Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.

A novel potent, selective inhibitor of phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation.

A novel potent, selective KCNQ2/Q3 (Kv7.2/Kv7.3) potassium channel opener/activator with EC50 of 0.38 uM..

A novel potent, selective Sirt2 inhibitor with IC50 of 3.745 uM.

A novel potent, selective, competitive and orally active DPP4 inhibitor with potential for the treatment of type 2 diabetes.

A novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM.

LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.

Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.

A novel potent, specific TOPK inhibitor that has no effect on ERK1, JNK1, or p38 kinase activity.

A novel prodrug S1P receptor modulator lacking S1P3 receptor agonism to avoid bradycardia associated with fingolimod and other S1P receptor modulators.

A novel protein kinase affinity probe...

SLMP53-1 is a novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells.

A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src.

A novel selective, orally available fungal CYP51 (lanosterol 14-α-demethylase) inhibitor.

AKI-603 is a novel small molecule Aurora A kinase inhibitor with IC50 of 12.3 nM, also inhibits Aurora B kinase activity to a less extent; disrupts normal spindle structure, and induces cell-cycle arrest; t; suppresses stem cell properties in breast cancer cells, and also suppresses the expression of self-renewal genes (β-catenin, c-Myc, Sox2, and Oct4); reduces xenograft tumor growth after intragastric administration.

JP-153 (JP153) is a novel small molecule targets the Src-FAK-Paxillin signaling, inhibits Src-dependent phosphorylation of paxillin (Y118) and downstream activation of Akt (S473) in RECs; potently inhibits VEGF-induced proliferation and migration, inhibits retinal neovascularization in the murine oxygen-induced retinopathy model.

CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells.

A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM.

A novel stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].

A novel VPS34 inhibitor.

A novel, highly potent positive modulator of Kv7 channels with EC50 of 100 nM (Kv7.2-Kv7.5).