Assay Detail
Binding
CHEMBL1101142
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Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs
23
Total Activities
23
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
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.50 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL589305 | — | — | 1 | 9.00 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.85 |
| CHEMBL1086408 | — | — | 1 | 8.82 |
| CHEMBL1085691 | — | — | 1 | 8.62 |
| CHEMBL1098376 | — | — | 1 | 8.52 |
| CHEMBL1091811 | — | — | 1 | 8.47 |
| CHEMBL1094712 | — | — | 1 | 8.29 |
| CHEMBL1090058 | — | — | 1 | 8.18 |
| CHEMBL1098377 | — | — | 1 | 8.10 |
| CHEMBL1091810 | — | — | 1 | 7.85 |
| CHEMBL1077231 | — | — | 1 | 7.68 |
| CHEMBL1090414 | — | — | 1 | 7.64 |
| CHEMBL1091476 | — | — | 1 | 7.50 |
| CHEMBL1094714 | — | — | 1 | 7.28 |
| CHEMBL1094713 | — | — | 1 | 7.23 |
| CHEMBL1085454 | — | — | 1 | 6.86 |
| CHEMBL1083834 | — | — | 1 | 6.85 |
| CHEMBL1085455 | — | — | 1 | 6.75 |
| CHEMBL1085188 | — | — | 1 | 6.00 |
| CHEMBL1083835 | — | — | 1 | 5.70 |
| CHEMBL1082892 | — | — | 1 | 5.43 |
| CHEMBL1091809 | — | — | 1 | 5.29 |
| CHEMBL1085189 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL589305 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1086408 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1085691 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1098376 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1091811 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1094712 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1090058 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL1098377 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL1091810 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1077231 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1090414 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1091476 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1094714 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1094713 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1085454 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL1083834 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1085455 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1085188 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1083835 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1082892 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1091809 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1085189 | — | IC50 | > | 10000.0 | nM | - |