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. Author manuscript; available in PMC: 2013 May 28.
Published in final edited form as: Nat Rev Drug Discov. 2012 Jan 3;11(1):52–68. doi: 10.1038/nrd3620

Table 2.

Examples of serine hydrolase targets and lead inhibitors with potential therapeutic value.

Target Compound (Company, if applicable) Structure Ref(s) Potential Indication Developmen t Stage
FAAH OL-135 graphic file with name nihms466655t15.jpg 184 inflammatory pain; nervous system disorders preclinical
URB597 (Kadmus Pharmaceuticals) graphic file with name nihms466655t16.jpg 77 preclinical
PF-04457845 (Pfizer) graphic file with name nihms466655t17.jpg 13 Phase II
FAP/ dipeptidyl peptidases PT-100 (Point Therapeutics) graphic file with name nihms466655t18.jpg 143, 144 cancer Phase III (on hold)
LIPG ‘Sulfonylfuran urea 1’ (GlaxoSmithKline) graphic file with name nihms466655t19.jpg 121 cardiovascular disease preclinical
PLA2G7 Darapladib (GlaxoSmithKline) graphic file with name nihms466655t20.jpg 104 atherosclerosis Phase III
PRCP ‘Compound 8o’ (Merck) graphic file with name nihms466655t21.jpg 109 obesity preclinical
PREP S 17092 graphic file with name nihms466655t22.jpg 127 cognitive deficits preclinical
JTP-4819 (Japan Tobacco) graphic file with name nihms466655t23.jpg 126 preclinical
TGH GR148672X (GlaxoSmithKline) graphic file with name nihms466655t24.jpg 115 hypertriglycerid- emia preclinical

The electrophilic moieties of each compound, if applicable, are colored red.