Assay Detail
Binding
CHEMBL1005353
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Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake by fluorescence polarization assay
32
Total Activities
32
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
Design and synthesis of fluorescent SGLT2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.48 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL496138 | — | — | 1 | 7.92 |
| CHEMBL497971 | — | — | 1 | 7.48 |
| CHEMBL521565 | — | — | 1 | 7.35 |
| CHEMBL447975 | — | — | 1 | 7.26 |
| CHEMBL449080 | — | — | 1 | 7.02 |
| CHEMBL500268 | — | — | 1 | 6.99 |
| CHEMBL448655 | — | — | 1 | 6.91 |
| CHEMBL499912 | — | — | 1 | 6.91 |
| CHEMBL452214 | — | — | 1 | 6.88 |
| CHEMBL500780 | — | — | 1 | 6.84 |
| CHEMBL504484 | — | — | 1 | 6.83 |
| CHEMBL445964 | — | — | 1 | 6.81 |
| CHEMBL444227 | — | — | 1 | 6.81 |
| CHEMBL511083 | — | — | 1 | 6.69 |
| CHEMBL508623 | — | — | 1 | 6.69 |
| CHEMBL506354 | — | — | 1 | 6.57 |
| CHEMBL501165 | — | — | 1 | 6.54 |
| CHEMBL509911 | — | — | 1 | 6.50 |
| CHEMBL443616 | — | — | 1 | 6.46 |
| CHEMBL503496 | — | — | 1 | 6.43 |
| CHEMBL442864 | — | — | 1 | 6.38 |
| CHEMBL473046 | — | — | 1 | 6.37 |
| CHEMBL496518 | — | — | 1 | 6.30 |
| CHEMBL245067 | PHLORIZIN | — | 1 | 6.12 |
| CHEMBL449778 | — | — | 1 | 6.08 |
| CHEMBL171648 | — | — | 1 | 6.07 |
| CHEMBL509278 | — | — | 1 | 5.80 |
| CHEMBL508141 | — | — | 1 | 5.70 |
| CHEMBL500899 | — | — | 1 | 5.62 |
| CHEMBL457594 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL496138 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL497971 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL521565 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL447975 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL449080 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL500268 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL448655 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL499912 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL452214 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL500780 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL504484 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL445964 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL444227 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL511083 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL508623 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL506354 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL501165 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL509911 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL443616 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL503496 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL442864 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL473046 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL496518 | — | IC50 | = | 495.0 | nM | 6.30 |
| CHEMBL245067 | PHLORIZIN | IC50 | = | 752.0 | nM | 6.12 |
| CHEMBL449778 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL171648 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL509278 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL508141 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL500899 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL457594 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL445247 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL466749 | — | IC50 | = | 15050.0 | nM | 4.82 |