Assay Detail
ADMET
CHEMBL3767771
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Inhibition of CYP2D6 in human liver microsomes assessed as dextraomethorphan O-demethylation
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.73 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1684585 | — | — | 1 | 5.66 |
| CHEMBL111201 | — | — | 1 | 4.96 |
| CHEMBL3764774 | — | — | 1 | 4.51 |
| CHEMBL3763594 | — | — | 1 | 4.41 |
| CHEMBL3128178 | — | — | 1 | 4.10 |
| CHEMBL3128188 | — | — | 1 | - |
| CHEMBL3764088 | — | — | 1 | - |
| CHEMBL2107826 | VIBEGRON | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1684585 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL111201 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3764774 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL3763594 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3128178 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL3128188 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3764088 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2107826 | VIBEGRON | IC50 | > | 100000.0 | nM | - |