Runcaciguat is a potent soluble guanylyl cyclase (sGC) stimulator/activator..

Inaxaplin is an apolipoprotein L1 (APOL1) function inhibitor (WO2020131807, compound 2). Inaxaplin can be used for the research of kidney disease.

NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 µM and a Kd of 54.8 nM[1].

DNDI-6148 acts principally through the inhibition of Leishmania cleavage and polyadenylation specificity factor (CPSF3) endonuclease for the treatment of visceral leishmaniasis (VL).

MK-4688 is an efficient inhibitor of the HDM2-p53 protein-protein interaction.

Carcainium chloride (QX 572) is a quaternary derivative of the local anesthetic Lidocaine. Antitussive effect.

ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) .

NPT200-11 is an orally bioavailable and brain penetrating alpha-synuclein (ASYN) misfolding and aggregation inhibitor.

.Valemetostat is an antineoplastic agent.

Lepidiline C shows cytotoxic activity against HL-60 cells with an IC50 of 27.7 μM.

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines[1]. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli[2].

α-Lapachone shows trypanocidal activity[1].

MM-3122 is a selective inhibitor of host cell serine protease TMPRSS2 (transmembrane protease serine 2) with IC50 of 0.34 nM against recombinant full-length TMPRSS2 protein.

MS9715 (MS-9715) is a NSD3-targeting PROTAC designed by linking BI-9321, a NSD3 antagonist, which binds NSD3's PWWP1 domain, with an E3 ligase VHL ligand.MS9715 achieves effective and specific targeting of NSD3 and associated cMyc node in tumor cells.MS9715 effectively suppresses growth of NSD3-dependent hematological cancer cells.MS 9715 effectively suppresses NSD3-and cMyc-associated gene expression programs, resembling effects of the CRISPR-Cas9-mediated knockout of NSD3.

Siponimod, also known as BAF-312, is a a potent and orally selective S1P Receptor Modulator with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively. Development of sphingosine-1-phosphate receptor 1 (S1P1) modulators to dampen inflammation and its sequelae is becoming increasingly promising for treating medical conditions characterized by significant immunopathology.

4-CPPC is the first reversible and selective inhibitor of pro-inflammatory protein macrophage migration inhibitory factor-2 (MIF-2) with Ki of 33 uM, 13-fold selectivity for human MIF-2 versus human MIF-1.

6-Thioguanosine (6-Mercaptoguanosine), an active nucleoside, is an Azathioprine metabolite. 6-Thioguanosine has immunosuppressive effects.

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

ALB-127158A, also known as ALB-127158(a), is a MCH1 antagonist for the treatment of obesity.

Alpha-Lipoic Acid Choline Ester, also known as alpha-LACE, EV-06 or UNR844, is a drug candidate potentially for the treatment of presbyopia. Alpha-LACE was designed to permeate biological membranes with the incorporation of the cationic choline head grou

AVP-786 is a novel, next-generation investigational drug product consisting of a combination of deudextromethorphan, and an ultra-low dose of quinidine.

BAY-1816032 (BAY1816032) is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM, displays excellent selectivity on a panel of 395 kinases.

Ciraparantag(PER977) is an intravenously administered anticoagulant Reversal Agent.

Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.

DL-AP4 is a Broad spectrum EAA antagonist.

ENOblock Hcl(AP-III-a4 Hcl) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.

GSK199 is a reversible inhibitor of PAD4 (IC50 = 200 nM) that binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3.

KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2.

LEI110 (LEI－110) is a potent Phospholipase A2 group XVI (PLA2G16) inhibitor with Ki of 20 nM, also has activity on HRASLS2, RARRES3 and iNAT (pIC50=6.8-7.6).

Lifitegrast sodium, also known as SAR-1118, is an LFA-1 antagonist intended for the treatment of vascular complications of the eye.