Assay Detail
Binding
CHEMBL3887243
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Compounds were tested for their ability to inhibit recombinant soluble epoxide hydrolase (sEH) protein. The assay utilizes (3-Phhenyl-oxiranyl)-acetic acid cyano-(6-methoxy-naphthalen-2-yl)-methyl ester (PHOME), a sensitive substrate for sEH that can be used to monitor the activity of both human and murine enzymes. Hydrolysis of the substrate epoxide yields a highly fluorescent product, 6-methoxy-2-Naphthaldehyde, which can be monitored at excitation and emission wavelengths of 330 and 465 nm, respectively. See Wolf et al., Anal Biochem 355:71-80, 2006 PMID: 16729954. Human recombinant sEH was incubated with substrate and compounds ranging in concentration from 0.1 to 1000 nM.
37
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Epoxyeicosatrienoic acid analogs and methods of making and using the same
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.30 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3322807 | — | — | 1 | 8.22 |
| CHEMBL3322818 | — | — | 1 | 8.00 |
| CHEMBL3322814 | — | — | 2 | 7.96 |
| CHEMBL3322808 | — | — | 1 | 7.96 |
| CHEMBL3322809 | — | — | 1 | 7.66 |
| CHEMBL3322812 | — | — | 1 | 7.64 |
| CHEMBL3322821 | — | — | 1 | 7.51 |
| CHEMBL3322804 | — | — | 1 | 7.50 |
| CHEMBL3322815 | — | — | 1 | 7.50 |
| CHEMBL3322810 | — | — | 1 | 7.50 |
| CHEMBL3322802 | — | — | 1 | 7.39 |
| CHEMBL3558237 | — | — | 1 | 7.24 |
| CHEMBL3322823 | — | — | 1 | 7.24 |
| CHEMBL3322817 | — | — | 1 | 7.19 |
| CHEMBL3322803 | — | — | 1 | 7.15 |
| CHEMBL3322811 | — | — | 1 | 7.02 |
| CHEMBL3322822 | — | — | 1 | 6.64 |
| CHEMBL3322828 | — | — | 1 | 6.62 |
| CHEMBL3322797 | — | — | 1 | 6.59 |
| CHEMBL3322824 | — | — | 1 | 6.55 |
| CHEMBL4109511 | — | — | 1 | 6.41 |
| CHEMBL3558235 | — | — | 1 | 6.41 |
| CHEMBL3322827 | — | — | 1 | - |
| CHEMBL4111533 | — | — | 1 | - |
| CHEMBL3322826 | — | — | 1 | - |
| CHEMBL3322819 | — | — | 1 | - |
| CHEMBL4110025 | — | — | 1 | - |
| CHEMBL4107289 | — | — | 1 | - |
| CHEMBL3927470 | — | — | 1 | - |
| CHEMBL4114588 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3322807 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3322818 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3322814 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3322814 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3322808 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3322809 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3322812 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3322821 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3322810 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3322804 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3322815 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3322802 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3558237 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3322823 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3322817 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3322803 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3322811 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3322822 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL3322828 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL3322797 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL3322824 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL3558235 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL4109511 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL3322798 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4108921 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3322800 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3558236 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4109660 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3322816 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4114588 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3927470 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4107289 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4110025 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3322826 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4111533 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3322827 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3322819 | — | IC50 | > | 500.0 | nM | - |