A potent and selective melanocortin 4 receptor (MC4R) agonist with EC50 of 2.1 nM.

A potent and selective MCH-R1 antagonist with IC50 of 22 nM, Ki of 14 nM.

A potent and selective linear tachykinin NK2 receptor antagonist with pKb of 9.3.

A potent and selective inhibitors of leukotriene C4 synthase (LTC4S) with IC50 of 95 nM, Ki of 6 nM.

A potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM.

A potent and selective inhibitor of neutral endopeptidase (NEP) with IC50 of 18.9 nM for hNEP.

A potent and selective inhibitor of MTH1 protein with IC50 of 5 nM.

A potent and selective inhibitor of mediator-associated kinase CDK8 (IC50=12 nM) and its paralogue CDK19.

A potent and selective inhibitor of IRE1 endoribonuclease with IC50 of 0.41 uM.

A potent and selective inhibitor of HIV-1 protease with IC90 of 4-40 nM.

A potent and selective inhibitor of FAK phosphorylation with biochemical IC50 of 1.2 pM (pFAK Y397), cellular IC50 of 1 nM.

A potent and selective inhibitor of breast cancer cells via activation the aryl hydrocarbon receptor (AhR) pathway.

A potent and selective IKK-2 inhibitor with IC50 of 0.3 uM.

A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM.

A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM.

A potent and selective human PPARα agonist with EC50 of 4 nM, >1,000-fold selectivity over human PPARγ (EC50=4.5 uM) and PPARδ (EC50 >100 uM) in PPAR-GAL4 transactivation assays.

A potent and selective HDAC8 inhibitor with IC50 of 70 nM.

A potent and selective HDAC8 inhibitor with IC50 of 0.5 uM..

A potent and selective HDAC3 inhibitor with IC50 of 0.26 uM, with no activity against HDAC1/4/6/8.

A potent and selective HDAC3 inhibitor with IC50 of 0.24 uM, >75-fold selectivity over HDAC1 and no activity against HDAC4/6/8.

A potent and selective group I PAK (pan-PAK1/2/3) inhibitor with Ki of 0.95/2 nM for PAK1/2, respectively.

A potent and selective GlyT1 inhibitor with EC50 of 54 nM.

A potent and selective dopamine D3 receptor antagonist with pKi of 8.0.

A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.

A potent and selective ATP-competitive inhibitor of CHK2 K5777:N5777with IC50 of 3 nM.

A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.

A potent and selective antagonist of H3 receptor with Ki/EC50 of 0.16/1.5 nM.

A potent and selective ALK5 inhibitor with IC50 of 5.5 nM, displays 300-fold selecitvity over ALK3.

A potent and selective agonist for the cannabinoid receptor CB1 with Ki of 0.28 nM, 180-fold selectivity over CB2..

A potent and selective 5-HT3 receptor antagonist has been shown to be beneficial in the treatment of irritable bowel syndrome..