A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator.

A highly potent, selective inhibitor of checkpoint kinase TTK/Mps1 with IC50 of 0.6 nM.

A highly potent, selective imidazoline I2 receptor agonist with Ki of 9.8 nM, enhances supraspinal morphine analgesia in mice..

A highly potent, selective EZH2 inhibitor with biochemical IC50 of 2 nM, cellular EC50 of 32 nM.

A highly potent, selective CGRP receptor antagonist with Ki of 21 pM in in vitro binding assay and IC50 of 0.12 nM in cell-based functional assay.

A highly potent, selective beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.9 nM in Ca2+ flux assay.

A highly potent, selective beta-hairpin mimetic CXCR4 inhibitor with IC50 of 1.2 nM in Ca2+ flux assay.

A highly potent, selective and time-dependent Cdc7 kinase inhibitor with IC50 of 0.7 nM with slow dissociation property, with 200-fold and >14,000-fold selectivity over CDK2 and ROCK1, respectively.

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

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

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

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

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 glucagon receptor antagonist..

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

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

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

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 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 GRK2 inhibitor with IC50 of 18 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 antagonist of the platelet P2Y1 receptor with Ki of 0.78 nM.

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

A highly potent and competitive S-adenosylhomocysteine hydrolase inhibitor with Ki of 0.05 nM, also inhibits histone methyltransferase EZH2.

A high-affinity, selective platelet integrin αIIbβ3 receptor antagonist with IC50 of 96 nM.

A high-affinity, allosteric HIV-1 and HIV-2 reverse transcriptase inhibitor (NNRTI) with EC50 of 1 nM.