A highly potent and selective antagonist of the platelet P2Y1 receptor with Ki of 0.78 nM.

A highly potent and selective dual FAAH/MAGL inhibitor with IC50 of 1-3 nM against FAAH, inhibits mouse (IC50=410 nM) and human (IC50=1.4 uM) MAGL.

A highly potent and selective GRK2 inhibitor with IC50 of 18 nM.

A highly potent and selective inhibitor of CBP/p300 bromodomain with Kd of 0.23/0.47 uM respectively, with high selectivity over all other BD families, including the BET family.

A highly potent and selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT) in development for the treatment of nonalcoholic steatohepatitis (NASH)..

A highly potent and selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT) in development for the treatment of nonalcoholic steatohepatitis (NASH)..

A highly potent and selective kappa Opioid receptor (KOR) antagonist with Ki of 0.3 nM.

A highly potent and selective platelet activating factor (PAF) antagonist.

A highly potent and selective platelet activating factor (PAF) antagonist.

A highly potent and selective tankyrase inhibitor with pIC50 of 8.5 and 8.1 for TNKS1 and TNKS2, respectively.

A highly potent glucagon receptor antagonist..

A highly potent sigma receptor agonist with Ki of 1.7 nM and 25.2 nM for σ1 and σ2, respectively.

A highly potent, brain-penetrating ORL1 receptor (NOP receptor) agonist with Ki of 0.76 and 0.50  nM for rat and human ORL1 receptors, respectively.

A highly potent, functionally selective mGlu2 receptor agonist with EC50 of 13.6 nM in GTPγS functional binding assay.

A highly potent, long acting muscarinic receptor M3 antagonist with pIC50 of 9.8, inhibits M3 receptor in guinea pig trachea with pA2 of 9.4.

A highly potent, long-acting, orally active DPP4 inhibitor with Ki of 0.6 nM.

A highly potent, orally active hedgehog signaling (Hh) inhibitor with IC50 of 4.4 nM in Gli-luc reporter assays.

A highly potent, orally active VEGFR-2 inhibitor with IC50 of 8.5 nM, without activity against PKA, PKCα, PDK-1 and JNK3 (IC50>1 uM).

A highly potent, orally bioavailable, pan-VEGFR inibitor with IC50 of 1, 5, 3 nM for VEGFR1, 2, 3, respectively.

A highly potent, selective 5-HT2C receptor antagonist with pKi of 8.4 and 8.5 for human and rat 5-HT2C, respectively.

A highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor.