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ChEMBL ligand: CHEMBL1014 (Amias, Atacand, Candesartan 1-(((cyclohexyloxy)carbonyl)oxy)ethyl ester, Candesartan cilexetil, NSC-758697, Ratacand, TCV-116) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Angiotensin II type 1a (AT-1a) receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3948] [UniProtKB: P34976] | ||||||||
ChEMBL | Antagonist activity at angiotensin AT1 receptor in rabbit aortic strip assessed as inhibition of angiotensin 2-induced contractile response | F | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2010) 18: 8418-8456 [PMID:21071232] |
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux and measured after 60 mins using pheophorbide A as fluorescent substrate by flow cytometry | B | 5.3 | pIC50 | 5000 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779] | ||||||||
ChEMBL | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 | B | 4.38 | pIC50 | 42000 | nM | IC50 | J Med Chem (2010) 53: 4259-4265 [PMID:20426472] |
DNA polymerase eta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5542] [UniProtKB: Q9Y253] | ||||||||
ChEMBL | Inhibition of human DNA polymerase eta (1 to 437 residues) preincubated for 15 mins followed by replicating non-damaged DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay | B | 4.95 | pIC50 | 11200 | nM | IC50 | J Med Chem (2016) 59: 9321-9336 [PMID:27362876] |
DNA polymerase iota in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5391] [UniProtKB: Q9UNA4] | ||||||||
ChEMBL | Inhibition of human DNA polymerase iota preincubated for 15 mins followed by replicating non-damaged DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay | B | 5.21 | pIC50 | 6200 | nM | IC50 | J Med Chem (2016) 59: 9321-9336 [PMID:27362876] |
DNA polymerase kappa in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5365] [UniProtKB: Q9UBT6] | ||||||||
ChEMBL | Inhibition of human DNA polymerase kappa (19 to 526 residues) preincubated for 15 mins followed by replicating non-damaged DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay | B | 5.04 | pIC50 | 9200 | nM | IC50 | J Med Chem (2016) 59: 9321-9336 [PMID:27362876] |
ChEMBL | Inhibition of human DNA polymerase kappa (19 to 526 residues)-mediated TLS past acrolein derived ring-opened reduced form of gamma-HOPdG lesions preincubated for 15 mins followed by DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay | B | 5.25 | pIC50 | 5600 | nM | IC50 | J Med Chem (2016) 59: 9321-9336 [PMID:27362876] |
NEDD8-activating enzyme E1 regulatory subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2016431] [UniProtKB: Q13564] | ||||||||
ChEMBL | Inhibition of NAE (unknown origin)-mediated neddylation assessed as suppression of cullin1-Nedd8 adduct formation preincubated for 10 mins followed by ATP addition and measured after 30 mins by immunoblot analysis | B | 4.78 | pIC50 | 16430 | nM | IC50 | Eur J Med Chem (2021) 210: 112964-112964 [PMID:33129593] |
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
ChEMBL | Agonist activity at human PPARgammaDEF receptor expressed in african green monkey COS7 cells transfected with pGal5-TK-pGL3/pRenilla-CMV assessed as intrinsic activity measured after 39 hrs by dual luciferase reporter assay | B | 5.38 | pEC50 | 4200 | nM | EC50 | Eur J Med Chem (2020) 195: 112258-112258 [PMID:32272420] |
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]