Assay Detail
Binding
CHEMBL3705828
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Homogeneous Time Resolved Fluorescence Assay: The assay below is used to test the modulatory activity of compounds against FLAP. Human and mouse FLAP-encoding DNA was amplified by polymerase chain reaction and cloned into pFastBac1 (Invitrogen) with a NH2-terminal 6-His tag for expression in Spodoptera frugiperda (Sf-9) cells. FLAP-containing membranes were prepared as was a FITC-labeled FLAP modulator (3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid). The FLAP binding assay is performed in HTRF format (homogeneous time resolved fluorescence). FLAP-containing membranes (1 ug/well final for human) are incubated in the presence of the HTRF ligand, [5-[({[2-(2-{3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoyl}hydrazino)-2-oxoethyl]sulfanyl}acetyl)amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid] (25 nM final), a terbium labeled anti-His tag antibody (0.5 ng/well final, from Cisbio) and compounds.
335
Total Activities
332
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
Arachidonate 5-lipoxygenase-activating protein (CHEMBL4550) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Flap modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 335 | 7.33 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3704300 | — | — | 1 | 9.40 |
| CHEMBL3659304 | — | — | 1 | 9.30 |
| CHEMBL3659301 | — | — | 1 | 9.05 |
| CHEMBL3704245 | — | — | 1 | 9.00 |
| CHEMBL3704248 | — | — | 1 | 9.00 |
| CHEMBL3704256 | — | — | 1 | 9.00 |
| CHEMBL3704298 | — | — | 1 | 8.96 |
| CHEMBL3659272 | — | — | 1 | 8.92 |
| CHEMBL3704289 | — | — | 1 | 8.89 |
| CHEMBL3704294 | — | — | 1 | 8.89 |
| CHEMBL3704303 | — | — | 1 | 8.89 |
| CHEMBL3659293 | — | — | 1 | 8.89 |
| CHEMBL3659257 | — | — | 1 | 8.85 |
| CHEMBL3704296 | — | — | 1 | 8.77 |
| CHEMBL3704266 | — | — | 1 | 8.72 |
| CHEMBL3704181 | — | — | 1 | 8.70 |
| CHEMBL3640031 | — | — | 1 | 8.70 |
| CHEMBL3704351 | — | — | 1 | 8.66 |
| CHEMBL3659267 | — | — | 1 | 8.66 |
| CHEMBL3704307 | — | — | 1 | 8.64 |
| CHEMBL3704265 | — | — | 1 | 8.62 |
| CHEMBL3659340 | — | — | 1 | 8.62 |
| CHEMBL3659256 | — | — | 1 | 8.60 |
| CHEMBL3659261 | — | — | 1 | 8.60 |
| CHEMBL3704323 | — | — | 1 | 8.55 |
| CHEMBL3704297 | — | — | 1 | 8.54 |
| CHEMBL3704350 | — | — | 1 | 8.54 |
| CHEMBL3704249 | — | — | 1 | 8.52 |
| CHEMBL3704278 | — | — | 1 | 8.52 |
| CHEMBL3659266 | — | — | 1 | 8.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3704300 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3659304 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3659301 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3704256 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3704248 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3704245 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3704298 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3659272 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3704303 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3704294 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3704289 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3659293 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3659257 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3704296 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3704266 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3640031 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3704181 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3704351 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3659267 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3704307 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3659340 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3704265 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3659256 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3659261 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3704323 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3704297 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3704350 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3704278 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3704249 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3659266 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3659268 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3704290 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL3659273 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3659358 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3704291 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3704284 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3704349 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3659290 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3704293 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL3704276 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3704246 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3704247 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3704162 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3704309 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3704342 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3659322 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3704251 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3704178 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3704244 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3704295 | — | Ki | = | 5.0 | nM | 8.30 |