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ChEMBL ligand: CHEMBL9194 (A-127722, Atrasentan) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]