Assay Detail
Binding
CHEMBL1821170
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Inhibition of human SGLT1 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 | 5.05 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | — | 1 | 6.72 |
| CHEMBL270766 | SERGLIFLOZIN A | — | 1 | 5.64 |
| CHEMBL1819490 | — | — | 1 | 5.48 |
| CHEMBL1819492 | — | — | 1 | 5.46 |
| CHEMBL1819486 | — | — | 1 | 5.32 |
| CHEMBL1819489 | — | — | 1 | 5.25 |
| CHEMBL1819485 | — | — | 1 | 5.17 |
| CHEMBL1819487 | — | — | 1 | 5.11 |
| CHEMBL1819491 | — | — | 1 | 5.03 |
| CHEMBL1819484 | — | — | 1 | 4.89 |
| CHEMBL1819493 | — | — | 1 | 4.72 |
| CHEMBL1819488 | — | — | 1 | 4.70 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | 2.0 | 1 | 4.66 |
| CHEMBL1819495 | — | — | 1 | 4.66 |
| CHEMBL1819494 | — | — | 1 | 4.42 |
| CHEMBL1817688 | — | — | 1 | 4.39 |
| CHEMBL1819496 | — | — | 1 | 4.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL270766 | SERGLIFLOZIN A | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1819490 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1819492 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1819486 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1819489 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1819485 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1819487 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL1819491 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL1819484 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1819493 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1819488 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL1819495 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL1819494 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL1817688 | — | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL1819496 | — | IC50 | = | 57000.0 | nM | 4.24 |