Ligands organométalliques

VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic

Inhibitor of VEGFR, PDGR, c-Kit and Ret; inhibitor of angiogenesis

<p>Positive allosteric modulator of the metabotropic glutamate receptor mGluR5 with EC50 in submicromolar range. The compound is able to increase mGluR5 function in vitro and in vivo. A study showed that ADX-47273 enhanced fear extinction learning as well as improved reversal learning in experimental animals.</p>

Inhibits p38 MAP kinase; anti-inflammatory; neuroprotective

Lumiracoxib is a COX-2 selective non-steroidal anti-inflammatory drug that is used for the treatment of osteoarthritis. This drug inhibits prostaglandin synthesis via inhibition of COX-2.

<p>A reversible inhibitor of IGF-1R kinase and insulin receptor. Has anti-growth effects in mesenchymal, epithelial and hematopoietic tumor types. Synergistic with other cytotoxic, hormonal and targeted anti-cancer therapy.</p>

<p>3-Hydroxy-5-{[(naphthalen-2-yl)carbamoyl]amino}benzoic acid is a synthetic compound characterized by its complex molecular structure incorporating naphthalene and benzoic acid moieties. As a derivative of benzoic acid, it is typically synthesized through a series of chemical reactions designed to introduce the 3-hydroxy and carbamoyl functional groups, creating a compound with potentially unique bioactive properties.</p>

<p>Inhibitor of leucine-rich repeat kinase LRRK2Â</p>

Potent and selective positive allosteric modulator (PAM) of metabotropic glutamate receptor mGlu4. Valiglurax is orally bioavailable and CNS-penetrant mGlu4 PAM in preclinical development for the Parkinson’s disease therapy and alleviation of the motor symptoms.

<p>Cetirizine is a selective histamine-1 antagonist drug used for the treatment of allergies. One of the common uses is for a condition called allergic rhinitis. As Cetirizine is an antihistamine, its main mode of action is by selectively inhibiting H1 receptors. In vivo and ex vivo animal models have shown insignificant anticholinergic and antiserotonergic effects.</p>

<p>Crizotinib is a drug that belongs to the group of tyrosine kinase inhibitors. It is used in the treatment of cancers, including non-small cell lung cancer, small cell lung cancer, and other types of solid tumours. Crizotinib inhibits the activity of the tyrosine kinase ALK or anaplastic lymphoma kinase, which is involved in many signalling pathways and biological processes. The inhibition of this enzyme leads to decreased energy metabolism, reduced mitochondrial membrane potential and increased susceptibility to apoptosis.</p>

Inhibitor of NLRP3 inflammasome and suppressor of the inflammatory cytokine IL-1β secretion. The compound was tested in diabetic mice and was shown to decrease the incidence of cardiac arrythmias, which are common secondary complications in diabetes mellitus. MCC 950 has potential to reverse diabetes-induced pathologies in cardiac electrophysiology.

<p>Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).</p>

<p>Thioglycosyl Naphthalimide is a highly potent human O-GlcNAcase (hOGA) inhibitor with good selectivity against human β-N-acetylhexosaminidase B (HsHexB).</p>

Inhibits N-Acetyl-mediated interaction between BE2M (E2 conjugating enzyme) and DCN1 (a component of E3 ligase complex). Also has inhibitory action on DCN2 and NEDD8 ubiquitin-like protein. Reduces anchorage-independent growth in DCN1-amplified cell line.

<p>Inhibitor of human neutrophil elastase</p>

<p>Bosentan is a dual endothelin receptor antagonist that is used to treat hypertension. This drug works by blocking the action of endothelin molecules which prevents the narrowing of blood vessels and decreases blood pressure.</p>

Potent inhibitor of γ-secretase. LY 411575 inhibited production of amyloid β (Aβ) peptides with IC50 of 0.078 nM in vitro as well as decreased levels of Aβ40 and Aβ42 amyloids in brain of a mouse model for Alzheimer’s disease. In vitro studies confirmed that LY 411575 inhibited cleavage of Notch receptor at S3 site with IC50 of 0.39 nM, which blocked Notch activation and downstream signalling, leading to apoptosis in primary and immortalized Kaposi's sarcoma cells.

<p>Regaloside D is a natural product derived from plant sources, specifically isolated from certain species known for their bioactive properties. It functions as a glycoside, a compound in which a sugar is bound to a non-carbohydrate moiety, potentially influencing a variety of cellular processes through its interaction with specific molecular targets.</p>

Agonist of hypothalamic neuropeptide LHRH