Assay Detail
Binding
CHEMBL869679
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Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells
15
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.80 | 6.40 |
| Ki | 1 | 6.80 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL208528 | — | — | 2 | 6.80 |
| CHEMBL207831 | — | — | 1 | 6.40 |
| CHEMBL207982 | — | — | 1 | 6.22 |
| CHEMBL207832 | — | — | 1 | 6.16 |
| CHEMBL207278 | — | — | 1 | 6.16 |
| CHEMBL205154 | TERFENADONE | — | 1 | 6.16 |
| CHEMBL207389 | — | — | 1 | 5.89 |
| CHEMBL204362 | — | — | 1 | 5.72 |
| CHEMBL206576 | — | — | 1 | 5.66 |
| CHEMBL378460 | — | — | 1 | 5.60 |
| CHEMBL204998 | — | — | 1 | 5.38 |
| CHEMBL382604 | — | — | 1 | 5.17 |
| CHEMBL383199 | — | — | 1 | 5.12 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL208528 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL207831 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL208528 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL207982 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL207832 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL207278 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL205154 | TERFENADONE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL207389 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL204362 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL206576 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL378460 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL204998 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL382604 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL383199 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 8100.0 | nM | 5.09 |