A potent, specific inhibitor of the SGK1 kinase activity, induces autophagy, apoptosis and ER stress in cancer cells.

MMV019313 (MMV 019313, MMV-019313) is a potent, specific malaria bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) inhibitor with IC50 of 330 nM; shows no activity against human FPPS or GGPPS (>200 uM); exhibits distinct modes of inhibition compared with bisphosphonates, inhibits P. falciparum growth with EC50 of 268 nM, overexpression and an S228T variant of PfFPPS/GGPPS confer resistance to MMV 019313.

A potent, specific mechanism-based human NAD(P)H: quinone oxidoreductase 1 (NQO1) inhibitor that demonstrates efficient inactivation of NQO1 at 100 nM in in cellular systems.

A potent, specific P-gp inhibitor with Kd of 5.1 nM.

A potent, specific proteasome β5 subunit inhibitor with IC50 of 0.26 uM, 7.3 and 17.3-fold selectivity over β2i and β1i subunit, respecitvely..

A potent, specific RARα agonist with Ki of 2 nM, displays no significant effects on RARγ in reporter based assays..

A potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 3 nM, with no agonistic or antagonistic activities on other S1PRs.

A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.

A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM.

A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM.

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, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.

A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.

A potent, specific, orally bioactive small-molecule inhibitor of ubiquitin-conjugating enzyme UbcH5c with Kd of 283 nM.

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.