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 active lysine methyltransferase SMYD2 inhibitor with IC50 of 2.8 nM.

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 competitive CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with pKi of 8.92.

A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.

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.

A potent, selective and orally active Chk1 inhibitor.

A potent, selective and orally active COX-2 inhibitor with IC50 of 26 nM for inhibition of the COX-2-dependent production of PGE2 in human osteosarcoma cells.

A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors.

A potent, selective and orally active CRF1 receptor antagonist with Ki of 12 nM, shows no affinity for CRF2 receptor (Ki>10 uM).

A potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM.

A potent, selective and orally active human neutrophil elastase (HNE) inhibitor with Ki of 12 nM.

A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.

A potent, selective and orally active SGLT2 inhibitor with IC50 of 8.9 nM, 280-fold selectivity over SGLT1.

A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. Migraine.

A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM.

A potent, selective and orally available inhibitor of delta-5 desaturase (D5D) with Ki of <2.7 nM and IC50 of 19 nM, with excellent selectivity over D6D and SCD.