bexagliflozin [Ligand Id: 12335] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1808388 (Bexagliflozin, Bexagliflozina, Bexagliflozine, Brenzavvy, EGT-0001442, EGT0001442, EGT-1442, EGT1442, THR-1442, THR1442)
  • 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 - - 5.25 pIC50 5600 nM IC50 Bioorg Med Chem Lett (2011) 21: 4465-70 [PMID:21737266]
ChEMBL Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma B 5.25 pIC50 5600 nM IC50 Bioorg Med Chem Lett (2011) 21: 4465-4470 [PMID:21737266]
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
ChEMBL Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma B 8.64 pIC50 2.3 nM IC50 Bioorg Med Chem Lett (2011) 21: 4465-4470 [PMID:21737266]
GtoPdb - - 8.64 pIC50 2.3 nM IC50 Bioorg Med Chem Lett (2011) 21: 4465-70 [PMID:21737266]

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]