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

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ChEMBL ligand: CHEMBL3039507 (Inpefa, LP-802034, LX-4211, LX4211, Sar-439954, Sar439954, Sotagliflozin, Zynquista)
  • 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 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]