Assay Detail
Binding
CHEMBL4015644
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method
20
Total Activities
20
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 | 20 | 8.35 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4070727 | — | — | 1 | 9.00 |
| CHEMBL4071777 | — | — | 1 | 8.96 |
| CHEMBL4082283 | — | — | 1 | 8.89 |
| CHEMBL3039507 | SOTAGLIFLOZIN | 4.0 | 1 | 8.82 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.82 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | 4.0 | 1 | 8.66 |
| CHEMBL1770248 | ERTUGLIFLOZIN | 4.0 | 1 | 8.62 |
| CHEMBL4092561 | — | — | 1 | 8.60 |
| CHEMBL4073410 | — | — | 1 | 8.47 |
| CHEMBL4097849 | — | — | 1 | 8.36 |
| CHEMBL4090131 | — | — | 1 | 8.30 |
| CHEMBL4065901 | — | — | 1 | 8.23 |
| CHEMBL4063778 | — | — | 1 | 8.23 |
| CHEMBL4101799 | — | — | 1 | 8.23 |
| CHEMBL4091576 | — | — | 1 | 8.17 |
| CHEMBL4083794 | — | — | 1 | 7.97 |
| CHEMBL4076289 | — | — | 1 | 7.86 |
| CHEMBL4093508 | — | — | 1 | 7.65 |
| CHEMBL4070322 | — | — | 1 | 7.55 |
| CHEMBL4062100 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4070727 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4071777 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4082283 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3039507 | SOTAGLIFLOZIN | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1770248 | ERTUGLIFLOZIN | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4092561 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4073410 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4097849 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4090131 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4065901 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4063778 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4101799 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4091576 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4083794 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL4076289 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4093508 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL4070322 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL4062100 | — | IC50 | = | 31.0 | nM | 7.51 |