A potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with IC50 of 620 nM (inhibition of NO production).

A potent, selective high affinity TrkA receptor agonist with Kd of 75 nM.

A potent, selective HIF-1 inhibitor with IC50 of 1.9 nM, with no signigicant inhibition on HSF and NF-κB.

A potent, selective hERG potassium channel (Kv11.1) activator that increases peak tail hERG current of 111.1% at 10 uM in HEK293 cells.

A potent, selective HDAC6 inhibitor with IC50 of 84 nM, with IC50s of >3.5 uM for the other HDAC isoforms..

A potent, selective HDAC1 inhibitor with IC50 of 1.5 uM.

A potent, selective HDAC1 and HDAC2 inhibitor with IC50 of 6 nM and 45 nM, respectively.

A potent, selective Grp94 inhibitor with Kd of 0.44 uM.

A potent, selective Grp94 inhibitor with Kd of 0.2 uM.

A potent, selective Grp94 inhibitor with IC50 of 8 nM.

A potent, selective GlyT1 inhibitor that demonstrates >10-fold greater activity in in vitro functional glycine reuptake assay than racemic (±)-NFPS.

A potent, selective glycine transporter 1 (GlyT1) inhibitor with IC50 of 100 nM.

A potent, selective glucose transporter 4 (GLUT4) inhibitor with IC450 of 10.8 uM, inhibits MM cell proliferation.

A potent, selective GLP-1 agonist.

A potent, selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 8 nM.

A potent, selective FABP4 inhibitor with Ki of 30 nM..

A potent, selective estrogen receptor downregulator (SERD) with ER downregulation pIC50 of 9.68.

A potent, selective dopamine D4 receptor agonist with Ki of 12.1 and 7.9 nM for rat and human D4 receptors, respectively.

A potent, selective dopamine D4 receptor agonist that activates human dopamine D4 receptors with EC50 of 12.4 nM, with no effect on dopamine D1, D2, D3, or D5 receptors.

A potent, selective dopamine D4 receptor agonist that activates human dopamine D4 receptors with EC50 of 12.4 nM, with no effect on dopamine D1, D2, D3, or D5 receptors.

A potent, selective dopamine D1 receptor antagonist with Ki of 0.56 nM.

A potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor for treatment for type 2 diabetes..

A potent, selective D1 dopamine receptor antagonist with Ki of 3.6 nM, >300-fold selectivity over D2 and 5-HT2 receptors.

A potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM.

A potent, selective COX-2 inhibitor with IC50 of 0.34 ug/mL, >50-fold selectivity over COX-1 (IC50=19.4 ug/mL).

A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-fold selectivity over ChoKβ.

A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.13 uM, >385-fold selectivity over ChoKβ.

A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.12 uM, >400-fold selectivity over ChoKβ.

A potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD)..

A potent, selective cell permeable neuronal nitric oxide synthase (nNOS) inhibitor with Ki of 30 nM.