PF-04418948
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Inhibition of binding to PTGER2: IC50 = 5 nM |
| Selectivity within target family: > 30-fold | No agonist activity is observed across the family. Clean PDSP scan. |
| Selectivity outside target family | With the exception of LTB4R (960 fold), MT3 (104 fold) and PDE3A (700 fold), no significant off-target pharmacology in CEREP wide-ligand profiling at 10 μM. Antagonist activity: IC50 = 16 nM. |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Functional native assay: human myometrium KB = 5.4 nM |
| Control compound (100 times less potent than the probe) | Inhibition of binding to PTGER2: IC50 = 1.3 µM; Clean PDSP scan |