Assay Detail
ADMET
CHEMBL1002233
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Inhibition of human recombinant CYP1A2 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 | 6.13 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL447591 | — | — | 1 | 7.08 |
| CHEMBL502824 | — | — | 1 | 6.31 |
| CHEMBL453169 | — | — | 1 | 5.85 |
| CHEMBL500394 | — | — | 1 | 5.79 |
| CHEMBL405845 | FURAFYLLINE | 2.0 | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL447591 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL502824 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL453169 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL500394 | — | IC50 | = | 1619.0 | nM | 5.79 |
| CHEMBL405845 | FURAFYLLINE | IC50 | = | 2419.0 | nM | 5.62 |