A potent, specific, cell-active NADPH oxidase1 (Nox1) inhibitor that strongly blocks ROS generation in HT29 cells with IC50 of 0.129 uM.

A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM

A potent, specific, irreversible NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 16.65 nM.

A potent, specific, orally active melanin concentrating hormone receptor 1 (MCHR1) inhibitor with kI of 3.8 nM, >100-fold selectivity over a battery of GPCRs, ion channels and enzymes.

A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

A potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM.

Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability.

A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively).

A potent, state-dependent blocker of Cav2 channels that preferentially inhibits potassium-triggered calcium influx through recombinant Cav2.2 under depolarized conditions with IC50 of 0.27 uM, compared with hyperpolarized conditions (IC50>20 uM).

A potent, subtype-selective Grp94 inhibitor with Kd of 0.96 uM, 13-fold selectivity over Hsp90α.

A potent, subtype-selective mGluR5 negative allosteric modulator with Ki of 6.1 nM.

NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.

A PP1 analog that has greater selectivity and potency for Zap-70(AS) over wild-type Zap-70, as assessed by Erk and Lat phosphorylation, as well as by proliferative responses of mature CD4+ cells.

A proton pump inhibitor that inhibits gastric acid secretion.

A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells.

A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells.

A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells.

A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells.

A PSMA (prostate-​specific membrane antigen) ligand-​tubulysin compound..

A pungent agent isolated from Zingiber officinale Roscoe, has been known to have anti-tumor and anti-inflammatory effects.

A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS.

A quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine.