irbesartan [Ligand Id: 589] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1513 (Aprovel, Avapro, BMS-186295, Ifirmasta, Irbesartan, Irbesartan bms, Irbesartan teva, Irbesartan zentiva, Karvea, NSC-758696, Sabervel, Sarbevel, SR 47436, SR-47436)
  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
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  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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  • BLT2 receptor/Leukotriene B4 receptor 2 in Human [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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  • AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
  • AT1 receptor/Type-1B angiotensin II receptor in Rat [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
GtoPdb - - 4.92 pKi 11900 nM Ki Mol Pharm (2013) 10: 1008-19 [PMID:23339484]
ChEMBL Inhibition of NTCP (unknown origin) B 4.52 pIC50 30000 nM IC50 Bioorg Med Chem Lett (2019) 29: 126623-126623 [PMID:31439379]
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
ChEMBL Inhibitory concentration against endothelin receptor type A B 5 pKi >10000 nM Ki J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL Binding affinity to ETA receptor B 5 pKi 10000 nM Ki J. Med. Chem. (2012) 55: 9363-9392 [PMID:22931505]
BLT2 receptor/Leukotriene B4 receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1]
ChEMBL Agonist activity at human BLT2 overexpressed in CHO-K1 cells assessed as accumulation of inositol monophosphate measured after 90 mins by HTRF assay F 6.39 pEC50 410 nM EC50 ACS Med Chem Lett (2021) 12: 1261-1266 [PMID:34413955]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL In vitro binding affinity towards Angiotensin II receptor, type 1 of human hepatoma cell line PLC-PRF-5 B 8.7 pKi 2 nM Ki J. Med. Chem. (2002) 45: 4794-4798 [PMID:12361407]
ChEMBL Binding affinity against AT1 in human hepatoma cell line, PLC-PRF-5 B 8.7 pKi 2 nM Ki J. Med. Chem. (2000) 43: 2685-2697 [PMID:10893306]
ChEMBL Compound was evaluated for its binding affinity towards human Angiotensin II receptor, type 1 B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2002) 45: 3829-3835 [PMID:12190306]
ChEMBL Inhibitory concentration against angiotensin II receptor, type 1 B 9.1 pKi 0.8 nM Ki J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL Binding affinity to AT1 receptor B 9.1 pKi 0.8 nM Ki J. Med. Chem. (2012) 55: 9363-9392 [PMID:22931505]
ChEMBL Binding affinity to angiotensin AT1 receptor B 7.68 pIC50 20.8 nM IC50 Bioorg. Med. Chem. (2010) 18: 8418-8456 [PMID:21071232]
ChEMBL Antagonist activity at human AT1 overexpressed in CHO-K1 cells in presence of 10 nM [Val5-angiotensin II measured after 90 mins by HTRF based IP-one assay F 8.22 pIC50 6 nM IC50 ACS Med Chem Lett (2021) 12: 1261-1266 [PMID:34413955]
GtoPdb - - 8.8 pIC50 1.58 nM IC50 Br J Pharmacol (1999) 126: 1057-65 [PMID:10193788]
ChEMBL Displacement of [125I]- Ang II from type 1 Angiotensin II receptor B 9.05 pIC50 0.9 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 1527-1530
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 8.8 pIC50 1.58 nM IC50 Br J Pharmacol (1999) 126: 1057-65 [PMID:10193788]
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
ChEMBL Compound was evaluated for its binding affinity towards rat Angiotensin II receptor, type 1 B 9.1 pKi 0.8 nM Ki J. Med. Chem. (2002) 45: 3829-3835 [PMID:12190306]
ChEMBL Binding affinity for Angiotensin II receptor, type 1 measured by ability to displace [125I]- A II from its specific binding site in rat liver membrane B 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (1993) 36: 3371-3380 [PMID:8230127]
ChEMBL In vitro inhibition of specific binding of [125I]AII to Angiotensin II receptor, type 1 from rat liver membrane B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 157-162

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]