enavogliflozin [Ligand Id: 11905] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3703921 (Dwp16001, DWP-16001, Enavogliflozin, ODP-9401, ODP9401) |
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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 | Determined by measuring the uptake of the substrate methyl a-D-glucopyranoside (AMG) in CHO cells expressing hSGLT1. | - | 6.26 | pIC50 | 549 | nM | IC50 | Pharmaceutics (2020) 12: 268 [PMID:32183468] |
| ChEMBL | Inhibition of human SGLT1 expressed in CHO cells by methyl-alpha-D-glucopyranoside assay | B | 6.44 | pIC50 | 359 | nM | IC50 | Bioorg Med Chem Lett (2022) 56: 128466-128466 [PMID:34813882] |
| Sodium/glucose cotransporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3884] [GtoPdb: 916] [UniProtKB: P31639] | ||||||||
| GtoPdb | Determined by measuring the uptake of the substrate methyl a-D-glucopyranoside (AMG) in CHO cells expressing hSGLT2. | - | 9.1 | pIC50 | 0.8 | nM | IC50 | Pharmaceutics (2020) 12: 268 [PMID:32183468] |
| ChEMBL | Inhibition Assay: For sodium-dependent glucose transport assay, cells expressing hSGLT2 were seeded into a 96-well culture plate at a density of 5x104 cells/well in RPMI medium 1640 containing 10% fetal bovine serum. The cells were used 1 day after plating. They were incubated in pretreatment buffer (10 mM HEPES, 5 mM Tris, 140 mM choline chloride, 2 mM KCl, 1 mM CaCl2, and 1 mM MgCl2, pH 7.4) at 37 C. for 10 min. They were then incubated in uptake buffer (10 mM HEPES, 5 mM Tris, 140 mM NaCl, 2 mM KCl, 1 mM CaCl2, 1 mM MgCl2, and 1 mM 14C-nonlabeled AMG pH 7.4) containing 14C-labeled AMG (8 uM) and the inventive compound or dimethyl sulfoxide (DMSO) vehicle at 37 C. for 2 h. Cells were washed twice with washing buffer (pretreatment buffer containing 10 mM AMG at room temperature) and then the radioactivity was measured using a liquid scintillation counter. IC50 was determined by nonlinear regression analysis using GraphPad PRISM [Katsuno, K. et al. J. Pharmacol. Exp. Ther. 2007, 320, 323-330]. | B | 9.33 | pIC50 | 0.46 | nM | IC50 | US-9034921-B2. Diphenylmethane derivatives as SGLT2 inhibitors (2015) |
| ChEMBL | Inhibition of human SGLT2 expressed in CHO cells by methyl-alpha-D-glucopyranoside assay | B | 9.34 | pIC50 | 0.46 | nM | IC50 | Bioorg Med Chem Lett (2022) 56: 128466-128466 [PMID:34813882] |
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]
