ABT-546
Probe criteria
| Inhibitor/agonist potency: goal is < 50 nM (IC50, KD) | EDNRA: Ki = 0.46 nM |
| Selectivity within target family: > 30-fold | EDNRB: Ki = 13000 nM; Clean PDSP scanCEREP panel of receptors (at 10 µM): closest hits: EDNRB = 56% inhibition; OPRD1 (opioid receptor delta 1) = 62 % inhibition |
| Selectivity outside target family | CEREP panel for other targets: clean |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells: IC50 = 0.59 nM; Rat aortic ring contraction: EC50 = 1.1 nM |
| Control compound (100 times less potent than the probe) | Surpasses criteria; in vitro: >200-fold less potent; Shows activity on other GPCRs: closest hit is DRD4 (pKi = 8.26). For others check the PDSP scan data. |