sotagliflozin [Ligand Id: 8312] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3039507 (LP-802034, LX4211, LX-4211, Sar439954, Sar-439954, Sotagliflozin)
  • 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 - - 7.44 pIC50 36 nM IC50 Clin Pharmacol Ther (2012) 92: 158-69 [PMID:22739142]
ChEMBL Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method B 7.44 pIC50 36.2 nM IC50 J Med Chem (2017) 60: 710-721 [PMID:28045524]
ChEMBL Inhibition of SGLT1 (unknown origin) B 7.44 pIC50 36 nM IC50 Medchemcomm (2018) 9: 1273-1281 [PMID:30151080]
ChEMBL Inhibition of SGLT1 (unknown origin) B 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2020) 30: 127387-127387 [PMID:32738984]
ChEMBL Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method B 7.46 pIC50 34.6 nM IC50 J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
ChEMBL Inhibition of human SGLT1 B 7.46 pIC50 34.6 nM IC50 J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
ChEMBL Inhibition of human SGLT1 B 7.46 pIC50 34.6 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]
GtoPdb - - 8.74 pIC50 1.8 nM IC50 Clin Pharmacol Ther (2012) 92: 158-69 [PMID:22739142]
ChEMBL Inhibition of SGLT2 (unknown origin) B 8.74 pIC50 1.8 nM IC50 Medchemcomm (2018) 9: 1273-1281 [PMID:30151080]
ChEMBL Inhibition of SGLT2 (unknown origin) B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2020) 30: 127387-127387 [PMID:32738984]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method B 8.82 pIC50 1.5 nM IC50 J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
ChEMBL Inhibition of human SGLT2 B 8.82 pIC50 1.5 nM IC50 J Med Chem (2017) 60: 4173-4184 [PMID:28447791]
ChEMBL Inhibition of human SGLT2 B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]

ChEMBL data shown on this page come from version 32:

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]