NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.

LSN2463359 is a novel positive allosteric modulators of the mGlu? receptor.

A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM.

Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase. Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.

DY-268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM). It does not display any FXR agonistic activity and cytotoxicity.

GSK854 is a potent Inhibitor of Troponin I-Interacting Kinase (TNNI3K). GSK854 is a suitable lead for identifying new cardiac medicines and have been employed as in vivo tools in investigational studies aimed at defining the role of TNNI3K within heart failure.

A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..

A novel potent, selective and orally active enterocytic microsomal triglyceride transfer protein (MTP) inhibitor that inhibits only MTP localized to enterocytes with IC50 of 6 nM.

CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.

BAY-1797 is a potent and selective P2X4 antagonist.

K-756 is a a selective Wnt/β-catenin pathway inhibitor. K-756 is also a tankyrase (TNKS) inhibitor. K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. could be a leading compound in the development of anticancer agents.

MLS-573151 (MLS000573151) is a selective GTPase Cdc42 inhibitor with an EC50 of 2 μM. MLS-573151 is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to

Ninerafaxstat hifts cellular metabolism from fatty acid oxidation to glucose oxidation.Ninerafaxstat decreases fatty acid oxidation and improve overall mitochondrial respiration.Ninerafaxstat inhibit the growth and proliferation of cancer cells.

Ponatinib, also known as AP24534 is an oral drug for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome–positive (Ph+) acute lymphoblastic leukemia (ALL). It is a multi-targeted tyrosine-kinase inhibitor. Some forms of CML, those that have the T315I mutation, are resistant to current therapies such as imatinib. Ponatinib has been designed to be effective against these types of tumors. Ponatinib was approved in 2012.

Selective inhibitor of ADAMTS-5 (A disintegrin and metalloproteinase with thrombospondin motifs 5 or aggrecanase-2)

HBC620 is an analogue of HBC which is a GFP fluorophore-like synthetic dye that is nonfluorescent in solution, but strongly fluoresces upon forming tight complex with Pepper RNA aptamer. HBC-Pepper complex can be used to visualize RNA dynamics in live cells.

MGV354 is a novel potent, selective soluble Guanylate Cyclase (sGC) activator, lowers intraocular pressure (IOP) in preclinical models of glaucoma..

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior.

Novel Potent Inhibitor of the Protein Phosphatase Slingshot

AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf.

A selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).

A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia.

Ibiglustat (succinate) is a selective inhibitor of glucosylceramide synthase.

ML390 is a human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ML390 bioactivity: ER-HOX-GFP (EC50 μM) = 1.8 ± 0.6; U937 (EC50 μM) = 8.8 ± 0.8; THP-1 (EC50 μM) = 6.5 ± 0.9; DHODH (IC50, μM) = 0.56 ± 0.1. ML390 may offer insight into the mechanism of overcoming differentiation arrest, and will translate into a starting point for a much-needed new and potent treatment for patients with acute myeloid leukemia. Inhibitors of dihydroorotate dehydrogenase (DHODH) showed activity to induce differentiation in multiple animal models of AML in vitro and in vivo. DHODH inhibitors demonstrated effective at prolonging survival in animal models of leukemia.

A selective prostaglandin E receptor subtype 4 (EP4) antagonist with pKi of 8.5.

BIBF-1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR.

ML193 (CID 1261822) is a potent, selective GPR55 antagonist with IC50 of 221 nM, shows >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively.

Novel potent and selective 5-HT2B receptor antagonist

CID1231538, a benzothiazole analogue, is a potent GPR35 antagonist (IC50=0.55 μM). GPR35 is a G protein-coupled receptor (GPCR).

PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).