Assay Detail
Binding
CHEMBL3420840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-L-691831 from human FLAP expressed in insect SF9 cell membranes after 2 hrs by Topcount analysis
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 8.23 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3417524 | — | — | 1 | 8.96 |
| CHEMBL3417526 | — | — | 1 | 8.92 |
| CHEMBL3417520 | — | — | 1 | 8.89 |
| CHEMBL3417414 | — | — | 1 | 8.85 |
| CHEMBL3417518 | — | — | 1 | 8.80 |
| CHEMBL3417525 | BI 665915 | — | 1 | 8.77 |
| CHEMBL3417429 | — | — | 1 | 8.72 |
| CHEMBL3417517 | — | — | 1 | 8.70 |
| CHEMBL3417531 | — | — | 1 | 8.68 |
| CHEMBL3417415 | — | — | 1 | 8.66 |
| CHEMBL3417428 | — | — | 1 | 8.64 |
| CHEMBL3417425 | — | — | 1 | 8.62 |
| CHEMBL3417427 | — | — | 1 | 8.62 |
| CHEMBL3417431 | — | — | 1 | 8.62 |
| CHEMBL3417422 | — | — | 1 | 8.60 |
| CHEMBL3417522 | — | — | 1 | 8.59 |
| CHEMBL3417508 | — | — | 1 | 8.59 |
| CHEMBL3417421 | — | — | 1 | 8.54 |
| CHEMBL3417527 | — | — | 1 | 8.54 |
| CHEMBL3417530 | — | — | 1 | 8.51 |
| CHEMBL3417511 | — | — | 1 | 8.46 |
| CHEMBL3417509 | — | — | 1 | 8.44 |
| CHEMBL3417510 | — | — | 1 | 8.44 |
| CHEMBL3417423 | — | — | 1 | 8.33 |
| CHEMBL3417417 | — | — | 1 | 8.24 |
| CHEMBL3417418 | — | — | 1 | 8.22 |
| CHEMBL3417416 | — | — | 1 | 8.21 |
| CHEMBL3417516 | — | — | 1 | 8.21 |
| CHEMBL3417513 | — | — | 1 | 8.17 |
| CHEMBL3417519 | — | — | 1 | 8.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3417524 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3417526 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3417520 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3417414 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3417518 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3417525 | BI 665915 | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3417429 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3417517 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3417531 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3417415 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3417428 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3417427 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3417431 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3417425 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3417422 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3417522 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3417508 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3417421 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3417527 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3417530 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3417511 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3417510 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3417509 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3417423 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3417417 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3417418 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3417416 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3417516 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3417513 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3417519 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3417426 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3417419 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3417412 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3417424 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3417420 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3417430 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3417521 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3417411 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3417515 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3417514 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3417523 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3417413 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3417528 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3417529 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3417512 | — | IC50 | > | 1000.0 | nM | - |