Assay Detail
Binding
CHEMBL3292468
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Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis
22
Total Activities
22
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
The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.63 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 9.00 |
| CHEMBL3288755 | — | — | 1 | 7.96 |
| CHEMBL3288756 | — | — | 1 | 7.63 |
| CHEMBL3288752 | — | — | 1 | 7.48 |
| CHEMBL3288738 | — | — | 1 | 7.10 |
| CHEMBL3288737 | — | — | 1 | 7.08 |
| CHEMBL3288744 | — | — | 1 | 7.05 |
| CHEMBL3288739 | — | — | 1 | 6.97 |
| CHEMBL3288745 | — | — | 1 | 6.96 |
| CHEMBL3288740 | — | — | 1 | 6.92 |
| CHEMBL3288741 | — | — | 1 | 6.85 |
| CHEMBL3288742 | — | — | 1 | 6.65 |
| CHEMBL3288754 | — | — | 1 | 6.61 |
| CHEMBL3288746 | — | — | 1 | 6.60 |
| CHEMBL3288753 | — | — | 1 | 6.48 |
| CHEMBL3288757 | — | — | 1 | 6.31 |
| CHEMBL3288743 | — | — | 1 | 6.12 |
| CHEMBL3288751 | — | — | 1 | 5.48 |
| CHEMBL3288747 | — | — | 1 | 5.26 |
| CHEMBL3288748 | — | — | 1 | 5.24 |
| CHEMBL3288750 | — | — | 1 | 5.05 |
| CHEMBL3288749 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3288755 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL3288756 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL3288752 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3288738 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3288737 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3288744 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3288739 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3288745 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3288740 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3288741 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL3288742 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL3288754 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL3288746 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL3288753 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL3288757 | — | IC50 | = | 489.0 | nM | 6.31 |
| CHEMBL3288743 | — | IC50 | = | 762.0 | nM | 6.12 |
| CHEMBL3288751 | — | IC50 | = | 3296.0 | nM | 5.48 |
| CHEMBL3288747 | — | IC50 | = | 5478.0 | nM | 5.26 |
| CHEMBL3288748 | — | IC50 | = | 5699.0 | nM | 5.24 |
| CHEMBL3288750 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3288749 | — | IC50 | = | 9916.0 | nM | 5.00 |