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ChEMBL ligand: CHEMBL314691 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]