A potent, second generation HCV NS3 serine protease inhibitor with Ki of 6 nM.

A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity.

A potent, selectiive inhibitor of WNK1 kinase with IC50 of 95 nM, shows IC50 of 1.39 uM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility..

A potent, selective 5-HT2A receptor antagonist with Ki of 0.36 nM, > 80-fold selectivity for 5-HT2A over other serotonergic receptors.

A potent, selective 5-HT2B receptor agonist with pKi of 7.1, >10-fold selectivity over 5-HT2A, 5-HT2C, and other 5-HT subtypes.

A potent, selective 5-HT2C receptor agonist with IC50 of 20 nM in HEK293 cells-exppressed 5-HT2C, shows weakly activity for 5-HT2A.

A potent, selective A2A adenosine receptor antagonist with Ki of 6.6 nM.

A potent, selective agonist of 5-HT1A and 5-HT1B receptors, with preference for 5-HT1B.

A potent, selective agonist of PBR/TSPO that inhibits [3H]PK 11195 binding to crude mitochondrial preparations of rat whole brain with IC50 of 0.92 nM..

A potent, selective agonist of the human and rat CCK1 receptor with Ki of 36 nM.

A potent, selective agonist of the orphan GPR88 receptor with EC50 of 877 nM.

A potent, selective agonist of the rat (EC50=97 nM) and human (EC50=23 nM) TRPA1 channel.

A potent, selective ALK5 inhibitor with IC50 of 4.8 nM, >100-fold selectivity over 95 different kinases.

A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM.

A potent, selective and ATP-competitive inhibitor of IKK2 with IC50 of 60 nM and Ki of 20 nM, also interfers directly with FLT3 kinase activation.

A potent, selective and cell active Hedgehog acyltransferase (Hhat) inhibitor with IC50 of 0.87 uM.

A potent, selective and cell permeable inhibitor of mitotic kinesin Eg5 with IC50 of 0.8 uM, does not interact with other microtubule motor proteins.

A potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist with Ki of 1.4 nM, 100-fold selectiivity over CRF1.

A potent, selective and oral lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.23 nM, for the treatment of Alzheimer's disease and atherosclerosis..

A potent, selective and orally active adenosine A1 receptor antagonist with Ki of 1.3 nM.

A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively.

NI-42 is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies.