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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 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]