Assay Detail
Binding
CHEMBL5730515
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FLAP 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. The reaction is allowed to proceed for two hours after which the plate is read on an Envision plate reader in HTRF mode.
704
Total Activities
217
Compounds Tested
3
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 |
|---|---|---|---|
| kon | 235 | - | - |
| k_off | 235 | - | - |
| Ki | 234 | 7.69 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3667000 | — | — | 3 | 9.47 |
| CHEMBL3667001 | — | — | 3 | 9.38 |
| CHEMBL3666967 | — | — | 3 | 9.33 |
| CHEMBL3666952 | — | — | 3 | 9.28 |
| CHEMBL3666951 | — | — | 3 | 9.21 |
| CHEMBL3666964 | — | — | 3 | 9.19 |
| CHEMBL3666965 | — | — | 3 | 9.18 |
| CHEMBL3662244 | — | — | 3 | 9.13 |
| CHEMBL3666999 | — | — | 6 | 9.09 |
| CHEMBL3666998 | — | — | 3 | 9.08 |
| CHEMBL3666989 | — | — | 3 | 9.02 |
| CHEMBL5965002 | — | — | 3 | 9.02 |
| CHEMBL3667002 | — | — | 3 | 8.96 |
| CHEMBL3666954 | — | — | 3 | 8.96 |
| CHEMBL3666953 | — | — | 3 | 8.96 |
| CHEMBL3666924 | — | — | 3 | 8.96 |
| CHEMBL3667003 | — | — | 3 | 8.92 |
| CHEMBL3667018 | — | — | 3 | 8.89 |
| CHEMBL3667004 | — | — | 3 | 8.89 |
| CHEMBL3667014 | — | — | 3 | 8.85 |
| CHEMBL3662259 | — | — | 6 | 8.85 |
| CHEMBL3666916 | — | — | 3 | 8.85 |
| CHEMBL3666976 | — | — | 3 | 8.85 |
| CHEMBL3662265 | — | — | 3 | 8.72 |
| CHEMBL3667016 | — | — | 3 | 8.66 |
| CHEMBL3662266 | — | — | 3 | 8.66 |
| CHEMBL3666993 | — | — | 3 | 8.66 |
| CHEMBL3666925 | — | — | 3 | 8.62 |
| CHEMBL3666978 | — | — | 3 | 8.62 |
| CHEMBL5903428 | — | — | 3 | 8.62 |
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 |
| CHEMBL5965002 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL3666953 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3666924 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3666954 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3667002 | — | 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 |
| CHEMBL3662259 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3667014 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3666976 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3666916 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3662265 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3662266 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3666993 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3667016 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL5903428 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3666978 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3666925 | — | 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 |
| CHEMBL3666960 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3662283 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3666912 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3666983 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3667005 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3662278 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3666968 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5869688 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL3666926 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3666980 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL5858788 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL5797242 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3666986 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL3662239 | — | 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 |