Assay Detail
Binding
CHEMBL1924645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calcium ionophore A23187-induced LTB4 production after 1 hr by ELISA in absence of human serum albumin
4
Total Activities
4
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
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.80 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL313489 | QUIFLAPON SODIUM | -1.0 | 1 | 9.00 |
| CHEMBL1922660 | FIBOFLAPON | 3.0 | 1 | 9.00 |
| CHEMBL557527 | — | — | 1 | 8.96 |
| CHEMBL29097 | — | — | 1 | 8.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL313489 | QUIFLAPON SODIUM | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1922660 | FIBOFLAPON | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL557527 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL29097 | — | IC50 | = | 5.7 | nM | 8.24 |