Assay Detail
Binding
CHEMBL961709
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Inhibition of human kidney SGLT2 assessed as renal glucose reabsorption
12
Total Activities
8
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 7.78 | 8.96 |
| Ki | 3 | 8.09 | 8.62 |
| IC50 | 1 | 7.30 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.96 |
| CHEMBL270766 | SERGLIFLOZIN A | — | 2 | 8.62 |
| CHEMBL183937 | — | — | 2 | 8.18 |
| CHEMBL3958686 | REMOGLIFLOZIN | -1.0 | 2 | 7.91 |
| CHEMBL245067 | PHLORIZIN | — | 2 | 7.73 |
| CHEMBL488696 | — | — | 1 | 7.66 |
| CHEMBL429911 | — | — | 1 | 6.30 |
| CHEMBL494396 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL270766 | SERGLIFLOZIN A | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL183937 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL270766 | SERGLIFLOZIN A | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3958686 | REMOGLIFLOZIN | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL3958686 | REMOGLIFLOZIN | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL245067 | PHLORIZIN | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL488696 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL245067 | PHLORIZIN | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL183937 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL429911 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL494396 | — | EC50 | > | 2.0 | nM | - |