candesartan cilexetil [Ligand Id: 8352] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1014 (Amias, Atacand, Candesartan, 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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
