Organometallic Ligands

<p>Inhibits aromatic amino acid decarboxylase</p>

<p>Agonist of A3 adenosine receptor; antineoplastic</p>

<p>Inhibitor of DNA topoisomerase I</p>

<p>Spla2-X Inhibitor 31 is a chemical inhibitor specifically targeting the human secreted phospholipase A2 group X (sPLA2-X), which is derived synthetically through chemical synthesis. Its mode of action involves binding to the active site of sPLA2-X, effectively blocking its enzymatic activity. This enzyme catalyzes the hydrolysis of phospholipids, leading to the release of arachidonic acid, a precursor for bioactive lipids involved in inflammation and other cellular processes.</p>

<p>Inhibitor of prolyl 4-hydroxylase PHD</p>

<p>A potent and selective covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4). This receptor tyrosine kinase activates an oncogenic driver in hepatocellular carcinoma, the fibroblast growth factor 19 (FGF19). The FGFR4 inhibitor is therefore a promising candidate for the treatment of advanced liver cancer.</p>

<p>Histamine (H1) receptor antagonist; anti-ulcer agent</p>

<p>Bupropion is an antidepressant drug that has been used in treatment trials for major depressive disorder. It has been shown to be effective in combination therapy with other drugs, such as a serotonin reuptake inhibitor (SSRI) or a tricyclic antidepressant (TCA). The drug's mechanism of action is not well understood but is said to increase the levels of dopamine and norepinephrine by inhibiting their reuptake.</p>

<p>Amlexanox is an antiallergic and anti-inflammatory drug that has been shown to be effective in treating rhinitis and allergic asthma in clinical studies. It prevents the slow-reacting substance of anaphylaxis (SRS-A) from being released chemically as a mediator and may have antagonistic effects on interleukin-3.</p>

<p>Inhibits c-MET tyrosine kinases</p>

<p>WIN 64338 hydrochloride is a bradykinin receptor antagonist that inhibits the action of bradykinin, an inflammatory and pain-causing agent.  It also blocks the binding of bradykinin to its receptors, thereby preventing their activation which causes inflammation and pain.  The affinity values for WIN 64338 hydrochloride at the bradykinin B2 receptor are more than 1000 times greater than those at the bradykinin B1 receptor.</p>

<p>Activates muscarinic GPCR DREADDs, which are unaffected by the endogenous ligand acetycholamine of the parent receptor. Clozapine is metabolized to clozapine N oxide in the liver, mainly by CYP3A4. Has anti-seizure effects, when induced by chemoconvulsants pilocarpine and picrotoxin.</p>

<p>Inhibitor of Factor Xa; anti-thrombotic</p>

<p>Glimepiride is a sulfonylurea drug that is used in the treatment of type 2 diabetes mellitus. This drug works by inhibiting ATP-sensitive potassium channels by binding non-specifically to the B sites of both sulfonylurea receptor-1 (SUR1) and sulfonylurea receptor-2A (SUR2A) subunits. As a result, this promotes insulin secretion from beta cells.</p>

<p>This compound is a novel negative allosteric modulator of glutamate metabotropic receptor mGlu7. It is highly selective for mGlu7 over other receptors of mGlu class with IC50 = 795 nM. Although VU 6010608 showed favourable brain penetration in rats, it has been proposed as an in vitro tool for electrophysiology studies. The mGlu7 is broadly distributed within the mammalian central nervous system and it plays a key role in neuronal function and synaptic plasticity.</p>

<p>Dual IGF-1R and InsR kinase inhibitor; antineoplastic</p>

<p>Inhibitor of isocitrate dehydrogenase 2</p>

<p>Inhibits proto-oncogene Pim kinases (Pim-1, Pim-2 and Pim-3); antineoplastic</p>

<p>Lovastatin is an HMG-CoA reductase inhibitor that is used to lower LDL cholesterol levels and to aid in the management of cardiovascular diseases. Animal studies have demonstrated that this drug has vasculoprotective properties.</p>

<p>Duloxetine is a serotonin and norepinephrine reuptake inhibitor drug that is used to treat anxiety, pain, osteoarthritis and stress incontinence. This drug inhibits the reuptake of the neurotransmitters serotonin and norepinephrine so that there are increased levels of them in the synaptic cleft.</p>