Assay Detail
Binding
CHEMBL3420848
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLAP in calcimycin-stimulated mouse whole blood assessed as inhibition of LTB4 synthesis preincubated for 15 mins followed by calcimycin stimulation measured after 30 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Arachidonate 5-lipoxygenase-activating protein (CHEMBL3414408) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.57 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3417531 | — | — | 1 | 5.82 |
| CHEMBL3417525 | BI 665915 | — | 1 | 5.32 |
| CHEMBL3417530 | — | — | 1 | - |
| CHEMBL3417511 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3417531 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3417525 | BI 665915 | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3417530 | — | IC50 | - | — | - | |
| CHEMBL3417511 | — | IC50 | - | — | - |