Ligands organométalliques

Nateglinide is used to treat type 2 diabetes mellitus as an oral hypoglycemic, insulinotropic agent. It is a blocker of ATP-dependent potassium channels and works by increasing the body's production of insulin, which lowers blood glucose levels. Nateglinide has been shown to be effective in reducing postprandial blood glucose levels in patients with type 2 diabetes who have not responded well to other treatments. The effects of nateglinide are reversible.

Promethazine is an antihistamine drug that is used to treat allergic conditions, nausea and vomiting. This drug is an antagonist of histamine receptors and NDMA receptors. Antagonism of NDMA receptors help to aid in better sleep and anxiety relief. Additionally, antagonism of histamine receptors aid in preventing nausea and vomiting.

Alarelin is a form of a hypothalamic peptide that is used to treat endometriosis and induce ovulation. It works by stimulating the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland.

Clopidogrel is a potent inhibitor of the platelet aggregation. It reduces blood clotting by inhibiting the ADP receptor on the surface of platelets, thereby inhibiting the aggregation and adhesion of platelets. Clopidogrel has been shown to be effective in preventing thrombosis, myocardial infarction (heart attack), and stroke. Clopidogrel inhibits the activity of cytochrome P450 3A4 (CYP3A4) and p2Y 12 receptors. Clopidogrel has been shown to have synergic effects with nonsteroidal anti-inflammatory drugs (NSAIDs). The polymorphic nature of Clopidogrel can be monitored using a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for quantification in biological samples such as human serum and plasma.

Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.

Inhibitor of VEGF receptor tyrosine kinases and non-receptor tyrosine kinases

Dopamine (D2) receptor antagonist; 5-HT4 serotonin receptor agonist

Antagonist of OX1 orexin receptor

Smoothened agonist and activator of the Hedgehog signalling pathway with EC50 of 3 nM. SAG binds to the Smoothened heptahelical bundle and antagonises effects of the Smoothened antagonist cyclopamine. In previous studies, SAG activated neurogenesis and neuronal survival in cell and animal models as well as improved cell differentiation of human induced pluripotent cells into the neuronal lineage.

HMG-CoA reductase inhibitor; anti-hypercholesterolemia agent

Cyclosporin A (CsA) is a cyclic undecapeptide that is extracted from the fungus Tolypocladium inflatum. CsA is used as an immunosuppressive drug to prevent rejection of transplanted organs and to treat autoimmune diseases such as rheumatoid arthritis and psoriasis. CsA works by binding to a protein called cyclophilin D, which is a component of the enzyme calcineurin. Calcineurin is an important enzyme involved in the activation of immune cells, and by binding to cyclophilin D, CsA inhibits its activity. This leads to the inhibition of T-cell activation and the suppression of the immune response. Cyclosporin A has has been rpeorted to exhibit some nephrotoxicity, hypertension and also increases the risk of infections and tumors when used in transplantation

MK-0812 succinate is a synthetic pharmaceutical compound, which is a product of chemical synthesis with high purity standards suitable for therapeutic use. This compound is synthesized from raw chemical materials using controlled reactions to ensure specific molecular characteristics and potency. MK-0812 succinate functions by inhibiting specific biological pathways that are implicated in disease progression, primarily by binding to target proteins and altering their function. This action results in modulation of cellular processes that contribute to the pathophysiology of certain diseases.

Acitretin is a synthetic retinoid that can be used to treat skin conditions such as acne, psoriasis, and eosinophilic fasciitis. It has been shown to be an active inhibitor of squamous cell carcinoma in the laboratory. Acitretin works by inhibiting the excessive cell growth and keratinisation seen in psoriasis therefore reducing the thickening of the skin, plaque formation and scaling.

Dipeptidyl peptidase-4 inhibitor; anti-diabetic agent

Clemastine is an antihistamine drug that has anticholinergic and sedative effects. It is a selective histamine H1 antagonist and binds to the histamine H1 receptor, blocking the action of endogenous histamine. Clemastine is used in cases of allergy or cold. Also, it has shown to reduce the symptoms of the rhinovirus infection, such as, sneezing and rhinorrhea.

Zoledronic acid is a drug that is used for the treatment of malignancy associated with hypercalcemia and bone metastasis from tumors. This drug induces apoptosis pf hematopoietic tumor cells by inhibiting farnesyl diphosphate. Zoledronic acid is a bisphosphate that inhibits osteoclast function and bone resorption.

HIF prolyl-hydroxylase inhibitor for treatment of anaemia

Eletriptan is a triptan drug used for the treatment of migraines. This drug is an agonist of serotonin receptors, mainly 5-HT 1B/D. It acts to relieve migraines by causing vasoconstriction in intracranial blood vessels.

Inhibitor of Hsp90 chaperone protein; anti-neoplastic

Agonist of glucagon-like peptide GLP1 which is used for treatment of type 2 diabetes mellitus. Exenatide is more resistant to degradation by dipeptidyl peptidase IV than GLP1 and possesses GLP1-like glucoregulatory activities such as stimulation of insulin production by pancreatic β cells and lowering of serum glucagon levels during hyperglycaemia. In a mouse model for type 2 diabetes, exenatide was shown to reverse neuropathy and to possess anxiolytic and anti-depressant-like effects.