5-LOX activating protein   Click here for help

GtoPdb Ligand ID: 5183

Abbreviated name: FLAP
Synonyms: 5-lipoxygenase-activating protein | arachidonate 5-lipoxygenase-activating protein
Immunopharmacology Ligand
Compound class: Endogenous peptide in human, mouse or rat
Comment: FLAP is a scaffolding protein involved in leukotriene (eicosanoid proinflammatory mediator) biosynthesis. It has been investigated as a molecular target for novel anti-inflammatory drugs [3,5], in particular for airway inflammation [4,6].
Species: Human
Natural/Endogenous Targets
Target
5-LOX
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
5-LOX Ligand is endogenous in the given species Hs Activator Activation - - -
⤷
Other ligands which bind to or alter the activity of this ligand
Key to terms and symbols Click column headers to sort
Ligand Sp. Type Action Value Parameter Concentration range (M) Reference
BI 665915 Small molecule or natural product Hs Inhibitor Inhibition 8.8 pIC50 - 7
⤷ pIC50 8.8 (IC50 1.7x10-9 M) [7]
AZD5718 Small molecule or natural product Hs Inhibitor Inhibition 8.2 pIC50 - 2
⤷ pIC50 8.2 (IC50 6.3x10-9 M) [2]
Description: In a FLAP competition binding assay using cell membranes prepared from COS-7 cells expressing hFLAP and [3H]-MK0591 as tracer.
diflapolin Small molecule or natural product Primary target of this compound Hs Inhibitor Inhibition 7.5 pIC50 - 1
⤷ pIC50 7.5 (IC50 3x10-8 M) [1]
Description: Inhibition of 5-LOX product formation in intact human monocytes.