atrasentan [Ligand Id: 3487] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL9194 (A-127722, Atrasentan)
  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
  • ETA receptor/Endothelin receptor ET-A in Rat [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684]
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  • ETB receptor/Endothelin receptor ET-B in Human [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
  • Endothelin receptor ET-B in Pig [ChEMBL: CHEMBL3949] [UniProtKB: P35463]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]