ChEMBL ligand: CHEMBL314691
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120] There should be some charts here, you may need to enable JavaScript!
ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] Endothelin receptor ET-A in Pig [ChEMBL: CHEMBL4130] [UniProtKB: Q29010] 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] ETB receptor/Endothelin receptor ET-B in Rat [ChEMBL: CHEMBL4631] [GtoPdb: 220] [UniProtKB: P21451] 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
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
ChEMBL	TP_TRANSPORTER: inhibition of BQ-485 uptake in bile canalicular membrane vesicles from SD rat	F	4.08	pKi	84100	nM	Ki	J Pharmacol Exp Ther (1999) 288: 575-581 [PMID:9918561]
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
ChEMBL	Affinity against ET A receptor	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem Lett (1995) 5: 253-258
ChEMBL	Antagonist activity at Homo sapiens (human) ETA receptor	B	7.43	pIC50	37	nM	IC50	Med Chem Res (2013) 22: 5472-5480
ChEMBL	Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer	B	7.61	pIC50	24.8	nM	IC50	Bioorg Med Chem Lett (2010) 20: 6840-6844 [PMID:20932745]
ChEMBL	Displacement of [125I]ET-1 from Endothelin A receptor	B	7.66	pIC50	22	nM	IC50	J Med Chem (2004) 47: 1969-1986 [PMID:15055997]
ChEMBL	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	B	7.69	pIC50	20.5	nM	IC50	J Med Chem (2012) 55: 7849-7861 [PMID:22862294]
ChEMBL	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	F	9.21	pIC50	0.62	nM	IC50	Eur J Med Chem (2016) 121: 658-670 [PMID:27318985]
GtoPdb	-	-	7.4	pA2	-	-	Ki	Br J Pharmacol (1995) 115: 191-7 [PMID:7647976]
Endothelin receptor ET-A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4130] [UniProtKB: Q29010]
ChEMBL	Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle	B	4.66	pIC50	22000	nM	IC50	J Med Chem (1992) 35: 1493-1508 [PMID:1315867]
ChEMBL	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.	B	7.66	pIC50	22	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1483-1488
ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684]
ChEMBL	Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor	B	7.4	pKi	40	nM	Ki	J Med Chem (1998) 41: 5198-5218 [PMID:9857090]
ChEMBL	Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr	B	7.55	pIC50	28	nM	IC50	Med Chem Res (2013) 22: 5472-5480
ChEMBL	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	B	7.85	pIC50	14	nM	IC50	J Med Chem (1998) 41: 2732-2744 [PMID:9667964]
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
ChEMBL	Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis	B	6	pIC50	>1000	nM	IC50	J Med Chem (2012) 55: 7849-7861 [PMID:22862294]
Endothelin receptor ET-B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3949] [UniProtKB: P35463]
ChEMBL	Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.	B	4.64	pIC50	23000	nM	IC50	J Med Chem (1992) 35: 1493-1508 [PMID:1315867]
ChEMBL	Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes	B	4.74	pIC50	18000	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1483-1488
ETB receptor/Endothelin receptor ET-B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4631] [GtoPdb: 220] [UniProtKB: P21451]
ChEMBL	Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)	B	4.49	pKi	32000	nM	Ki	J Med Chem (1998) 41: 5198-5218 [PMID:9857090]
ChEMBL	Affinity against ET B receptor	B	5.15	pKi	7000	nM	Ki	Bioorg Med Chem Lett (1995) 5: 253-258
ChEMBL	In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (1998) 41: 2732-2744 [PMID:9667964]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]