Organometallic Ligands

Ondansetron is a serotonin 5-HT3 receptor antagonist that is used to prevent vomiting and nausea in patients undergoing chemotherapy. This drug blocks the initiation of the vomiting reflex.

Mianserin is a tetracyclic antidepressant drug that has antihistaminic and hypnosedative properties. It is used to treat depression in adults and children, as well as other disorders such as chronic pain and irritable bowel syndrome. This drug’s mechanism of action is not fully understood but is said to block alpha-adrenergic, histamine H1 and serotonin receptors.

Nicardipine is calcium channel blocker drug that is used for the treatment of hypertension and angina. This drug can also be used in the treatment of asthma and is said to enhance the action of various antineoplastic agents.

<p>2-[4-(Piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide is a synthetic small molecule compound, which is a product of advanced medicinal chemistry. This compound is derived from a structured synthesis process focusing on the indazole core, which is known for its bioactive properties. The piperidin-3-yl phenyl moiety is intricately designed to optimize interaction with biological targets.</p>

Naftopidil is an alpha adrenergic antagonist drug that is used to treat urinary symptoms and conditions related to benign prostatic hypertrophy. This drug works to relax smooth muscles by inhibiting alpha adrenergic receptors, thus allowing an improvement in urine flow.

Methotrexate is a chemotherapeutic and immunosuppressive medication, which is a synthetic analog of folic acid. Its source is through chemical synthesis, mimicking the structure of dihydrofolate in order to exert its effects. Methotrexate acts primarily by inhibiting the enzyme dihydrofolate reductase (DHFR), leading to a decrease in tetrahydrofolate production. This disruption in folate metabolism results in the inhibition of DNA, RNA, and protein synthesis, which affects rapidly dividing cells.Methotrexate is employed broadly in clinical oncology as an antineoplastic agent, particularly in the treatment of leukemias, lymphomas, breast cancer, and osteosarcoma. Additionally, it serves as a cornerstone for managing autoimmune diseases such as rheumatoid arthritis and psoriasis, where it helps modulate the aberrant immune response. The dual role of Methotrexate in oncology and immunosuppression underscores its versatility and critical importance in therapeutic regimens. However, its use demands careful monitoring due to potential adverse effects on non-cancerous cells and organ systems, necessitating precise dosage management and patient evaluation.

A potent inhibitor of EGFR with sensitizing and T790M resistance mutations, selective over the wild-type form of the receptor. Causes tumour regression in EGFR mutant T790M transgenic and xenograft models in vivo.

<p>Gardos channel inhibitor</p>

Astemizole is an antihistamine drug used to treat allergy symptoms. This drug is a histamine-1 receptor antagonist and does not cross the blood-brain barrier. Its binding to histamine receptors suppresses flare ups and pruritus.

Atorvastatin is an HMG-CoA reductase inhibitor which is used to lower lipid levels and to reduce the risk of cardiovascular disease. This drug belongs to the class of medicines called statins. It lowers abnormal levels of cholesterol and lipids to reduce the risk of cardiovascular disease by inhibiting the enzyme HMG-CoA.

A 939572 is an inhibitor of stearoyl-CoA desaturase 1 (SCD1). It exhibits anticancer activity as it inhibits cell growth and promotes cell death in human non-small cell lung carcinoma cells.

Bremelanotide is a 7 amino acid peptide that is used to treat hypoactive sexual desire disorder in premenopausal women. This drug is an agonist of many melanocortin receptors. Although, its mechanism is unknown, it is said to increase melanin expression which aids in the regulation of sexual arousal.

Drotaverine is an antispasmodic drug that is used to alleviate gastrointestinal and genitourinary smooth muscle spasms. This drug works by inhibiting phosphodiesterase-4 and increasing levels of cAMP leading to smooth muscle relaxation.

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.

Vanilloid receptor 1 antagonist

<p>Inhibitor of Rho-kinases</p>

<p>A selective inhibitor of MEK5 protein kinase with an IC50 value of 4.3 nM. Blocks transcriptional activation of myocyte-specific enhancer factor 2C (MEF2C). Inhibits phosphorylation of ERK5 protein kinase and thereby reverses inhibition of TNF signaling induced by fluid shear stress in endothelial cells. Induces apoptosis in FLT3-ITD cells.</p>

13:0 Lyso PS is a lysophosphatidylserine, which is a synthetic lipid derivative that serves as a crucial component in biochemical research. It is synthesized from naturally occurring phospholipids, offering a structurally simplified molecule that retains the functional headgroup critical for biological activity. As a single fatty acid chain molecule, its mode of action includes the modulation of cellular processes through interactions with lysophospholipid receptors and participation in signaling pathways. These interactions can influence cell proliferation, apoptosis, or differentiation, depending on the biological context.

<p>Inhibitor of p38 kinase</p>

Estrogen receptor alpha (ERα) agonist