Assay Detail
ADMET
CHEMBL2051079
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP3A4 using BFC substrate in which compound added to reaction mixture simultaneously with BFC substrate by fluorometric assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
C-Aryl 5a-carba-β-d-glucopyranosides as novel sodium glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 4.42 | 4.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2048496 | — | — | 1 | 4.59 |
| CHEMBL2048497 | — | — | 1 | 4.54 |
| CHEMBL2048492 | — | — | 1 | 4.44 |
| CHEMBL2048487 | — | — | 1 | 4.12 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | 2.0 | 1 | - |
| CHEMBL270766 | SERGLIFLOZIN A | — | 1 | - |
| CHEMBL429910 | DAPAGLIFLOZIN | 4.0 | 1 | - |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | 4.0 | 1 | - |
| CHEMBL2048485 | — | — | 1 | - |
| CHEMBL2048486 | — | — | 1 | - |
| CHEMBL2048488 | — | — | 1 | - |
| CHEMBL245067 | PHLORIZIN | — | 1 | - |
| CHEMBL2048490 | — | — | 1 | - |
| CHEMBL2048491 | — | — | 1 | - |
| CHEMBL2048493 | — | — | 1 | - |
| CHEMBL2048494 | — | — | 1 | - |
| CHEMBL2048495 | — | — | 1 | - |
| CHEMBL2048489 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2048496 | — | IC50 | = | 25700.0 | nM | 4.59 |
| CHEMBL2048497 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL2048492 | — | IC50 | = | 36600.0 | nM | 4.44 |
| CHEMBL2048487 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL450044 | SERGLIFLOZIN ETABONATE | IC50 | - | — | - | |
| CHEMBL270766 | SERGLIFLOZIN A | IC50 | - | — | - | |
| CHEMBL429910 | DAPAGLIFLOZIN | IC50 | - | — | - | |
| CHEMBL2048484 | CANAGLIFLOZIN ANHYDROUS | IC50 | - | — | - | |
| CHEMBL2048485 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2048486 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2048488 | — | IC50 | - | — | - | |
| CHEMBL245067 | PHLORIZIN | IC50 | - | — | - | |
| CHEMBL2048490 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2048491 | — | IC50 | - | — | - | |
| CHEMBL2048493 | — | IC50 | - | — | - | |
| CHEMBL2048494 | — | IC50 | - | — | - | |
| CHEMBL2048495 | — | IC50 | - | — | - | |
| CHEMBL2048489 | — | IC50 | - | — | - |