Assay Detail
Binding
CHEMBL1050643
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Inhibition of human SGLT2 transfected in HEK293.ETN cells assessed as AMG uptake after 1.5 hrs by scintillation counting
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.92 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565781 | — | — | 1 | 9.52 |
| CHEMBL565377 | — | — | 1 | 9.10 |
| CHEMBL566224 | — | — | 1 | 8.89 |
| CHEMBL585477 | — | — | 1 | 8.60 |
| CHEMBL567474 | — | — | 1 | 8.42 |
| CHEMBL585482 | — | — | 1 | 8.24 |
| CHEMBL565784 | — | — | 1 | 8.19 |
| CHEMBL585021 | — | — | 1 | 8.18 |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | 8.17 |
| CHEMBL567276 | — | — | 1 | 8.15 |
| CHEMBL567067 | — | — | 1 | 8.15 |
| CHEMBL584689 | — | — | 1 | 8.07 |
| CHEMBL566622 | — | — | 1 | 8.00 |
| CHEMBL565376 | — | — | 1 | 8.00 |
| CHEMBL585315 | — | — | 1 | 7.89 |
| CHEMBL567058 | — | — | 1 | 7.66 |
| CHEMBL565786 | — | — | 1 | 7.37 |
| CHEMBL566017 | — | — | 1 | 7.17 |
| CHEMBL566018 | — | — | 1 | 7.16 |
| CHEMBL570868 | — | — | 1 | 7.15 |
| CHEMBL565391 | — | — | 1 | 7.00 |
| CHEMBL566413 | — | — | 1 | 7.00 |
| CHEMBL566019 | — | — | 1 | 6.00 |
| CHEMBL584916 | — | — | 1 | - |
| CHEMBL593522 | — | — | 1 | - |
| CHEMBL585092 | — | — | 1 | - |
| CHEMBL585484 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565781 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL565377 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL566224 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL585477 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL567474 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL585482 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL565784 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL585021 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL567276 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL567067 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL584689 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL566622 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL565376 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL585315 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL567058 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL565786 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL566017 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL566018 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL570868 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL565391 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL566413 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL566019 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL584916 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL593522 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL585092 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL585484 | — | IC50 | > | 1000.0 | nM | - |