Assay Detail
Binding
CHEMBL2034136
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-lipoxygenase in cell free S100 freshly isolated human PMNL cells assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PMNL |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of a class of 5-benzylidene-2-phenyl-thiazolinones as potent 5-lipoxygenase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.49 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL314360 | — | — | 1 | 7.30 |
| CHEMBL2029857 | — | — | 1 | 7.22 |
| CHEMBL2029849 | — | — | 1 | 7.16 |
| CHEMBL2029848 | — | — | 1 | 7.10 |
| CHEMBL2029847 | — | — | 1 | 7.10 |
| CHEMBL2029845 | — | — | 1 | 7.10 |
| CHEMBL2029844 | — | — | 1 | 7.10 |
| CHEMBL2029843 | — | — | 1 | 7.10 |
| CHEMBL2029832 | — | — | 1 | 7.05 |
| CHEMBL2029855 | — | — | 1 | 7.05 |
| CHEMBL2029846 | — | — | 1 | 7.05 |
| CHEMBL2029834 | — | — | 1 | 7.05 |
| CHEMBL2029836 | — | — | 1 | 7.00 |
| CHEMBL2029850 | — | — | 1 | 6.89 |
| CHEMBL2029854 | — | — | 1 | 6.89 |
| CHEMBL2029840 | — | — | 1 | 6.85 |
| CHEMBL2029856 | — | — | 1 | 6.85 |
| CHEMBL2029838 | — | — | 1 | 6.82 |
| CHEMBL2029858 | — | — | 1 | 6.77 |
| CHEMBL2029837 | — | — | 1 | 6.75 |
| CHEMBL2029831 | — | — | 1 | 6.68 |
| CHEMBL2029833 | — | — | 1 | 6.68 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.30 |
| CHEMBL2029835 | — | — | 1 | 6.26 |
| CHEMBL2029853 | — | — | 1 | 6.24 |
| CHEMBL1765905 | — | — | 1 | 6.20 |
| CHEMBL2029841 | — | — | 1 | 6.12 |
| CHEMBL2029859 | — | — | 1 | 6.10 |
| CHEMBL2029860 | — | — | 1 | 5.68 |
| CHEMBL2029851 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL314360 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2029857 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2029849 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2029848 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2029847 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2029845 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2029844 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2029843 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2029846 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2029834 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2029855 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2029832 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2029836 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2029850 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2029854 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2029840 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2029856 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2029838 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2029858 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2029837 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2029831 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2029833 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL93 | ZILEUTON | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2029835 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2029853 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL1765905 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2029841 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2029859 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL2029860 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL2029851 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL1765904 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2029353 | — | IC50 | = | 4310.0 | nM | 5.37 |
| CHEMBL2029839 | — | IC50 | = | 4660.0 | nM | 5.33 |
| CHEMBL2029852 | — | IC50 | = | 5840.0 | nM | 5.23 |
| CHEMBL2029861 | — | IC50 | = | 6260.0 | nM | 5.20 |
| CHEMBL2029842 | — | IC50 | = | 11050.0 | nM | 4.96 |