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Synonyms: SB 659032
Compound class: Synthetic organic
Comment: Lipoprotein-associated phospholipase A2 (Lp-PLA2, PLA2-G7) inhibitors such as rilapladib and darapladib have been evaluated in clinical trials: darapladib for coronary heart disease, and rilapladib for Alzheimer's disease. Compounds of different chemotypes are being explored as tools to further optimise the pharmacological modulation of PLA2-G7 as a target for clinical intervention- see also (S)-23 [PMID: 27933945] (tool compound).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Davidson JE, Lockhart A, Amos L, Stirnadel-Farrant HA, Mooser V, Sollberger M, Regeniter A, Monsch AU, Irizarry MC. (2012)
Plasma lipoprotein-associated phospholipase A2 activity in Alzheimer's disease, amnestic mild cognitive impairment, and cognitively healthy elderly subjects: a cross-sectional study.
Alzheimers Res Ther, 4 (6): 51. [PMID:23217243]
2. Fitzpatrick AL, Irizarry MC, Cushman M, Jenny NS, Chi GC, Koro C. (2014)
Lipoprotein-associated phospholipase A2 and risk of dementia in the Cardiovascular Health Study.
Atherosclerosis, 235 (2): 384-91. [PMID:24929287]
3. Staurenghi G, Ye L, Magee MH, Danis RP, Wurzelmann J, Adamson P, McLaughlin MM, Darapladib DME Study Group. (2015)
Darapladib, a lipoprotein-associated phospholipase A2 inhibitor, in diabetic macular edema: a 3-month placebo-controlled study.
Ophthalmology, 122 (5): 990-6. [PMID:25749297]
4. Tjoelker LW, Wilder C, Eberhardt C, Stafforini DM, Dietsch G, Schimpf B, Hooper S, Le Trong H, Cousens LS, Zimmerman GA et al.. (1995)
Anti-inflammatory properties of a platelet-activating factor acetylhydrolase.
Nature, 374 (6522): 549-53. [PMID:7700381]
5. Wilensky RL, Macphee CH. (2009)
Lipoprotein-associated phospholipase A(2) and atherosclerosis.
Curr Opin Lipidol, 20 (5): 415-20. [PMID:19667981]