AZD5718

Ligand id: 10352

Name: AZD5718

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 7
Hydrogen bond donors 3
Rotatable bonds 6
Topological polar surface area 121.77
Molecular weight 446.21
XLogP 3.32
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

Classification
Compound class Synthetic organic
IUPAC Name
(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]-N-(4-oxo-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-3-yl)cyclohexane-1-carboxamide
Synonyms
compound 12 [PMID: 30869888]
Comments
AZD5718 is an inhibitor of 5-LOX activating protein (FLAP) that was developed by Astra Zeneca [4]. It is orally active and is suitable for once-daily dosing. Initial clinical findings from a first-in-human study confirmed AZD5718 target engagement, and indicated that the compound is safe and well tolerated [2]. It is being advanced for further evaluation in patients with coronary artery disease. The 5-LOX pathway has been targeted for drug development as an intervention in a number of diseases where chronic inflammation drives the pathophysiology (e.g. asthma, chronic obstructive pulmonary disease and atherosclerotic coronary artery disease). Since FLAP is a crucial regulator of 5-LOX activity, it too is being pursued as a druggable anti-inflammatory target. FLAP inhibitors and 5-LOX inhibitors reduce production of the leukotriene precursor LTA4 [1,3].
Database Links
PubChem CID 122678117
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Search UniChem for chemical match using the InChIKey ROTWSDMXHVGAHZ-QZTJIDSGSA-N
Search UniChem for chemicals with the same backbone ROTWSDMXHVGAHZ