A potent and selective small-molecule inhibitor of Lck with IC50 of 147 nM.

A potent and selective tachykinin NK1 receptor antagonist with Ki of 2.9 nM.

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

A potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 34 nM, prevents tissue hyperplasia in the rat urethra or common iliac artery..

NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. IC50 value: 6.8 nMTarget: Cav3.1 T-type channelNNC 55-0396 can be an essential tool in preventing human ovarian cancer cell proliferation as a result of its ability to inhibit the function of T-type Ca2+ channels. It is believed that NNC 55-0396 may functions by dissolving in or passing through the plasma membrane of cells.

A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

A potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.

A potent and selective α4β2 nAChR agonist with Ki of 16 nM.

A potent and selective δ-opioid receptor agonist that has high affinity and selectivity for the δ1 subtype with Ki of 1.12 nM.

A potent and selective, brain penetrant FAAH inhibitor with IC50 of 11 nM.

A potent and selective, CNS penetrant mGlu2 negative allosteric modulator with IC50 of 78 nM.

A potent and selective, CNS penetrant mGlu3 negative allosteric modulator with IC50 of 245 nM.

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 2.4 nM for PDE1B..

A potent and selective, CNS-penetrant PDE1 inhibitor with IC50 of 35 nM for PDE1B..

A potent and selective, non-ATP competitive, allosteric MAPKAPK2/3 (MK2/3) inhibitor with IC50 of 8 nM for MK2, hTNFα EC50 of 0.31 uM.

A potent and selective, orally bioavailable aromatase inhibitor with IC50 of 1.7 nM, 180 times more potent than aminoglutethimide.

A potent and selective, orally bioavailable JAK2 inhibitor with IC50 of 2 nM.

A potent and selective, orally bioavailable, reversible BTK inhibitor with IC50 of 2.8 nM.

A potent and specific antagonist of platelet activating factor (PAF) receptor that inhibits PAF-induced human platelet and neutrophil aggregation in vitro with IC50 of 0.17 and 0.36 uM, respectively.

A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4.