ChEMBL ligand: CHEMBL9194 (A-127722, Atrasentan)
ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] ETA receptor/Endothelin receptor ET-A in Rat [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] 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] Endothelin receptor ET-B in Pig [ChEMBL: CHEMBL3949] [UniProtKB: P35463] 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]
ChEMBL	Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cells	B	10.47	pKi	0.03	nM	Ki	J Med Chem (1996) 39: 1039-1048 [PMID:8676339]
ChEMBL	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	B	10.47	pKi	0.03	nM	Ki	J Med Chem (2016) 59: 8168-8188 [PMID:27266371]
GtoPdb	CHO cells expressing human ETA receptor.	-	10.47	pKi	0.03	nM	Ki	J Pharmacol Exp Ther (1996) 276: 473-81 [PMID:8632312]; J Med Chem (1996) 39: 1039-48 [PMID:8676339]
ChEMBL	Displacement of [125I]ET-1 from Endothelin A receptor	B	9.51	pIC50	0.31	nM	IC50	J Med Chem (2004) 47: 1969-1986 [PMID:15055997]
ChEMBL	Binding affinity towards human Endothelin A receptor (hET -A)	B	10.1	pIC50	0.08	nM	IC50	J Med Chem (1999) 42: 3668-3678 [PMID:10479298]
ChEMBL	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	B	10.26	pIC50	0.06	nM	IC50	J Med Chem (2016) 59: 8168-8188 [PMID:27266371]
ChEMBL	Ability to displace endothelin ([125I]ET1) from human Endothelin A receptor	B	10.47	pIC50	0.03	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
ChEMBL	Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor	B	10.47	pIC50	0.03	nM	IC50	J Med Chem (1999) 42: 3679-3689 [PMID:10479299]
GtoPdb	-	-	9.2	pA2	-	-	-	J Pharmacol Exp Ther (1996) 276: 473-81 [PMID:8632312]
ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684]
ChEMBL	binding affinity against human Endothelin A receptor	B	10.33	pKi	0.05	nM	Ki	J Med Chem (2001) 44: 3978-3984 [PMID:11689084]
ChEMBL	Binding affinity towards Endothelin A receptor	B	10.47	pKi	0.03	nM	Ki	J Med Chem (2004) 47: 1969-1986 [PMID:15055997]
ChEMBL	In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor	B	8.82	pIC50	1.5	nM	IC50	Bioorg Med Chem Lett (1998) 8: 1771-1776 [PMID:9873432]
ChEMBL	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	B	9.4	pIC50	0.4	nM	IC50	J Med Chem (1997) 40: 322-330 [PMID:9022798]
ChEMBL	Binding affinity against Endothelin A receptor in MMQ cells in rat	B	9.44	pIC50	0.36	nM	IC50	J Med Chem (2001) 44: 3978-3984 [PMID:11689084]
ChEMBL	Inhibitory activity against the Endothelin A receptor of rat MMQ cells	B	9.51	pIC50	0.31	nM	IC50	J Med Chem (1996) 39: 1039-1048 [PMID:8676339]
ChEMBL	Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.	B	9.51	pIC50	0.31	nM	IC50	J Med Chem (2004) 47: 2750-2760 [PMID:15139753]
ChEMBL	Inhibitory activity against human Endothelin A receptor	B	10.1	pIC50	0.08	nM	IC50	J Med Chem (2001) 44: 3978-3984 [PMID:11689084]
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
GtoPdb	CHO cells expressing human ETB receptor.	-	6.86	pKi	138	nM	Ki	J Med Chem (1996) 39: 1039-48 [PMID:8676339]
ChEMBL	Binding affinity against endothelin B receptor in porcine cerebellar tissue	B	6.29	pIC50	515	nM	IC50	J Med Chem (2001) 44: 3978-3984 [PMID:11689084]
ChEMBL	Inhibitory activity against human endothelin B receptor	B	7.06	pIC50	88	nM	IC50	J Med Chem (2001) 44: 3978-3984 [PMID:11689084]
ChEMBL	Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor	B	7.2	pIC50	63.3	nM	IC50	J Med Chem (1999) 42: 3679-3689 [PMID:10479299]
Endothelin receptor ET-B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3949] [UniProtKB: P35463]
ChEMBL	Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.	B	6.28	pIC50	520	nM	IC50	J Med Chem (1997) 40: 322-330 [PMID:9022798]
ChEMBL	Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellum	B	6.72	pIC50	191	nM	IC50	J Med Chem (1996) 39: 1039-1048 [PMID:8676339]
ChEMBL	In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor	B	6.96	pIC50	110	nM	IC50	Bioorg Med Chem Lett (1998) 8: 1771-1776 [PMID:9873432]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]