Assay Detail
Binding
CHEMBL4015645
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Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.44 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3039507 | SOTAGLIFLOZIN | 4.0 | 1 | 7.46 |
| CHEMBL4070727 | — | — | 1 | 6.63 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | 4.0 | 1 | 6.58 |
| CHEMBL1770248 | ERTUGLIFLOZIN | 4.0 | 1 | 6.41 |
| CHEMBL4076289 | — | — | 1 | 6.34 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 6.20 |
| CHEMBL4070322 | — | — | 1 | 5.97 |
| CHEMBL4082283 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3039507 | SOTAGLIFLOZIN | IC50 | = | 34.6 | nM | 7.46 |
| CHEMBL4070727 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL1770248 | ERTUGLIFLOZIN | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL4076289 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 629.0 | nM | 6.20 |
| CHEMBL4070322 | — | IC50 | = | 1082.0 | nM | 5.97 |
| CHEMBL4082283 | — | IC50 | = | 1096.0 | nM | 5.96 |