Assay Detail
Binding
CHEMBL3706320
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding 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 μg/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.
190
Total Activities
174
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
1,2,6-substituted benzimidazoles as flap modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 190 | 7.75 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3667000 | — | — | 1 | 9.47 |
| CHEMBL3667001 | — | — | 1 | 9.38 |
| CHEMBL3666967 | — | — | 1 | 9.33 |
| CHEMBL3666952 | — | — | 1 | 9.28 |
| CHEMBL3666951 | — | — | 1 | 9.21 |
| CHEMBL3666964 | — | — | 1 | 9.19 |
| CHEMBL3666965 | — | — | 1 | 9.18 |
| CHEMBL3662244 | — | — | 1 | 9.13 |
| CHEMBL3666999 | — | — | 2 | 9.09 |
| CHEMBL3666998 | — | — | 1 | 9.08 |
| CHEMBL3666989 | — | — | 1 | 9.02 |
| CHEMBL3666924 | — | — | 1 | 8.96 |
| CHEMBL3666953 | — | — | 1 | 8.96 |
| CHEMBL3666954 | — | — | 1 | 8.96 |
| CHEMBL3667002 | — | — | 1 | 8.96 |
| CHEMBL3667003 | — | — | 1 | 8.92 |
| CHEMBL3667018 | — | — | 1 | 8.89 |
| CHEMBL3667004 | — | — | 1 | 8.89 |
| CHEMBL3662239 | — | — | 6 | 8.85 |
| CHEMBL3662259 | — | — | 3 | 8.85 |
| CHEMBL3666916 | — | — | 1 | 8.85 |
| CHEMBL3666976 | — | — | 1 | 8.85 |
| CHEMBL3662265 | — | — | 1 | 8.72 |
| CHEMBL3662266 | — | — | 1 | 8.66 |
| CHEMBL3666993 | — | — | 1 | 8.66 |
| CHEMBL3666925 | — | — | 1 | 8.62 |
| CHEMBL3666978 | — | — | 1 | 8.62 |
| CHEMBL3662240 | — | — | 1 | 8.60 |
| CHEMBL3666966 | — | — | 1 | 8.60 |
| CHEMBL3666939 | — | — | 1 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3667000 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL3667001 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL3666967 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL3666952 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL3666951 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL3666964 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL3666965 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL3662244 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL3666999 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL3666998 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL3666989 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL3666954 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3667002 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3666953 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3666924 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3667003 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3667004 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3667018 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3662239 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3666916 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3666976 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3662259 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3662265 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3666993 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3662266 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3662239 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3666925 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3666978 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3662240 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3666966 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3666939 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3666912 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3662283 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3666960 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3666968 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3667005 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3662278 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3666983 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3666911 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3666926 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3666980 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3662239 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3666986 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3662268 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL3666987 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3662262 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3666914 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3662258 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL3666979 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL3662243 | — | Ki | = | 4.5 | nM | 8.35 |