Assay Detail
Binding
CHEMBL947997
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Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.70 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.96 |
| CHEMBL183937 | — | — | 1 | 8.18 |
| CHEMBL270766 | SERGLIFLOZIN A | — | 1 | 8.04 |
| CHEMBL245067 | PHLORIZIN | — | 1 | 7.45 |
| CHEMBL429911 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL183937 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL270766 | SERGLIFLOZIN A | EC50 | = | 9.2 | nM | 8.04 |
| CHEMBL245067 | PHLORIZIN | EC50 | = | 35.6 | nM | 7.45 |
| CHEMBL429911 | — | EC50 | = | 1300.0 | nM | 5.89 |