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

Dovramilast (CC-11050) is a potent and orally active phosphodiesterase 4 (PDE4) inhibitor, CC-11050 is a promising candidate for host directed therapy of patients with pulmonary TB.

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.

Tigulixostat is a novel (indolyl)heteroarylcarboxylate derivatives effective as non-purine selective xanthine oxidase inhibitor, which lowers the production of uric acid.

SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells).

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.

Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM).

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..

Thalidomide-NH-PEG1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

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.

SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.

SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM, respectively.

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.

A endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro.

NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >500

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.

Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.

SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining.

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

Velufenacin is a muscarinic receptor antagonist.

Bersacapavir is a novel Hepatitis B Virus capsid assembly modulator.

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.

GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia.

GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 11.01 ± 2.73 μM).

JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1.

JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16).

RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM.

MMV666810, a 2-aminopyrazine similar to MMV390048, is potent against asexual parasites at 5.94 nM, but against gametocytes, it has a 3.3-fold selectivity to late-stage gametocytes compared to earlier stages (early-stage gametocyte: IC50 603 ± 88 nM; late-stage gametocyte: IC50 179 ± 8 nM).