tofogliflozin [Ligand Id: 9395] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2110731 (CSG-452, R-7201, RO-4998452, RO4998452, Tofogliflozin anhydrous)
  • 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]
GtoPdb Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT1. - 5.07 pIC50 8444 nM IC50 J Med Chem (2012) 55: 7828-40 [PMID:22889351]
ChEMBL Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins B 5.07 pIC50 8444 nM IC50 J Med Chem (2012) 55: 7828-7840 [PMID:22889351]
ChEMBL Inhibition of human SGLT1 B 5.07 pIC50 8444 nM IC50 Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
ChEMBL Inhibition of SGLT2 (unknown origin) B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins B 8.54 pIC50 2.9 nM IC50 J Med Chem (2012) 55: 7828-7840 [PMID:22889351]
ChEMBL Inhibition of human SGLT2 B 8.54 pIC50 2.9 nM IC50 Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
GtoPdb Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT2. - 8.54 pIC50 2.9 nM IC50 J Med Chem (2012) 55: 7828-40 [PMID:22889351]

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]