Assay Detail
Binding
CHEMBL3420841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLAP in calcimycin-stimulated human whole blood assessed as inhibition of LTB4 synthesis preincubated for 15 mins followed by calcimycin stimulation measured after 30 mins
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Arachidonate 5-lipoxygenase-activating protein (CHEMBL4550) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 45 | 6.73 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3417530 | — | — | 1 | 7.85 |
| CHEMBL3417520 | — | — | 1 | 7.82 |
| CHEMBL3417531 | — | — | 1 | 7.70 |
| CHEMBL3417527 | — | — | 1 | 7.52 |
| CHEMBL3417518 | — | — | 1 | 7.48 |
| CHEMBL3417525 | BI 665915 | — | 1 | 7.35 |
| CHEMBL3417429 | — | — | 1 | 7.35 |
| CHEMBL3417517 | — | — | 1 | 7.34 |
| CHEMBL3417509 | — | — | 1 | 7.33 |
| CHEMBL3417431 | — | — | 1 | 7.19 |
| CHEMBL3417524 | — | — | 1 | 7.18 |
| CHEMBL3417511 | — | — | 1 | 7.16 |
| CHEMBL3417526 | — | — | 1 | 7.14 |
| CHEMBL3417510 | — | — | 1 | 7.09 |
| CHEMBL3417522 | — | — | 1 | 7.04 |
| CHEMBL3417513 | — | — | 1 | 7.03 |
| CHEMBL3417428 | — | — | 1 | 6.96 |
| CHEMBL3417427 | — | — | 1 | 6.80 |
| CHEMBL3417516 | — | — | 1 | 6.72 |
| CHEMBL3417425 | — | — | 1 | 6.70 |
| CHEMBL3417508 | — | — | 1 | 6.62 |
| CHEMBL3417416 | — | — | 1 | 6.62 |
| CHEMBL3417415 | — | — | 1 | 6.60 |
| CHEMBL3417422 | — | — | 1 | 6.57 |
| CHEMBL3417426 | — | — | 1 | 6.51 |
| CHEMBL3417418 | — | — | 1 | 6.47 |
| CHEMBL3417521 | — | — | 1 | 6.46 |
| CHEMBL3417417 | — | — | 1 | 6.44 |
| CHEMBL3417519 | — | — | 1 | 6.44 |
| CHEMBL3417419 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3417530 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3417520 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3417531 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3417527 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3417518 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3417525 | BI 665915 | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3417429 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3417517 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3417509 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3417431 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3417524 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3417511 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3417526 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3417510 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3417522 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3417513 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3417428 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3417427 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3417516 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3417425 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3417508 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3417416 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3417415 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3417422 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3417426 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3417418 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3417521 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3417417 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3417519 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3417419 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3417411 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3417412 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3417414 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3417420 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3417528 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3417515 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3417423 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3417514 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3417424 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3417523 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3417512 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3417413 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3417430 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3417529 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3417421 | — | IC50 | > | 5000.0 | nM | - |