Assay Detail
Binding
CHEMBL1217373
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SGLT2
18
Total Activities
18
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
Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.38 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 9.31 |
| CHEMBL1213935 | — | — | 1 | 6.92 |
| CHEMBL1213936 | — | — | 1 | 6.60 |
| CHEMBL1213861 | — | — | 1 | 6.59 |
| CHEMBL1213937 | — | — | 1 | 6.39 |
| CHEMBL1213736 | — | — | 1 | 6.21 |
| CHEMBL1213858 | — | — | 1 | 6.11 |
| CHEMBL1213857 | — | — | 1 | 5.98 |
| CHEMBL1213859 | — | — | 1 | 5.63 |
| CHEMBL1213738 | — | — | 1 | 5.33 |
| CHEMBL1213860 | — | — | 1 | 5.06 |
| CHEMBL1213800 | — | — | 1 | - |
| CHEMBL1213801 | — | — | 1 | - |
| CHEMBL1213802 | — | — | 1 | - |
| CHEMBL1213803 | — | — | 1 | - |
| CHEMBL1213799 | — | — | 1 | - |
| CHEMBL1213739 | — | — | 1 | - |
| CHEMBL1213737 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL1213935 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL1213936 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL1213861 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL1213937 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL1213736 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1213858 | — | IC50 | = | 786.0 | nM | 6.11 |
| CHEMBL1213857 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL1213859 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL1213738 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL1213860 | — | IC50 | = | 8640.0 | nM | 5.06 |
| CHEMBL1213800 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1213801 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1213802 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1213803 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1213799 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1213739 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1213737 | — | IC50 | > | 10000.0 | nM | - |