canagliflozin [Ligand Id: 4582] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2048484 (Canagliflozin, JNJ-24831754-ZAE, JNJ-28431754, JNJ-28431754-AAA, TA-7284) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Sodium/glucose cotransporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866] | ||||||||
| ChEMBL | Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay | B | 5.72 | pIC50 | 1900 | nM | IC50 | Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255] |
| ChEMBL | Inhibition of human SGLT1 | B | 6.16 | pIC50 | 684 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| GtoPdb | - | - | 6.2 | pIC50 | 684 | nM | IC50 | PLoS ONE (2012) 7: e30555 [PMID:22355316] |
| ChEMBL | Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 6.58 | pIC50 | 265 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
| ChEMBL | Inhibition of SGLT1 (unknown origin) | B | 6.04 | pEC50 | 910 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] | ||||||||
| ChEMBL | Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay | B | 8.17 | pIC50 | 6.7 | nM | IC50 | Bioorg Med Chem (2012) 20: 4117-4127 [PMID:22652255] |
| ChEMBL | Inhibition of human SGLT2 | B | 8.36 | pIC50 | 4.4 | nM | IC50 | Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053] |
| GtoPdb | - | - | 8.4 | pIC50 | 4.4 | nM | IC50 | PLoS ONE (2012) 7: e30555 [PMID:22355316] |
| ChEMBL | Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2017) 60: 4173-4184 [PMID:28447791] |
| ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682] |
| ChEMBL | Inhibition of SGLT2 (unknown origin) | B | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
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]
