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

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ChEMBL ligand: CHEMBL2110731 (Tofogliflozin)
  • 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 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]