2-AG, 2-arachidonoyl glycerol; 2-Arachidaoylglycerol; 2-OG, 2-oleoylglycerol; 4-NPA, 4-nitrophenylacetate; 7-HCA, 7-hydroxycoumarinyl arachidonate; AA, arachidonic acid; ABHD6 and ABHD12, α/ß-hydrolase 6 and 12; ABP, activity-based probes; ABPP, activity-based protein profiling; AD, Alzheimer's disease; AEA, anandamide; Arachidonic acid; BCRP, breast cancer resistant protein; CB1R and CB2R, cannabinoid receptors; CC-ABPP, click chemistry activity-based protein profiling; CFA, complete Freund's adjuvant; CNS, central nervous system; COX, cyclooxygenases; CYP, cytochrome P450 proteins; Cancer; DAG, diacylglycerol; DAGLs, diacylglycerol lipases; DTT, dithiothreitol; Drug discovery; EAE, encephalomyelitis; EI, enzyme­inhibitor complex; FAAH, amide hydrolase; FFAs, free fatty acids; FP, fluorophosphonate; FP-Rh, fluorophosphonate-rhodamine; FQ, fit quality; HFD, high-fat diet; HFIP, hexafluoroisopropyl; LC­MS, liquid chromatographic mass spectrometry; LFD, low-fat diet; MAGL, monoacylglycerol lipase; MAGs, monoglycerides; MS, multiple sclerosis; Metabolic syndrome; Monoacylglycerol lipases; NAM, N-arachidonoyl maleimide; NHS, N-hydroxysuccinimidyl; Neuroinflammation; OCT2, organic cation transporter 2; P-gp, P-glycoprotein; PA, phosphatidic acid; PD, Parkinson's disease; PET, positron emission tomography; PGE2, prostaglandin; PGs, prostaglandins; PK, pharmacokinetic; PLA2G7, phospholipase A2 group VII; SAR, structure­activity relationship; SBDD, structure-based drug design; SDS-PAGE, sodium dodecyl sulphate polyacrylamide gel electrophoresis; THL, tetrahydrolipstatin; cPLA2, cytosolic phospholipase A2