A potent, selective noncovalent competitive inhibitor of HCV NS3/4A protease with Ki of 2.6 and 2.0 nM for GT1a and 1b NS3-NS4A protease, respectively.

A potent, selective NaV1.7 blocker with IC50 of 3 nM.

A potent, selective mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM.

A potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, respectively.

A potent, selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 10.4 nM.

A potent, selective melanin concentrating hormone receptor 1 (MCH-R1) antagonist with binding Ki of 12.2 nM.

A potent, selective LPA2 (EDG4) antagonist with IC50 of 17 nM.

A potent, selective LIMK inhibitor with IC50 of 3.2 nM and 1.2 nM for LIMK1 and LIMK2, respectively.

A potent, selective LIMK inhibitor with IC50 of 0.9 nM and 0.5 nM and 1.2 nM for LIMK1 and LIMK2, respectively.

A potent, selective kappa-opioid receptor agonist with no μ-opioid antagonist effects.

A potent, selective IRAK4 inhibitor with IC50 of 1.3 nM, 200-fold selectivity over IRAK1 (IC50=290 nM).

A potent, selective IRAK4 inhibitor with IC50 of 0.094 nM, >500-fold selectivity over IRAK1 (IC50=65 nM).

A potent, selective intermediate-conductance KCa3.1 positive-gating modulator with EC50 of 111 nM.

A potent, selective inhibitor of protein phosphatase 2A (PP2A) with IC50 of 0.04 nM.

A potent, selective inhibitor of p300 histone acetyltransferase (IC50=4.2 uM).

A potent, selective inhibitor of HIV integrase (IC50=8-15 nM) with potent antiviral activity in cell culture and good pharmacokinetic properties.

A potent, selective inhibitor of CXCR4 with IC50 of 13 nM, has no effect on CXCR1, CCR3, CCR4, or CCR5.

A potent, selective inhibitor of cdc2-like kinase CLK1 and CLK2 with IC50 of 1.1 and 2.4 nM, respectively.

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 and HDAC2 inhibitor with IC50 of 6 nM and 45 nM, respectively.

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

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