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 clathrin-independent endocytosis with IC50 of 18 uM (inhibition of clathrin TD-amphiphysin B/C complex formation).

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

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

A potent, selective CCK1 receptor agonist with EC50 of 0.47 nM.

a potent, selective CBP bromodomain inhibitor with IC50 of 69 nM, displays exquisite selectivity over BRD4(1) (IC50=18 uM) and the broader bromodomain family..

A potent, selective CB1 cannabinoid receptor antagonist with Ki of 350 fM, >60,000-fold selective for the CB1 receptor versus CB2 receptor (Ki=21 nM).