canagliflozin [Ligand Id: 4582] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2048484 (JNJ-28431754-AAA, Canagliflozin, JNJ-24831754-ZAE, JNJ-28431754, TA-7284)
  • Sodium/glucose cotransporter 1 in Human [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866]
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  • Sodium/glucose cotransporter 2 in Human [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]