Assay Detail
Binding
CHEMBL1108920
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Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of glucose uptake
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.20 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1093422 | — | — | 1 | 8.94 |
| CHEMBL1090821 | — | — | 1 | 8.86 |
| CHEMBL1090786 | — | — | 1 | 8.82 |
| CHEMBL1090820 | — | — | 1 | 8.78 |
| CHEMBL1093777 | — | — | 1 | 8.77 |
| CHEMBL1090822 | — | — | 1 | 8.75 |
| CHEMBL1091946 | — | — | 1 | 8.75 |
| CHEMBL1093423 | LUSEOGLIFLOZIN | 2.0 | 1 | 8.65 |
| CHEMBL1092287 | — | — | 1 | 8.64 |
| CHEMBL1093778 | — | — | 1 | 8.57 |
| CHEMBL1091547 | — | — | 1 | 8.40 |
| CHEMBL1092738 | — | — | 1 | 8.03 |
| CHEMBL1090560 | — | — | 1 | 7.97 |
| CHEMBL1091966 | — | — | 1 | 7.87 |
| CHEMBL1091947 | — | — | 1 | 7.76 |
| CHEMBL1093013 | — | — | 1 | 7.73 |
| CHEMBL245067 | PHLORIZIN | — | 1 | 7.56 |
| CHEMBL1091948 | — | — | 1 | 7.42 |
| CHEMBL1092273 | — | — | 1 | 7.13 |
| CHEMBL1092274 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1093422 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL1090821 | — | IC50 | = | 1.37 | nM | 8.86 |
| CHEMBL1090786 | — | IC50 | = | 1.51 | nM | 8.82 |
| CHEMBL1090820 | — | IC50 | = | 1.68 | nM | 8.78 |
| CHEMBL1093777 | — | IC50 | = | 1.71 | nM | 8.77 |
| CHEMBL1090822 | — | IC50 | = | 1.78 | nM | 8.75 |
| CHEMBL1091946 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL1093423 | LUSEOGLIFLOZIN | IC50 | = | 2.26 | nM | 8.65 |
| CHEMBL1092287 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL1093778 | — | IC50 | = | 2.68 | nM | 8.57 |
| CHEMBL1091547 | — | IC50 | = | 4.01 | nM | 8.40 |
| CHEMBL1092738 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL1090560 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL1091966 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL1091947 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL1093013 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL245067 | PHLORIZIN | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL1091948 | — | IC50 | = | 37.9 | nM | 7.42 |
| CHEMBL1092273 | — | IC50 | = | 73.6 | nM | 7.13 |
| CHEMBL1092274 | — | IC50 | = | 283.0 | nM | 6.55 |