ipragliflozin [Ligand Id: 9394] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2018096 (ASP-1941, Ipragliflozin, Ipragliflozina, Ipragliflozine)
  • Sodium/glucose cotransporter 1 in Human [ChEMBL: CHEMBL4979] [GtoPdb: 915] [UniProtKB: P13866]
  • Sodium/glucose cotransporter 1 in Mouse [GtoPdb: 915] [UniProtKB: Q8C3K6]
  • Sodium/glucose cotransporter 1 in Rat [GtoPdb: 915] [UniProtKB: P53790]
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  • Sodium/glucose cotransporter 2 in Human [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
  • Sodium/glucose cotransporter 2 in Mouse [GtoPdb: 916] [UniProtKB: Q923I7]
  • Sodium/glucose cotransporter 2 in Rat [GtoPdb: 916] [UniProtKB: P53792]
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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]
ChEMBL Inhibition of human SGLT1 B 5.73 pIC50 1876 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 hSGLT1. - 5.73 pIC50 1876 nM IC50 Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434]
ChEMBL Inhibition of SGLT1 (unknown origin) B 5.72 pEC50 1900 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
Sodium/glucose cotransporter 1 in Mouse [GtoPdb: 915] [UniProtKB: Q8C3K6]
GtoPdb Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing mSGLT1. - 5.86 pIC50 1380 nM IC50 Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434]
Sodium/glucose cotransporter 1 in Rat [GtoPdb: 915] [UniProtKB: P53790]
GtoPdb Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing rSGLT1. - 5.93 pIC50 1166 nM IC50 Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434]
Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639]
ChEMBL Inhibition of SGLT2 (unknown origin) B 8.08 pIC50 8.4 nM IC50 Bioorg Med Chem (2018) 26: 3947-3952 [PMID:29954682]
GtoPdb Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing hSGLT2. - 8.13 pIC50 7.38 nM IC50 Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434]
ChEMBL Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG accumulation after 2 hrs by scintillation counting B 8.13 pIC50 7.4 nM IC50 Bioorg Med Chem (2012) 20: 3263-3279 [PMID:22507206]
ChEMBL Inhibition of recombinant human full-length SGLT2 expressed in CHO cells assessed as decrease in [14C]-AMG uptake measured after 2 hrs by topcount scintillation counting method B 8.13 pIC50 7.4 nM IC50 Medchemcomm (2018) 9: 1273-1281 [PMID:30151080]
ChEMBL Inhibition of human SGLT2 B 8.13 pIC50 7.38 nM IC50 Eur J Med Chem (2019) 184: 111773-111773 [PMID:31630053]
ChEMBL Inhibition of SGLT2 (unknown origin) B 8.13 pEC50 7.4 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
Sodium/glucose cotransporter 2 in Mouse [GtoPdb: 916] [UniProtKB: Q923I7]
GtoPdb Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing mSGLT2. - 8.25 pIC50 5.64 nM IC50 Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434]
Sodium/glucose cotransporter 2 in Rat [GtoPdb: 916] [UniProtKB: P53792]
GtoPdb Measuring inhibition of sodium-dependent [14C]AMG-uptake in CHO cells expressing rSGLT2. - 8.2 pIC50 6.37 nM IC50 Naunyn Schmiedebergs Arch Pharmacol (2012) 385: 423-36 [PMID:22139434]

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]