Assay Detail
ADMET
CHEMBL4004099
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Inhibition of human SGLT1 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 | ADMET |
| 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 | 4.88 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | — | 1 | 6.30 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 5.75 |
| CHEMBL503375 | — | — | 1 | 5.10 |
| CHEMBL4092575 | — | — | 1 | 5.02 |
| CHEMBL4082151 | — | — | 1 | 5.01 |
| CHEMBL1645378 | — | — | 1 | 5.00 |
| CHEMBL4084816 | — | — | 1 | 5.00 |
| CHEMBL2234026 | — | — | 1 | 4.98 |
| CHEMBL4063790 | — | — | 1 | 4.97 |
| CHEMBL4068024 | — | — | 1 | 4.94 |
| CHEMBL45068 | PHLORETIN | — | 1 | 4.91 |
| CHEMBL4101262 | — | — | 1 | 4.88 |
| CHEMBL4091589 | — | — | 1 | 4.86 |
| CHEMBL4072377 | — | — | 1 | 4.84 |
| CHEMBL4074544 | — | — | 1 | 4.82 |
| CHEMBL4099324 | — | — | 1 | 4.81 |
| CHEMBL4082869 | — | — | 1 | 4.72 |
| CHEMBL129371 | 2',4',6-TRIHYDROXYCHALCONE | — | 1 | 4.59 |
| CHEMBL334384 | 4-FLUORO-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 4.59 |
| CHEMBL4100313 | — | — | 1 | 4.51 |
| CHEMBL4082294 | — | — | 1 | 4.47 |
| CHEMBL131703 | 4-BROMO-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 4.46 |
| CHEMBL133588 | 4-METHOXYL-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 4.29 |
| CHEMBL4071789 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245067 | PHLORIZIN | IC50 | = | 499.0 | nM | 6.30 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL503375 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4092575 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL4082151 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL1645378 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4084816 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL2234026 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL4063790 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4068024 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL45068 | PHLORETIN | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL4101262 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL4091589 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL4072377 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL4074544 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL4099324 | — | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL4082869 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL129371 | 2',4',6-TRIHYDROXYCHALCONE | IC50 | = | 25400.0 | nM | 4.59 |
| CHEMBL334384 | 4-FLUORO-2',4',6'-TRIHYDROXYCHALCONE | IC50 | = | 25600.0 | nM | 4.59 |
| CHEMBL4100313 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4082294 | — | IC50 | = | 33900.0 | nM | 4.47 |
| CHEMBL131703 | 4-BROMO-2',4',6'-TRIHYDROXYCHALCONE | IC50 | = | 34600.0 | nM | 4.46 |
| CHEMBL133588 | 4-METHOXYL-2',4',6'-TRIHYDROXYCHALCONE | IC50 | = | 50900.0 | nM | 4.29 |
| CHEMBL4071789 | — | IC50 | = | 52600.0 | nM | 4.28 |