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).

PDD 00017273 is the first-in-class, selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with Kd, biochemical EC50 of 1.45 nM, 26 nM.

A xanthone derivative that fuctions as an EP and DP receptor antagonist.

BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively.

MMV390048 is a novel potent Plasmodium PI4K inhibitor with IC50 of 28 nM against intraerythrocytic life cycle stages of P. falciparum (NF54 drug-sensitive strain).

PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells.

GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.

Bruton tyrosine kinase inhibitor

TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics

NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.

LIT-001 trifluoroacetate (LIT001) is the first nonpeptide Oxytocin receptor (OT-R) agonist with EC50 of 55 nM, Emax=96%.

Second generation papaverine analog, acting as an anticholinergic agent