canagliflozin [Ligand Id: 4582] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2048484 (Canagliflozin anhydrous, JNJ-28431754, 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 SGLT1 (unknown origin) | B | 6.15 | pIC50 | 710 | nM | IC50 | J Med Chem (2023) 66: 12536-12543 [PMID:37608596] |
| 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 SGLT2 (unknown origin) | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (2023) 66: 12536-12543 [PMID:37608596] |
| 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 human SGLT2 by liquid scintillation counter analysis | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2023) 66: 991-1010 [PMID:36584305] |
| 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 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]
