Assay Detail
ADMET
CHEMBL1002235
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Inhibition of human recombinant CYP2C9 expressed in insect microsomes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.61 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1109 | SULFAPHENAZOLE | 4.0 | 1 | 6.50 |
| CHEMBL500394 | — | — | 1 | 5.90 |
| CHEMBL447591 | — | — | 1 | 5.72 |
| CHEMBL453169 | — | — | 1 | 4.31 |
| CHEMBL502824 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1109 | SULFAPHENAZOLE | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL500394 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL447591 | — | IC50 | = | 1888.0 | nM | 5.72 |
| CHEMBL453169 | — | IC50 | = | 48970.0 | nM | 4.31 |
| CHEMBL502824 | — | IC50 | > | 200000.0 | nM | - |