A potent bactericidal agent that inhibits the KinA autophosphorylation with IC50 of 1.6 uM.

A potent anticancer agent that demonstrates potent antitumor activity in vitro against several cancer cell lines as well as in vivo against several tumor models, effectively inhibits in vitro tubulin polymerization. .

A potent anthrax lethal toxin entry inhibitor with IC50 of 1.7 uM, inhibits endosomal trafficking pathways exploited by multiple toxins and viruses.

A potent and specific, nonlipid agonist of LPA2 receptor with EC50 of 100 nM, without activating or inhibiting LPA1/3/4/5 receptors.

A potent and specific CCR6 antagonist.

A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4.

A potent and selective, orally bioavailable, reversible BTK inhibitor with IC50 of 2.8 nM.

A potent and selective, orally bioavailable JAK2 inhibitor with IC50 of 2 nM.

A potent and selective, orally bioavailable aromatase inhibitor with IC50 of 1.7 nM, 180 times more potent than aminoglutethimide.

A potent and selective, non-ATP competitive, allosteric MAPKAPK2/3 (MK2/3) inhibitor with IC50 of 8 nM for MK2, hTNFα EC50 of 0.31 uM.

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 35 nM for PDE1B..

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 2.4 nM for PDE1B..

A potent and selective, CNS penetrant mGlu3 negative allosteric modulator with IC50 of 245 nM.

A potent and selective, CNS penetrant mGlu2 negative allosteric modulator with IC50 of 78 nM.

A potent and selective δ-opioid receptor agonist that has high affinity and selectivity for the δ1 subtype with Ki of 1.12 nM.

A potent and selective α4β2 nAChR agonist with Ki of 16 nM.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

A potent and selective tachykinin NK1 receptor antagonist with Ki of 2.9 nM.

A potent and selective small-molecule inhibitor of Lck with IC50 of 147 nM.

A potent and selective ROCK inhibitor with Ki of 1.6 nM.

A potent and selective RARγ receptor agonist with Ki of 150 nM.

A potent and selective PDE10A inhibitor with IC50 of 7.28 nM.

A potent and selective PDE10A inhibitor with binding affinity (Kd) of 0.15 nM, IC50 of 2.11 nM.

A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor.

A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.

A potent and selective mTOR inhibitor with Ki of 1.5 nM.

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.