Assay Detail
Binding
CHEMBL3420867
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-LOX in A23187-stimulated human blood PMNL assessed as reduction in lipoxygenase products formation in presence of arachidonic acid pre-incubated for 15 mins followed by stimulation with A23187 for 10 mins by RP-HPLC based cell based assay
49
Total Activities
49
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
Novel series of benzoquinones with high potency against 5-lipoxygenase in human polymorphonuclear leukocytes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 6.01 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3416360 | — | — | 1 | 7.30 |
| CHEMBL3416357 | — | — | 1 | 7.16 |
| CHEMBL3416361 | — | — | 1 | 7.05 |
| CHEMBL3416365 | — | — | 1 | 7.00 |
| CHEMBL3416358 | — | — | 1 | 7.00 |
| CHEMBL3416359 | — | — | 1 | 6.82 |
| CHEMBL3416348 | — | — | 1 | 6.51 |
| CHEMBL3416364 | — | — | 1 | 6.41 |
| CHEMBL2228912 | — | — | 1 | 6.31 |
| CHEMBL3416347 | — | — | 1 | 6.31 |
| CHEMBL3416180 | — | — | 1 | 6.24 |
| CHEMBL2296071 | — | — | 1 | 6.23 |
| CHEMBL3416356 | — | — | 1 | 6.09 |
| CHEMBL3416350 | — | — | 1 | 6.07 |
| CHEMBL3416174 | — | — | 1 | 6.07 |
| CHEMBL3416355 | — | — | 1 | 6.00 |
| CHEMBL3416175 | — | — | 1 | 5.96 |
| CHEMBL3416173 | — | — | 1 | 5.96 |
| CHEMBL3416353 | — | — | 1 | 5.92 |
| CHEMBL471270 | 5-O-METHYLEMBELIN | — | 1 | 5.89 |
| CHEMBL3416179 | — | — | 1 | 5.85 |
| CHEMBL3416349 | — | — | 1 | 5.85 |
| CHEMBL3416352 | — | — | 1 | 5.80 |
| CHEMBL2228913 | — | — | 1 | 5.77 |
| CHEMBL2269075 | Sorgoleone-364 | — | 1 | 5.64 |
| CHEMBL3416177 | — | — | 1 | 5.62 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 5.60 |
| CHEMBL3416172 | — | — | 1 | 5.57 |
| CHEMBL3416351 | — | — | 1 | 5.46 |
| CHEMBL221137 | EMBELIN | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3416360 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3416357 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3416361 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3416365 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3416358 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3416359 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3416348 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3416364 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2228912 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3416347 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3416180 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2296071 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3416356 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3416350 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3416174 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3416355 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL3416175 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3416173 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3416353 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL471270 | 5-O-METHYLEMBELIN | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3416179 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3416349 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3416352 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2228913 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2269075 | Sorgoleone-364 | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3416177 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL93 | ZILEUTON | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3416172 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3416351 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL221137 | EMBELIN | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3416164 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL462801 | Rapanone | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3416165 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3416354 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3416163 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3416178 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3416162 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416176 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416171 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416170 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416169 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416168 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416167 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416166 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL462998 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416362 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3416363 | — | IC50 | - | — | - | |
| CHEMBL221598 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3263323 | — | IC50 | > | 10000.0 | nM | - |