Assay Detail
Binding
CHEMBL1831435
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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
34
Total Activities
34
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 thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.41 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 9.31 |
| CHEMBL1830353 | — | — | 1 | 8.35 |
| CHEMBL1830357 | — | — | 1 | 8.06 |
| CHEMBL1830354 | — | — | 1 | 7.99 |
| CHEMBL1830356 | — | — | 1 | 7.94 |
| CHEMBL1830349 | — | — | 1 | 7.92 |
| CHEMBL1829088 | — | — | 1 | 7.91 |
| CHEMBL1830347 | — | — | 1 | 7.89 |
| CHEMBL1829080 | — | — | 1 | 7.68 |
| CHEMBL1829086 | — | — | 1 | 7.61 |
| CHEMBL1829079 | — | — | 1 | 7.56 |
| CHEMBL1829090 | — | — | 1 | 7.53 |
| CHEMBL1830870 | — | — | 1 | 7.46 |
| CHEMBL1830348 | — | — | 1 | 7.32 |
| CHEMBL1829078 | — | — | 1 | 7.30 |
| CHEMBL1829089 | — | — | 1 | 7.30 |
| CHEMBL1830873 | — | — | 1 | 7.26 |
| CHEMBL1830350 | — | — | 1 | 7.24 |
| CHEMBL1830352 | — | — | 1 | 7.22 |
| CHEMBL1829087 | — | — | 1 | 7.22 |
| CHEMBL1830872 | — | — | 1 | 7.19 |
| CHEMBL1829082 | — | — | 1 | 7.16 |
| CHEMBL1829085 | — | — | 1 | 7.16 |
| CHEMBL1829081 | — | — | 1 | 7.15 |
| CHEMBL1830346 | — | — | 1 | 7.15 |
| CHEMBL1830869 | — | — | 1 | 7.06 |
| CHEMBL1829084 | — | — | 1 | 7.05 |
| CHEMBL1830355 | — | — | 1 | 7.04 |
| CHEMBL1830344 | — | — | 1 | 7.03 |
| CHEMBL1830874 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL1830353 | — | IC50 | = | 4.47 | nM | 8.35 |
| CHEMBL1830357 | — | IC50 | = | 8.73 | nM | 8.06 |
| CHEMBL1830354 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL1830356 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL1830349 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL1829088 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL1830347 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL1829080 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL1829086 | — | IC50 | = | 24.8 | nM | 7.61 |
| CHEMBL1829079 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL1829090 | — | IC50 | = | 29.3 | nM | 7.53 |
| CHEMBL1830870 | — | IC50 | = | 34.6 | nM | 7.46 |
| CHEMBL1830348 | — | IC50 | = | 48.4 | nM | 7.32 |
| CHEMBL1829089 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL1829078 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL1830873 | — | IC50 | = | 54.6 | nM | 7.26 |
| CHEMBL1830350 | — | IC50 | = | 57.2 | nM | 7.24 |
| CHEMBL1830352 | — | IC50 | = | 60.2 | nM | 7.22 |
| CHEMBL1829087 | — | IC50 | = | 59.8 | nM | 7.22 |
| CHEMBL1830872 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1829082 | — | IC50 | = | 68.9 | nM | 7.16 |
| CHEMBL1829085 | — | IC50 | = | 69.6 | nM | 7.16 |
| CHEMBL1829081 | — | IC50 | = | 71.4 | nM | 7.15 |
| CHEMBL1830346 | — | IC50 | = | 70.7 | nM | 7.15 |
| CHEMBL1830869 | — | IC50 | = | 86.5 | nM | 7.06 |
| CHEMBL1829084 | — | IC50 | = | 88.3 | nM | 7.05 |
| CHEMBL1830355 | — | IC50 | = | 91.3 | nM | 7.04 |
| CHEMBL1830344 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1830874 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL1830345 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL1830871 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1830351 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL1829083 | — | IC50 | = | 451.0 | nM | 6.35 |