Assay Detail
ADMET
CHEMBL2051080
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Inhibition of CYP3A4 using BFC substrate in which compound added to reaction mixture before addition of 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 | 4.44 | 4.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2048487 | — | — | 1 | 4.48 |
| CHEMBL2048496 | — | — | 1 | 4.39 |
| 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 | - |
| CHEMBL2048492 | — | — | 1 | - |
| CHEMBL2048493 | — | — | 1 | - |
| CHEMBL2048494 | — | — | 1 | - |
| CHEMBL2048495 | — | — | 1 | - |
| CHEMBL2048497 | — | — | 1 | - |
| CHEMBL2048489 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2048487 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2048496 | — | IC50 | = | 40300.0 | nM | 4.39 |
| 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 | - | — | - | |
| CHEMBL2048492 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2048493 | — | IC50 | - | — | - | |
| CHEMBL2048494 | — | IC50 | - | — | - | |
| CHEMBL2048495 | — | IC50 | - | — | - | |
| CHEMBL2048497 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2048489 | — | IC50 | - | — | - |