Assay Detail
Binding
CHEMBL1769274
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Inhibition of 5-lipoxygenase in S100 supernatant 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 |
| Confidence | 8 — Homologous 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 | 6.35 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL314360 | — | — | 1 | 7.30 |
| CHEMBL1765899 | — | — | 1 | 7.05 |
| CHEMBL1765909 | — | — | 1 | 6.96 |
| CHEMBL1765906 | — | — | 1 | 6.96 |
| CHEMBL1765908 | — | — | 1 | 6.92 |
| CHEMBL1765907 | — | — | 1 | 6.89 |
| CHEMBL1765889 | — | — | 1 | 6.89 |
| CHEMBL1765900 | — | — | 1 | 6.82 |
| CHEMBL1765901 | — | — | 1 | 6.72 |
| CHEMBL1765896 | — | — | 1 | 6.64 |
| CHEMBL1765884 | — | — | 1 | 6.52 |
| CHEMBL1765885 | — | — | 1 | 6.52 |
| CHEMBL1765898 | — | — | 1 | 6.52 |
| CHEMBL1765897 | — | — | 1 | 6.52 |
| CHEMBL1765888 | — | — | 1 | 6.52 |
| CHEMBL1765895 | — | — | 1 | 6.46 |
| CHEMBL1765890 | — | — | 1 | 6.40 |
| CHEMBL1765883 | — | — | 1 | 6.30 |
| CHEMBL1765886 | — | — | 1 | 6.27 |
| CHEMBL1765902 | — | — | 1 | 6.24 |
| CHEMBL1765905 | — | — | 1 | 6.20 |
| CHEMBL1765903 | — | — | 1 | 6.19 |
| CHEMBL1765891 | — | — | 1 | 6.01 |
| CHEMBL1765894 | — | — | 1 | 5.90 |
| CHEMBL1765892 | — | — | 1 | 5.89 |
| CHEMBL1765893 | — | — | 1 | 5.57 |
| CHEMBL1765887 | — | — | 1 | 5.52 |
| CHEMBL1339294 | — | — | 1 | 5.52 |
| CHEMBL1765904 | — | — | 1 | 5.40 |
| CHEMBL1765913 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL314360 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1765899 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1765909 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1765906 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1765908 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1765907 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1765889 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1765900 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1765901 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1765896 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1765884 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1765885 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1765898 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1765897 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1765888 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1765895 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1765890 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1765883 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1765886 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1765902 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1765905 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL1765903 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1765891 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL1765894 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL1765892 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1765893 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1765887 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1339294 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1765904 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1765913 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1342644 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1907659 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1765911 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1765912 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1363033 | — | IC50 | > | 30000.0 | nM | - |