Assay Detail
Binding
CHEMBL3128638
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Inhibition of SGLT2 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of novel l-rhamnose derived acyclic C-nucleosides with substituted 1,2,3-triazole core as potent sodium-glucose co-transporter (SGLT) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.74 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | — | 1 | 7.23 |
| CHEMBL3125147 | — | — | 1 | 6.90 |
| CHEMBL3125151 | — | — | 1 | 6.87 |
| CHEMBL3125155 | — | — | 1 | 6.83 |
| CHEMBL3125154 | — | — | 1 | 6.83 |
| CHEMBL3125143 | — | — | 1 | 6.82 |
| CHEMBL3125142 | — | — | 1 | 6.82 |
| CHEMBL3125152 | — | — | 1 | 6.79 |
| CHEMBL3125146 | — | — | 1 | 6.76 |
| CHEMBL3125141 | — | — | 1 | 6.73 |
| CHEMBL3125144 | — | — | 1 | 6.72 |
| CHEMBL3125153 | — | — | 1 | 6.67 |
| CHEMBL3125149 | — | — | 1 | 6.64 |
| CHEMBL3125156 | — | — | 1 | 6.51 |
| CHEMBL3125145 | — | — | 1 | 6.43 |
| CHEMBL3125148 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | IC50 | = | 58.6 | nM | 7.23 |
| CHEMBL3125147 | — | IC50 | = | 125.9 | nM | 6.90 |
| CHEMBL3125151 | — | IC50 | = | 134.7 | nM | 6.87 |
| CHEMBL3125155 | — | IC50 | = | 146.9 | nM | 6.83 |
| CHEMBL3125154 | — | IC50 | = | 149.1 | nM | 6.83 |
| CHEMBL3125143 | — | IC50 | = | 151.8 | nM | 6.82 |
| CHEMBL3125142 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3125152 | — | IC50 | = | 163.2 | nM | 6.79 |
| CHEMBL3125146 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL3125141 | — | IC50 | = | 185.8 | nM | 6.73 |
| CHEMBL3125144 | — | IC50 | = | 190.3 | nM | 6.72 |
| CHEMBL3125153 | — | IC50 | = | 214.2 | nM | 6.67 |
| CHEMBL3125149 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3125156 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL3125145 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL3125148 | — | IC50 | = | 458.0 | nM | 6.34 |