Assay Detail
Binding
CHEMBL2051076
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
18
Total Activities
18
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
C-Aryl 5a-carba-β-d-glucopyranosides as novel sodium glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.71 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.89 |
| CHEMBL270766 | SERGLIFLOZIN A | — | 1 | 8.32 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | 4.0 | 1 | 8.17 |
| CHEMBL2048488 | — | — | 1 | 8.08 |
| CHEMBL2048496 | — | — | 1 | 8.07 |
| CHEMBL2048497 | — | — | 1 | 8.00 |
| CHEMBL2048493 | — | — | 1 | 8.00 |
| CHEMBL2048487 | — | — | 1 | 7.96 |
| CHEMBL2048490 | — | — | 1 | 7.92 |
| CHEMBL2048491 | — | — | 1 | 7.85 |
| CHEMBL245067 | PHLORIZIN | — | 1 | 7.80 |
| CHEMBL2048492 | — | — | 1 | 7.72 |
| CHEMBL2048486 | — | — | 1 | 7.31 |
| CHEMBL2048494 | — | — | 1 | 7.28 |
| CHEMBL2048485 | — | — | 1 | 7.14 |
| CHEMBL2048489 | — | — | 1 | 7.00 |
| CHEMBL2048495 | — | — | 1 | 6.77 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | 2.0 | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL270766 | SERGLIFLOZIN A | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL2048488 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL2048496 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL2048497 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2048493 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL2048487 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2048490 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2048491 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL245067 | PHLORIZIN | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2048492 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2048486 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2048494 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2048485 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2048489 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2048495 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | IC50 | = | 260.0 | nM | 6.58 |