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ABT-546

2D structure
Target EDNRA 
Mode of action Antagonist
Control A-545
Recommended cellular usage concentration ≤ 100 nM
In vivo use yes
Synonyms A-216546
Donated by Abbvie


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 scan
CEREP 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.