Assay Detail
Binding
CHEMBL4053619
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Inhibition of human recombinant 5-LO expressed in Escherichia coli MV1190 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by RP-HPLC analysis
16
Total Activities
16
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
Evaluation of Dual 5-Lipoxygenase/Microsomal Prostaglandin E2 Synthase-1 Inhibitory Effect of Natural and Synthetic Acronychia-Type Isoprenylated Acetophenones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.59 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.10 |
| CHEMBL1242095 | — | — | 1 | 6.00 |
| CHEMBL4087914 | — | — | 1 | 5.77 |
| CHEMBL4077368 | — | — | 1 | 5.70 |
| CHEMBL4069303 | — | — | 1 | 5.62 |
| CHEMBL4075212 | — | — | 1 | 5.60 |
| CHEMBL488313 | — | — | 1 | 5.57 |
| CHEMBL4080027 | — | — | 1 | 5.44 |
| CHEMBL1992376 | ACROFOLIONE A | — | 1 | 5.28 |
| CHEMBL4101532 | — | — | 1 | 5.22 |
| CHEMBL4078358 | — | — | 1 | 5.14 |
| CHEMBL29097 | — | — | 1 | - |
| CHEMBL4096534 | — | — | 1 | - |
| CHEMBL4104264 | — | — | 1 | - |
| CHEMBL1241050 | — | — | 1 | - |
| CHEMBL1984096 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL93 | ZILEUTON | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1242095 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4087914 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4077368 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4069303 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4075212 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL488313 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4080027 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1992376 | ACROFOLIONE A | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4101532 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4078358 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL29097 | — | IC50 | - | — | - | |
| CHEMBL4096534 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4104264 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1241050 | — | IC50 | - | — | - | |
| CHEMBL1984096 | — | IC50 | > | 10000.0 | nM | - |