Assay Detail
Binding
CHEMBL4004100
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Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
24
Total Activities
24
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
Targeting Type 2 Diabetes with C-Glucosyl Dihydrochalcones as Selective Sodium Glucose Co-Transporter 2 (SGLT2) Inhibitors: Synthesis and Biological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.85 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 9.10 |
| CHEMBL4082151 | — | — | 1 | 8.04 |
| CHEMBL4082869 | — | — | 1 | 7.92 |
| CHEMBL4063790 | — | — | 1 | 7.74 |
| CHEMBL1645378 | — | — | 1 | 7.70 |
| CHEMBL4091589 | — | — | 1 | 7.67 |
| CHEMBL4072377 | — | — | 1 | 7.66 |
| CHEMBL4099324 | — | — | 1 | 7.64 |
| CHEMBL245067 | PHLORIZIN | — | 1 | 7.17 |
| CHEMBL503375 | — | — | 1 | 4.83 |
| CHEMBL4092575 | — | — | 1 | 4.80 |
| CHEMBL4068024 | — | — | 1 | 4.79 |
| CHEMBL4074544 | — | — | 1 | 4.78 |
| CHEMBL4084816 | — | — | 1 | 4.75 |
| CHEMBL133588 | 4-METHOXYL-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 4.74 |
| CHEMBL45068 | PHLORETIN | — | 1 | 4.74 |
| CHEMBL4101262 | — | — | 1 | 4.73 |
| CHEMBL4071789 | — | — | 1 | 4.64 |
| CHEMBL131703 | 4-BROMO-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 4.63 |
| CHEMBL4100313 | — | — | 1 | 4.58 |
| CHEMBL4082294 | — | — | 1 | 4.58 |
| CHEMBL129371 | 2',4',6-TRIHYDROXYCHALCONE | — | 1 | 4.48 |
| CHEMBL2234026 | — | — | 1 | 4.47 |
| CHEMBL334384 | 4-FLUORO-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 4.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4082151 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4082869 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL4063790 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL1645378 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4091589 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL4072377 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL4099324 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL245067 | PHLORIZIN | IC50 | = | 67.3 | nM | 7.17 |
| CHEMBL503375 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL4092575 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL4068024 | — | IC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL4074544 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL4084816 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL133588 | 4-METHOXYL-2',4',6'-TRIHYDROXYCHALCONE | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL45068 | PHLORETIN | IC50 | = | 18300.0 | nM | 4.74 |
| CHEMBL4101262 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL4071789 | — | IC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL131703 | 4-BROMO-2',4',6'-TRIHYDROXYCHALCONE | IC50 | = | 23500.0 | nM | 4.63 |
| CHEMBL4100313 | — | IC50 | = | 26200.0 | nM | 4.58 |
| CHEMBL4082294 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL129371 | 2',4',6-TRIHYDROXYCHALCONE | IC50 | = | 33300.0 | nM | 4.48 |
| CHEMBL2234026 | — | IC50 | = | 34100.0 | nM | 4.47 |
| CHEMBL334384 | 4-FLUORO-2',4',6'-TRIHYDROXYCHALCONE | IC50 | = | 51700.0 | nM | 4.29 |