Assay Detail
Binding
CHEMBL1040741
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Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake
27
Total Activities
23
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 | Intermediate |
Publication
Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.70 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569434 | — | — | 4 | 7.85 |
| CHEMBL568164 | — | — | 1 | 7.50 |
| CHEMBL585876 | — | — | 2 | 7.48 |
| CHEMBL569903 | — | — | 1 | 7.44 |
| CHEMBL567743 | — | — | 1 | 7.44 |
| CHEMBL567953 | — | — | 1 | 7.35 |
| CHEMBL585703 | — | — | 1 | 7.26 |
| CHEMBL566471 | — | — | 1 | 7.24 |
| CHEMBL567572 | — | — | 1 | 7.00 |
| CHEMBL566076 | — | — | 1 | 6.82 |
| CHEMBL566484 | — | — | 1 | 6.77 |
| CHEMBL577519 | — | — | 1 | 6.75 |
| CHEMBL567372 | — | — | 1 | 6.55 |
| CHEMBL583016 | — | — | 1 | 6.23 |
| CHEMBL566940 | — | — | 1 | 6.22 |
| CHEMBL567778 | — | — | 1 | 6.21 |
| CHEMBL568609 | — | — | 1 | 6.13 |
| CHEMBL568398 | — | — | 1 | 5.96 |
| CHEMBL567373 | — | — | 1 | 5.62 |
| CHEMBL567954 | — | — | 1 | 5.44 |
| CHEMBL567777 | — | — | 1 | 5.34 |
| CHEMBL576252 | — | — | 1 | - |
| CHEMBL582979 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569434 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL569434 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL569434 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL568164 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL585876 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL567743 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL569903 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL567953 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL585703 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL566471 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL567572 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL566076 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL566484 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL577519 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL567372 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL585876 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL583016 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL566940 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL567778 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL568609 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL568398 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL567373 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL567954 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL567777 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL569434 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL576252 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL582979 | — | IC50 | > | 30000.0 | nM | - |