Timapiprant (formerly known as OC000459; OC-000459) is a novel, potent, selective, and orally bioactive prostanoid receptor 2 (DP2- also known as CRTH2)) antagonist with IC50 of 13 nM.

Latanoprost (PHXA-41, XA-34) is a novel prostaglandin F2α analogue that lowers the pressure by increasing the outflow of aqueous fluid from the eyes through the uvealsclearal tract.

CID 1375606 is the first selective surrogate agonist of orphan G protein-coupled receptor (GPCR) GPR27 identified from screening a diversity-oriented synthesis library.

GW9508 is a novel, potent and selective agonist for FFA1 (fatty acid receptor GPR40) with pEC50 of 7.32, and is 100-fold selective against GPR120, it stimulates insulin secretion in a glucose-sensitive manner.

TC-H 106 is a novel and potent HDAC inhibitor.

AS1269574 is a novel and potent GPR119 agonist.

Fasiglifam (formerly known as TAK-875; TAK875) is a novel, long-acting, selective and orally bioavailable GPR40 agonist with anti-diabetic activity.

AZD1981 is a novel potent and selective CRTh2 (Chemoattractant receptor-homologous molecule expressed on TH2 cells; DP2-Prostaglandin D2 receptor 2, ) receptor antagonist with IC50 of 4 nM, it displayed >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1.

GSK1292263 is a novel and potent GPR119 (G-protein-coupled receptor 119) agonist which has potential for the treatment of type 2 diabetes.

NE 52-QQ57 is a selective, and orally bioavailable GPR4 antagonist with an IC50 of 70 nM.