CRTH2 antagonist
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: PTGDR2: Ki = 2.5 nM (Prostanoid receptor binding assay) |
| Selectivity within target family: > 30-fold | Surpasses criterion: > 100-fold against related receptors; Hits in the PDSP scan are SLC6A3 (Ki = 283 nM), GABA/PBR (Ki = 1115 nM) and DRD2 (Ki = 3746 nM); Prostanoid receptor binding assay: TBXA2R (Ki = 3804 nM); |
| Selectivity outside target family | No relevant activity < 10 µM |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: cAMP Functional Assay: IC50 = 3 nM (HEK-CRTH2 cells) ; Eosinophil Shape Change (whole blood): IC50 = 2.2 nM; Eosinophil CD11b (whole blood): IC50 = 2.3 nM |
| Control compound (100 times less potent than the probe) | Surpasses criterion: The control is > 100-fold less potent biochemically and shows no activity in cells @ 10 µM. PTGDR2: Ki = 1083 nM (Prostanoid receptor binding assay); cAMP Functional Assay: IC50 > 10 µM; Clean PDSP scan |