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 |
![]() |
184 | inflammatory pain; nervous system disorders | preclinical |
URB597 (Kadmus Pharmaceuticals) |
![]() |
77 | preclinical | ||
PF-04457845 (Pfizer) |
![]() |
13 | Phase II | ||
FAP/ dipeptidyl peptidases | PT-100 (Point Therapeutics) |
![]() |
143, 144 | cancer | Phase III (on hold) |
LIPG | ‘Sulfonylfuran urea 1’ (GlaxoSmithKline) |
![]() |
121 | cardiovascular disease | preclinical |
PLA2G7 | Darapladib (GlaxoSmithKline) |
![]() |
104 | atherosclerosis | Phase III |
PRCP | ‘Compound 8o’ (Merck) |
![]() |
109 | obesity | preclinical |
PREP | S 17092 |
![]() |
127 | cognitive deficits | preclinical |
JTP-4819 (Japan Tobacco) |
![]() |
126 | preclinical | ||
TGH | GR148672X (GlaxoSmithKline) |
![]() |
115 | hypertriglycerid- emia | preclinical |
The electrophilic moieties of each compound, if applicable, are colored red.