A novel potent, selective hERG potassium channel (Kv11.1) activator that induces a leftward shift in the voltage dependence of activation..

A novel potent, selective cannabinoid receptor 2 (CB2) agonist with Ki of 12 nM, >30-fold selectivity over CB1.

A novel potent, partial LXRβ-selective agonist (EC50=9 nM) with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays.

A novel potent, orally active, dual-acting aromatase and steroid sulfatase (STS) inhibitor with ICI0 of 0.82 nM and 39 nM, respectively.

A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM.

A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively.

A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively.

A novel potent, irreversible and orally active inhibitor of steroid sulfatase (STS) with IC50 of 13 nM in ZR-75-1 cells.

A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays.

A novel potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1.

A novel potent, highly selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 0.99, 1.65 and 57.3 nM for human FAAH-1, FAAH-1 (P129T) and FAAH-2, respectively.

A novel potent, competitive squalene synthase inhibitor that upregulate the LDLR in mouse and human liver cell lines with EC50 of 26 nM.

A novel potent, combined serotonin 5-HT1A and 5-HT1B receptor antagonist with Ki of 0.13 and 2.4 nM in brain homogenates, respectively.

A novel potent, and selective prostaglandin EP4 receptor antagonist with binding IC50 of 2.4 nM.

A novel potent TOPK inhibitor that effectively suppresses SUV-induced activation of MAPKs signal transduction resulting in reduced SUV-induced skin carcinogenesis.

A novel potent small-molecule BET bromodomain (BRD) inhibitor that binds to BET proteins with Ki values of <1 nM.

A novel potent LIMK inhibitor with IC50 of 8 nM and 32 nM for LIMK1 and LIMK2, respectively.

A novel potent LIMK inhibitor with IC50 of 0.3 nM and 1 nM for LIMK1 and LIMK2, respectively.

A novel potent gonadotrophin releasing hormone (GnRH) antagonist..

A novel potent gonadotrophin releasing hormone (GnRH) antagonist..

A novel potent CFTR potentiator with Kd of 31.7 nM.

A novel potent CFTR potentiator that blocks hCFTR with apparent Kd of 71.3 uM.

A novel potent CDK inhibitor with IC50 of 79 nM, 63 nM and 20 nM for Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, respectively.

A novel potent cdc2-like kinase (CLKs) and DYRKs inhibitor with IC50 of 40, 35 and 15 nM for DYRK1A, DYRK2 and CLK1, respectively.

A novel potent cannabinoid receptor agonist..

A novel potent bitter receptor (TAS2Rs) antagonist that inhibits activation of hTAS2R31 by saccharin and acesulfame K with IC50 of 6.4 and 7.9 uM respectively.

A novel potent Aurora kinase inhibitor that inhibits Aurora-A and Aurora-B with IC50 of 24 nM and 45 nM, respectively.

A novel potent and selective, orally active URAT1 inhibitor with Ki of 57 nM, 130 and 42-fold selectivity over OAT1 and OAT3, respectively.

A novel potent (IC50=910 ng/mL), highly selective microsomal prostaglandin E synthase 1 inhibitor (mPGES-1) for treatment of undisclosed indications..

A novel potent "funny" If current channel (If channel) inhibitor that inhibits rOct1- and hOCT1-mediated [3H]MPP uptake with IC50 of 23.8 and 40.5 uM, respectively.