 = 10.6 µM Eurofins-Panlabs radioligand binding assay (68) at 10 µM: Closest hit: CNR1 (88 % inhibition) One hit in the PDSP scan: TMEM97 (pKi = 5.94). |
| Selectivity outside target family | Surpasses criterion: Eurofins-Panlabs radioligand binding assay (68) at 10 µM: Closest hit outside the GPCR family is the Sarcolemmal Na+ channel site 2 (55 % inhibition) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: Functional cellular assay (HEK-cells): IC50 = 10 nM |
| Control compound (100 times less potent than the probe) | Surpasses criterion: Functional cellular assays (HEK cells): > 1,000 times less active on F2R (IC50 >10 µM) and F2RL3 (IC50 >> 5 µM); Binding assay (platelet membranes): IC50 > 10 µM); Eurofins-Cerep cellular and nuclear receptor functional assay screen (25) at 10 µM: clean; Clean PDSP scan |