Assay Detail
ADMET
CHEMBL972422
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Inhibition of CYP2C8 in human liver microsomes using montelukast substrate
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.78 | 5.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483352 | — | — | 1 | 5.24 |
| CHEMBL483353 | — | — | 1 | 5.23 |
| CHEMBL482768 | — | — | 1 | 4.96 |
| CHEMBL482980 | — | — | 1 | 4.70 |
| CHEMBL520136 | — | — | 1 | 4.64 |
| CHEMBL485196 | — | — | 1 | 4.36 |
| CHEMBL485326 | — | — | 1 | 4.33 |
| CHEMBL483160 | — | — | 1 | - |
| CHEMBL520299 | — | — | 1 | - |
| CHEMBL521326 | — | — | 1 | - |
| CHEMBL520620 | — | — | 1 | - |
| CHEMBL485185 | — | — | 1 | - |
| CHEMBL483139 | — | — | 1 | - |
| CHEMBL483140 | — | — | 1 | - |
| CHEMBL483336 | — | — | 1 | - |
| CHEMBL483337 | — | — | 1 | - |
| CHEMBL520513 | — | — | 1 | - |
| CHEMBL485327 | — | — | 1 | - |
| CHEMBL485184 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483352 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL483353 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL482768 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL482980 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL520136 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL485196 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL485326 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL483160 | — | IC50 | - | — | - | |
| CHEMBL520299 | — | IC50 | - | — | - | |
| CHEMBL521326 | — | IC50 | - | — | - | |
| CHEMBL520620 | — | IC50 | - | — | - | |
| CHEMBL485185 | — | IC50 | - | — | - | |
| CHEMBL483139 | — | IC50 | - | — | - | |
| CHEMBL483140 | — | IC50 | - | — | - | |
| CHEMBL483336 | — | IC50 | - | — | - | |
| CHEMBL483337 | — | IC50 | - | — | - | |
| CHEMBL520513 | — | IC50 | - | — | - | |
| CHEMBL485327 | — | IC50 | - | — | - | |
| CHEMBL485184 | — | IC50 | - | — | - |