Assay Detail
Binding
CHEMBL618070
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-lipoxygenase in intact rat basophilic leukemia cells stimulated with the calcium ionophore A-23187
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | RBL-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.93 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112733 | — | — | 1 | 6.80 |
| CHEMBL49249 | — | — | 1 | 6.77 |
| CHEMBL325065 | — | — | 1 | 6.66 |
| CHEMBL295739 | — | — | 1 | 6.42 |
| CHEMBL113525 | — | — | 1 | 6.32 |
| CHEMBL12594 | E-5110 | — | 1 | 6.25 |
| CHEMBL16048 | — | — | 1 | 6.20 |
| CHEMBL280226 | — | — | 1 | 6.19 |
| CHEMBL109501 | — | — | 1 | 6.16 |
| CHEMBL109745 | DARBUFELONE MESYLATE | -1.0 | 1 | 6.11 |
| CHEMBL48814 | — | — | 1 | 6.11 |
| CHEMBL47223 | — | — | 1 | 6.08 |
| CHEMBL16434 | — | — | 1 | 6.04 |
| CHEMBL111438 | — | — | 1 | 5.92 |
| CHEMBL113138 | — | — | 1 | 5.92 |
| CHEMBL15904 | — | — | 1 | 5.89 |
| CHEMBL49008 | — | — | 1 | 5.85 |
| CHEMBL278246 | — | — | 1 | 5.80 |
| CHEMBL113211 | — | — | 1 | 5.77 |
| CHEMBL2111719 | — | — | 1 | 5.77 |
| CHEMBL113908 | — | — | 1 | 5.64 |
| CHEMBL8562 | — | — | 1 | 5.60 |
| CHEMBL326108 | — | — | 1 | 5.58 |
| CHEMBL48568 | — | — | 1 | 5.55 |
| CHEMBL325315 | — | — | 1 | 5.48 |
| CHEMBL277721 | — | — | 1 | 5.43 |
| CHEMBL112720 | — | — | 1 | 5.14 |
| CHEMBL1562610 | MECLOFENAMATE SODIUM | 4.0 | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112733 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL49249 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL325065 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL295739 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL113525 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL12594 | E-5110 | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL16048 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL280226 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL109501 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL109745 | DARBUFELONE MESYLATE | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL48814 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL47223 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL16434 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL111438 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL113138 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL15904 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL49008 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL278246 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL113211 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2111719 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL113908 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL8562 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL326108 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL48568 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL325315 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL277721 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL112720 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1562610 | MECLOFENAMATE SODIUM | IC50 | = | 24000.0 | nM | 4.62 |