Assay Detail
Binding
CHEMBL1069022
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Inhibition of human recombinant SGLT2 expressed in CHO cells by liquid scintillation counting
51
Total Activities
51
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: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 7.01 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 9.31 |
| CHEMBL601510 | — | — | 1 | 8.46 |
| CHEMBL591949 | — | — | 1 | 8.39 |
| CHEMBL270766 | SERGLIFLOZIN A | — | 1 | 8.20 |
| CHEMBL605905 | — | — | 1 | 8.15 |
| CHEMBL590992 | — | — | 1 | 7.97 |
| CHEMBL591739 | — | — | 1 | 7.96 |
| CHEMBL606750 | — | — | 1 | 7.84 |
| CHEMBL603167 | — | — | 1 | 7.78 |
| CHEMBL590751 | — | — | 1 | 7.75 |
| CHEMBL590020 | — | — | 1 | 7.74 |
| CHEMBL590271 | — | — | 1 | 7.66 |
| CHEMBL590041 | — | — | 1 | 7.60 |
| CHEMBL590296 | — | — | 1 | 7.52 |
| CHEMBL600982 | — | — | 1 | 7.44 |
| CHEMBL590021 | — | — | 1 | 7.35 |
| CHEMBL590042 | — | — | 1 | 7.34 |
| CHEMBL601465 | — | — | 1 | 7.28 |
| CHEMBL590991 | — | — | 1 | 7.23 |
| CHEMBL590272 | — | — | 1 | 7.14 |
| CHEMBL589300 | — | — | 1 | 7.09 |
| CHEMBL590514 | — | — | 1 | 7.01 |
| CHEMBL606689 | — | — | 1 | 6.99 |
| CHEMBL590752 | — | — | 1 | 6.97 |
| CHEMBL592686 | — | — | 1 | 6.92 |
| CHEMBL589324 | — | — | 1 | 6.91 |
| CHEMBL602524 | — | — | 1 | 6.90 |
| CHEMBL591738 | — | — | 1 | 6.84 |
| CHEMBL602554 | — | — | 1 | 6.81 |
| CHEMBL591950 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL601510 | — | IC50 | = | 3.51 | nM | 8.46 |
| CHEMBL591949 | — | IC50 | = | 4.06 | nM | 8.39 |
| CHEMBL270766 | SERGLIFLOZIN A | IC50 | = | 6.25 | nM | 8.20 |
| CHEMBL605905 | — | IC50 | = | 7.03 | nM | 8.15 |
| CHEMBL590992 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL591739 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL606750 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL603167 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL590751 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL590020 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL590271 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL590041 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL590296 | — | IC50 | = | 30.3 | nM | 7.52 |
| CHEMBL600982 | — | IC50 | = | 36.4 | nM | 7.44 |
| CHEMBL590021 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL590042 | — | IC50 | = | 45.3 | nM | 7.34 |
| CHEMBL601465 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL590991 | — | IC50 | = | 58.3 | nM | 7.23 |
| CHEMBL590272 | — | IC50 | = | 72.6 | nM | 7.14 |
| CHEMBL589300 | — | IC50 | = | 81.6 | nM | 7.09 |
| CHEMBL590514 | — | IC50 | = | 97.4 | nM | 7.01 |
| CHEMBL606689 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL590752 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL592686 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL589324 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL602524 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL591738 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL602554 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL591950 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL608374 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL602721 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL590299 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL601947 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL591714 | — | IC50 | = | 379.0 | nM | 6.42 |
| CHEMBL591490 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL591937 | — | IC50 | = | 542.0 | nM | 6.27 |
| CHEMBL589545 | — | IC50 | = | 562.0 | nM | 6.25 |
| CHEMBL590277 | — | IC50 | = | 638.0 | nM | 6.20 |
| CHEMBL603166 | — | IC50 | = | 712.0 | nM | 6.15 |
| CHEMBL589980 | — | IC50 | = | 758.0 | nM | 6.12 |
| CHEMBL591485 | — | IC50 | = | 762.0 | nM | 6.12 |
| CHEMBL591936 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL589532 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL608672 | — | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL592687 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL591954 | — | IC50 | = | 6910.0 | nM | 5.16 |
| CHEMBL592667 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL592189 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL589079 | — | IC50 | > | 10000.0 | nM | - |