Assay Detail
Binding
CHEMBL4268906
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human kidneyl SGLT2 expressed in CHOK1 cells assessed as reduction in Na-dependent [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition measured after 2 hrs by TopCount method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.99 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4281478 | — | — | 1 | 8.70 |
| CHEMBL4294285 | — | — | 1 | 8.59 |
| CHEMBL4291795 | — | — | 1 | 8.52 |
| CHEMBL4286399 | — | — | 1 | 8.28 |
| CHEMBL4293989 | — | — | 1 | 8.12 |
| CHEMBL4289884 | — | — | 1 | 8.08 |
| CHEMBL4279519 | — | — | 1 | 8.05 |
| CHEMBL4279564 | — | — | 1 | 7.87 |
| CHEMBL4285963 | — | — | 1 | 7.63 |
| CHEMBL4285800 | — | — | 1 | 7.44 |
| CHEMBL4287888 | — | — | 1 | 7.44 |
| CHEMBL4282708 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4281478 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4294285 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4291795 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4286399 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4293989 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4289884 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4279519 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4279564 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4285963 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL4285800 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4287888 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4282708 | — | IC50 | = | 62.3 | nM | 7.21 |