Assay Detail
Binding
CHEMBL1117743
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Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.78 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 9.31 |
| CHEMBL1083975 | — | — | 1 | 7.94 |
| CHEMBL1085771 | — | — | 1 | 7.87 |
| CHEMBL1085547 | — | — | 1 | 7.77 |
| CHEMBL1085769 | — | — | 1 | 7.76 |
| CHEMBL1083690 | — | — | 1 | 7.37 |
| CHEMBL1083978 | — | — | 1 | 7.21 |
| CHEMBL1085272 | — | — | 1 | 7.19 |
| CHEMBL1083674 | — | — | 1 | 7.19 |
| CHEMBL1085297 | — | — | 1 | 7.15 |
| CHEMBL1086441 | — | — | 1 | 7.15 |
| CHEMBL1084166 | — | — | 1 | 7.15 |
| CHEMBL1084440 | — | — | 1 | 7.12 |
| CHEMBL1086192 | — | — | 1 | 7.11 |
| CHEMBL1084258 | — | — | 1 | 7.08 |
| CHEMBL1084259 | — | — | 1 | 6.99 |
| CHEMBL1085545 | — | — | 1 | 6.96 |
| CHEMBL1085770 | — | — | 1 | 6.96 |
| CHEMBL1085544 | — | — | 1 | 6.96 |
| CHEMBL1083079 | — | — | 1 | 6.88 |
| CHEMBL1085529 | — | — | 1 | 6.87 |
| CHEMBL1085015 | — | — | 1 | 6.78 |
| CHEMBL1083673 | — | — | 1 | 6.75 |
| CHEMBL1082759 | — | — | 1 | 6.70 |
| CHEMBL1083979 | — | — | 1 | 6.65 |
| CHEMBL1083369 | — | — | 1 | 6.62 |
| CHEMBL1083370 | — | — | 1 | 6.59 |
| CHEMBL1083980 | — | — | 1 | 6.57 |
| CHEMBL1086006 | — | — | 1 | 6.53 |
| CHEMBL1085271 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL1083975 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL1085771 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL1085547 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1085769 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL1083690 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1083978 | — | IC50 | = | 61.3 | nM | 7.21 |
| CHEMBL1085272 | — | IC50 | = | 64.9 | nM | 7.19 |
| CHEMBL1083674 | — | IC50 | = | 64.3 | nM | 7.19 |
| CHEMBL1084166 | — | IC50 | = | 71.4 | nM | 7.15 |
| CHEMBL1086441 | — | IC50 | = | 71.3 | nM | 7.15 |
| CHEMBL1085297 | — | IC50 | = | 70.8 | nM | 7.15 |
| CHEMBL1084440 | — | IC50 | = | 75.4 | nM | 7.12 |
| CHEMBL1086192 | — | IC50 | = | 77.6 | nM | 7.11 |
| CHEMBL1084258 | — | IC50 | = | 82.7 | nM | 7.08 |
| CHEMBL1084259 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL1085545 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL1085770 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL1085544 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1083079 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL1085529 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL1085015 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL1083673 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL1082759 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL1083979 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL1083369 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL1083370 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL1083980 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL1086006 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL1085271 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL1083671 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL1085546 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL1082416 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1085528 | — | IC50 | = | 811.0 | nM | 6.09 |
| CHEMBL1082502 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL1082417 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL1085844 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL1085273 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL1085772 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL1085845 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1086076 | — | IC50 | = | 10000.0 | nM | 5.00 |