Assay Detail
Binding
CHEMBL1821169
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Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins
17
Total Activities
17
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
5a-Carba-β-D-glucopyranose derivatives as novel sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.14 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270766 | SERGLIFLOZIN A | — | 1 | 8.32 |
| CHEMBL1819489 | — | — | 1 | 7.96 |
| CHEMBL245067 | PHLORIZIN | — | 1 | 7.80 |
| CHEMBL1819492 | — | — | 1 | 7.72 |
| CHEMBL1819486 | — | — | 1 | 7.55 |
| CHEMBL1819490 | — | — | 1 | 7.54 |
| CHEMBL1819491 | — | — | 1 | 7.38 |
| CHEMBL1819485 | — | — | 1 | 7.23 |
| CHEMBL1817688 | — | — | 1 | 6.96 |
| CHEMBL1819496 | — | — | 1 | 6.92 |
| CHEMBL1819487 | — | — | 1 | 6.92 |
| CHEMBL1819488 | — | — | 1 | 6.82 |
| CHEMBL1819495 | — | — | 1 | 6.82 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | 2.0 | 1 | 6.58 |
| CHEMBL1819493 | — | — | 1 | 6.54 |
| CHEMBL1819494 | — | — | 1 | 6.20 |
| CHEMBL1819484 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270766 | SERGLIFLOZIN A | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1819489 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL245067 | PHLORIZIN | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1819492 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1819486 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1819490 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1819491 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1819485 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1817688 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1819496 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1819487 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1819488 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1819495 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1819493 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1819494 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1819484 | — | IC50 | = | 690.0 | nM | 6.16 |