A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.

A potent BET bromodomian inhibitor with IC50 of 3-7 nM for BRD2/3/4 BD1 and BD2..

A potent benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity.

A potent BCL6 protein-protein interaction inhibitor with Kd of 78 nM.

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

A potent aromatase inhibitor for the treatment of hypogonadism..

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, brain penetrant FAAH inhibitor with IC50 of 11 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 voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 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.