Assay Detail
Binding
CHEMBL619403
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-lipoxygenase mediated conversion of [14C]arachidonic acid to leukotrienes in RBL-2H3 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | RBL-2H3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.96 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113724 | — | — | 1 | 7.77 |
| CHEMBL2113723 | — | — | 1 | 7.72 |
| CHEMBL2113721 | — | — | 1 | 7.48 |
| CHEMBL2113722 | — | — | 1 | 7.37 |
| CHEMBL2113730 | — | — | 1 | 7.15 |
| CHEMBL2113720 | — | — | 1 | 7.00 |
| CHEMBL2113725 | — | — | 1 | 6.93 |
| CHEMBL2113733 | — | — | 1 | 6.79 |
| CHEMBL59598 | — | — | 1 | 6.53 |
| CHEMBL59051 | — | — | 1 | 6.37 |
| CHEMBL2113732 | — | — | 1 | 6.28 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113724 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2113723 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2113721 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2113722 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2113730 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2113720 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2113725 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL2113733 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL59598 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL59051 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL2113732 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL93 | ZILEUTON | IC50 | = | 804.0 | nM | 6.09 |