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Inhibitor Report for: Rilapladib

Rilapladib is the third genomics-derived small molecule drug arising from the Human Genome Sciences-GlaxoSmithKline collaboration to enter clinical development. It is a lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor. Lp-PLA2 is an enzyme associated with the formation of atherosclerotic plaques.



General
Type: Trifluoro, Piperidine, Sulfur Compound
Chemical_Nomenclature: 2-[2-[(2,3-difluorophenyl)methylsulfanyl]-4-oxoquinolin-1-yl]-N-[1-(2-methoxyethyl)piperidin-4-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide
Canonical SMILES: COCCN1CCC(CC1)N(CC2=CC=C(C=C2)C3=CC=C(C=C3)C(F)(F)F)C(=O)CN4C5=CC=CC=C5C(=O)C=C4SCC6=C(C(=CC=C6)F)F
InChI: InChI=1S/C40H38F5N3O3S/c1-51-22-21-46-19-17-32(18-20-46)47(24-27-9-11-28(12-10-27)29-13-15-31(16-14-29)40(43,44)45)37(50)25-48-35-8-3-2-6-33(35)36(49)23-38(48)52-26-30-5-4-7-34(41)39(30)42/h2-16,23,32H,17-22,24-26H2,1H3
InChIKey: NNBGCSGCRSCFEA-UHFFFAOYSA-N
Other name(s): UNII-O14CWE893Z ; Rilapladib (USAN) ; SB 659032 ; SB659032 ; D05728 ; DB05119
MW: 735.80
Formula: C40H38F5N3O3S
CAS_number: 412950-08-4
PubChem: 9918381
IUPHAR: 7376
Wikipedia:

Target families
Rilapladib ligand of proteins in family: PAF-Acetylhydrolase
No structure

Protein target
Enzyme: human-PLA2G7

References
Search PubMed for references concerning: Rilapladib

3 more
    Title: Lipoprotein-associated phospholipase A2 and risk of dementia in the Cardiovascular Health Study
    Fitzpatrick AL, Irizarry MC, Cushman M, Jenny NS, Chi GC, Koro C
    Ref: Atherosclerosis, 235:384, 2014 : PubMed

            

    Title: Plasma lipoprotein-associated phospholipase A2 activity in Alzheimer's disease, amnestic mild cognitive impairment, and cognitively healthy elderly subjects: a cross-sectional study
    Davidson JE, Lockhart A, Amos L, Stirnadel-Farrant HA, Mooser V, Sollberger M, Regeniter A, Monsch AU, Irizarry MC
    Ref: Alzheimers Res Ther, 4:51, 2012 : PubMed

            

    Title: Lipoprotein-associated phospholipase A(2) and atherosclerosis
    Wilensky RL, Macphee CH
    Ref: Curr Opin Lipidol, 20:415, 2009 : PubMed