Assay Detail
Binding
CHEMBL2051077
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Inhibition of human SGLT1 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 | 5.16 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | — | 1 | 6.72 |
| CHEMBL2048488 | — | — | 1 | 6.29 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 6.10 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | 4.0 | 1 | 5.72 |
| CHEMBL270766 | SERGLIFLOZIN A | — | 1 | 5.64 |
| CHEMBL2048496 | — | — | 1 | 5.35 |
| CHEMBL2048497 | — | — | 1 | 5.07 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | 2.0 | 1 | 4.66 |
| CHEMBL2048494 | — | — | 1 | 4.60 |
| CHEMBL2048487 | — | — | 1 | 4.57 |
| CHEMBL2048489 | — | — | 1 | 4.51 |
| CHEMBL2048486 | — | — | 1 | 4.48 |
| CHEMBL2048485 | — | — | 1 | 4.32 |
| CHEMBL2048490 | — | — | 1 | 4.14 |
| CHEMBL2048491 | — | — | 1 | - |
| CHEMBL2048492 | — | — | 1 | - |
| CHEMBL2048493 | — | — | 1 | - |
| CHEMBL2048495 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2048488 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL270766 | SERGLIFLOZIN A | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2048496 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2048497 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2048494 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2048487 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2048489 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2048486 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2048485 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL2048490 | — | IC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL2048491 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2048492 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2048493 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2048495 | — | IC50 | > | 100000.0 | nM | - |