ChEMBL ligand: CHEMBL1111 (Ambrisentan, GSK1325760, GSK-1325760, GSK1325760A, GSK-1325760A, Letairis, LU-208075, Volibris)
ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] There should be some charts here, you may need to enable JavaScript!
ETB receptor/Endothelin receptor ET-B in Human [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] There should be some charts here, you may need to enable JavaScript!
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
GtoPdb	-	-	7.66	pIC50	21.7	nM	IC50	J Med Chem (2004) 47: 2776-95 [PMID:15139756]
ChEMBL	Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	F	7.66	pIC50	21.7	nM	IC50	J. Med. Chem. (2004) 47: 2776-2795 [PMID:15139756]
ChEMBL	Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	B	9	pIC50	1	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]
GtoPdb	-	-	7.1	pA2	-	-	-	J Med Chem (2004) 47: 2776-95 [PMID:15139756]
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
GtoPdb	-	-	5.92	pIC50	1190	nM	IC50	J Med Chem (2004) 47: 2776-95 [PMID:15139756]
ChEMBL	Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand	F	5.92	pIC50	1190	nM	IC50	J. Med. Chem. (2004) 47: 2776-2795 [PMID:15139756]
ChEMBL	Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting	B	6.71	pIC50	195	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787]
ChEMBL	Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform	F	4.2	pIC50	63095.73	nM	IC50	J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]