ChEMBL ligand: CHEMBL111277
ETA receptor/Endothelin-1 receptor in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] ETA receptor/Endothelin-1 receptor in Rat [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] There should be some charts here, you may need to enable JavaScript!
ETB receptor/Endothelin receptor type B in Human [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] Endothelin receptor type 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-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
ChEMBL	Binding affinity to human ETA receptor transfected in CHO cell membrane assessed as inhibition constant incubated for 3 hrs by 125I-labelled ET-1 saturation binding assay	B	9.7	pKi	0.2	nM	Ki	Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066]
GtoPdb	-	-	9.7	pKi	0.2	nM	Ki	Clin Sci (Lond) (2002) 103 Suppl 48: 107S-111S [PMID:12193066]
ChEMBL	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.	F	9.32	pIC50	0.48	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
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	Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).	B	10.11	pIC50	0.08	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
ChEMBL	Antagonist activity at human ETA receptor transfected in CHO cell membrane assessed as inhibition of 125I-labelled ET-1 binding to receptor incubated for 3 hrs by competition binding assay	F	10.15	pIC50	0.07	nM	IC50	Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066]
ETA receptor/Endothelin-1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684]
ChEMBL	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	B	9.28	pIC50	0.52	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
ChEMBL	Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.	B	9.89	pIC50	0.13	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
ChEMBL	Antagonist activity at ETA receptor in rat MMQ cells assessed as inhibition of phosphatidylinositol hydrolysis by myo-[3H]inositol radioactivity based assay	F	10.3	pIC50	0.05	nM	IC50	Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066]
ETB receptor/Endothelin receptor type B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
GtoPdb	-	-	8.91	pKi	1.23	nM	Ki	Clin Sci (Lond) (2002) 103 Suppl 48: 107S-111S [PMID:12193066]
ChEMBL	Binding affinity to human ETB receptor transfected in CHO cell membrane assessed as inhibition constant incubated for 3 hrs by 125I-labelled ET-1 saturation binding assay	B	8.91	pKi	1.23	nM	Ki	Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066]
ChEMBL	Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.	F	8.89	pIC50	1.28	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
ChEMBL	Antagonist activity at human ETB receptor transfected in CHO cell membrane assessed as inhibition of phosphatidylinositol hydrolysis by myo-[3H]inositol radioactivity based assay	F	8.95	pIC50	1.12	nM	IC50	Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066]
ChEMBL	Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)	B	9.55	pIC50	0.28	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
ChEMBL	Antagonist activity at human ETB receptor transfected in CHO cell membrane assessed as inhibition of 125I-labelled ET-3 binding to receptor incubated for 3 hrs by competition binding assay	F	9.55	pIC50	0.28	nM	IC50	Clin Sci (Lond) (2002) 103 Suppl 48: 107-111 [PMID:12193066]
Endothelin receptor type B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3949] [UniProtKB: P35463]
ChEMBL	Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.	B	9.07	pIC50	0.85	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]
ChEMBL	Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.	B	9.54	pIC50	0.29	nM	IC50	J Med Chem (1997) 40: 3217-3227 [PMID:9379441]

ChEMBL data shown on this page come from version 37:

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]