Assay Detail
Binding
CHEMBL1646352
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Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting
24
Total Activities
24
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
Exploration of SAR regarding glucose moiety in novel C-aryl glucoside inhibitors of SGLT2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.46 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 9.31 |
| CHEMBL1642509 | — | — | 1 | 8.76 |
| CHEMBL1642508 | — | — | 1 | 8.15 |
| CHEMBL1642516 | — | — | 1 | 8.02 |
| CHEMBL1642515 | — | — | 1 | 7.97 |
| CHEMBL1642510 | — | — | 1 | 7.87 |
| CHEMBL1642520 | — | — | 1 | 7.73 |
| CHEMBL1642514 | — | — | 1 | 7.68 |
| CHEMBL1642517 | — | — | 1 | 7.63 |
| CHEMBL1642511 | — | — | 1 | 7.62 |
| CHEMBL1642519 | — | — | 1 | 7.51 |
| CHEMBL1642521 | — | — | 1 | 7.50 |
| CHEMBL1642524 | — | — | 1 | 7.31 |
| CHEMBL1642513 | — | — | 1 | 7.26 |
| CHEMBL1642512 | — | — | 1 | 7.26 |
| CHEMBL1642525 | — | — | 1 | 7.23 |
| CHEMBL1642518 | — | — | 1 | 7.16 |
| CHEMBL1642729 | — | — | 1 | 7.16 |
| CHEMBL1642523 | — | — | 1 | 7.05 |
| CHEMBL1642730 | — | — | 1 | 6.97 |
| CHEMBL1642526 | — | — | 1 | 6.96 |
| CHEMBL1642527 | — | — | 1 | 6.81 |
| CHEMBL1642728 | — | — | 1 | 6.33 |
| CHEMBL1642522 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL1642509 | — | IC50 | = | 1.75 | nM | 8.76 |
| CHEMBL1642508 | — | IC50 | = | 7.01 | nM | 8.15 |
| CHEMBL1642516 | — | IC50 | = | 9.55 | nM | 8.02 |
| CHEMBL1642515 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL1642510 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL1642520 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL1642514 | — | IC50 | = | 20.8 | nM | 7.68 |
| CHEMBL1642517 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL1642511 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL1642519 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL1642521 | — | IC50 | = | 31.9 | nM | 7.50 |
| CHEMBL1642524 | — | IC50 | = | 48.9 | nM | 7.31 |
| CHEMBL1642513 | — | IC50 | = | 54.8 | nM | 7.26 |
| CHEMBL1642512 | — | IC50 | = | 54.9 | nM | 7.26 |
| CHEMBL1642525 | — | IC50 | = | 59.1 | nM | 7.23 |
| CHEMBL1642518 | — | IC50 | = | 68.7 | nM | 7.16 |
| CHEMBL1642729 | — | IC50 | = | 68.9 | nM | 7.16 |
| CHEMBL1642523 | — | IC50 | = | 89.5 | nM | 7.05 |
| CHEMBL1642730 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL1642526 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1642527 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL1642728 | — | IC50 | = | 471.0 | nM | 6.33 |
| CHEMBL1642522 | — | IC50 | = | 1450.0 | nM | 5.84 |