Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | solute carrier family 5 (sodium/glucose cotransporter), member 2 | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | solute carrier family 5 | 0.0181 | 0.5 | 0.5 |
Schistosoma mansoni | inositol transporter | 0.0181 | 0.5 | 0.5 |
Schistosoma mansoni | inositol transporter | 0.0181 | 0.5 | 0.5 |
Echinococcus granulosus | sodium:glucose cotransporter 2 | 0.0181 | 0.5 | 0.5 |
Echinococcus multilocularis | sodium:glucose cotransporter 2 | 0.0181 | 0.5 | 0.5 |
Echinococcus granulosus | sodium:myo inositol cotransporter | 0.0181 | 0.5 | 0.5 |
Echinococcus multilocularis | sodium:myo inositol cotransporter | 0.0181 | 0.5 | 0.5 |
Echinococcus granulosus | solute carrier family 5 | 0.0181 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 9.08 nM | BindingDB_Patents: 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]. | ChEMBL. | No reference |
IC50 (binding) | = 9.08 nM | BindingDB_Patents: 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]. | ChEMBL. | No reference |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.