Assay Detail
Binding
CHEMBL1769272
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-lipoxygenase in human polymorphonuclear leukocytes assessed as inhibition of LTB4 production preincubated for 15 mins measured after 10 mins by HPLC method
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A class of 5-benzylidene-2-phenylthiazolinones with high potency as direct 5-lipoxygenase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.93 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL314360 | — | — | 1 | 7.10 |
| CHEMBL1765908 | — | — | 1 | 6.62 |
| CHEMBL1765899 | — | — | 1 | 6.55 |
| CHEMBL1765904 | — | — | 1 | 6.50 |
| CHEMBL1765889 | — | — | 1 | 6.46 |
| CHEMBL1765907 | — | — | 1 | 6.42 |
| CHEMBL1765909 | — | — | 1 | 6.40 |
| CHEMBL1765896 | — | — | 1 | 6.40 |
| CHEMBL1765886 | — | — | 1 | 6.32 |
| CHEMBL1765900 | — | — | 1 | 6.28 |
| CHEMBL1765906 | — | — | 1 | 6.26 |
| CHEMBL1765884 | — | — | 1 | 6.24 |
| CHEMBL1765885 | — | — | 1 | 6.19 |
| CHEMBL1765888 | — | — | 1 | 6.18 |
| CHEMBL1765895 | — | — | 1 | 6.14 |
| CHEMBL1765892 | — | — | 1 | 6.10 |
| CHEMBL1765902 | — | — | 1 | 6.07 |
| CHEMBL1765897 | — | — | 1 | 6.04 |
| CHEMBL1765903 | — | — | 1 | 5.77 |
| CHEMBL1765905 | — | — | 1 | 5.71 |
| CHEMBL1765891 | — | — | 1 | 5.70 |
| CHEMBL1765883 | — | — | 1 | 5.70 |
| CHEMBL1765901 | — | — | 1 | 5.68 |
| CHEMBL1765890 | — | — | 1 | 5.61 |
| CHEMBL1765894 | — | — | 1 | 5.54 |
| CHEMBL1765898 | — | — | 1 | 5.37 |
| CHEMBL1765887 | — | — | 1 | 5.36 |
| CHEMBL1339294 | — | — | 1 | 5.02 |
| CHEMBL1765913 | — | — | 1 | 4.92 |
| CHEMBL1342644 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL314360 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1765908 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1765899 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1765904 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1765889 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1765907 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL1765909 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1765896 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1765886 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1765900 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL1765906 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1765884 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1765885 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1765888 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL1765895 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1765892 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1765902 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL1765897 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1765903 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL1765905 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL1765891 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL1765883 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1765901 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL1765890 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL1765894 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1765898 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1765887 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1339294 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL1765913 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1342644 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL1907659 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1765893 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1765911 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1765912 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1363033 | — | IC50 | > | 30000.0 | nM | - |