Assay Detail
Binding
CHEMBL1924526
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of COX1-mediated TXB2 production in human whole blood after 30 mins by competitive enzyme immunoassay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 11 | 5.06 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1922661 | — | — | 1 | 6.21 |
| CHEMBL1922664 | — | — | 1 | 5.50 |
| CHEMBL1922666 | — | — | 1 | 5.05 |
| CHEMBL1922655 | — | — | 1 | 4.75 |
| CHEMBL1229205 | — | — | 1 | 4.60 |
| CHEMBL1922660 | FIBOFLAPON | 3.0 | 1 | 4.24 |
| CHEMBL1922654 | — | — | 1 | - |
| CHEMBL1922657 | — | — | 1 | - |
| CHEMBL1922658 | — | — | 1 | - |
| CHEMBL1922663 | — | — | 1 | - |
| CHEMBL1922667 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1922661 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1922664 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1922666 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1922655 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1229205 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1922660 | FIBOFLAPON | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL1922654 | — | IC50 | - | — | - | |
| CHEMBL1922657 | — | IC50 | - | — | - | |
| CHEMBL1922658 | — | IC50 | - | — | - | |
| CHEMBL1922663 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1922667 | — | IC50 | - | — | - |