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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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | Binding affinity to NTCP (unknown origin) | B | 4.92 | pKi | 11900 | nM | Ki | J Med Chem (2022) 65: 12546-12561 [PMID:36111355] |
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 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-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095] | ||||||||
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/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] |
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 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]