Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis.

K306 is a small molecule agonist that specifically targets SH2-containing 5' inositol phosphatase 1 (SHIP1), an enzyme involved in regulating cellular signaling pathways. SHIP1 is a lipid phosphatase that hydrolyzes the 5' phosphate of phosphatidylinositol-3,4,5-trisphosphate (PIP3), converting it to phosphatidylinositol-3,4-bisphosphate (PI(3,4)P2). This activity modulates the PI3K (phosphoinositide 3-kinase) signaling pathway, which is critical for cell survival, proliferation, and immune responses.

Savirin (S. aureus virulence inhibitor) is a small molecule that targets the agr (accessory gene regulator) quorum sensing system in Staphylococcus aureus (S. aureus). The agr system is a key regulatory pathway that controls the expression of virulence factors in S. aureus, which are critical for its pathogenicity. The system involves a two-component signal transduction pathway consisting of AgrC (a histidine kinase) and AgrA (a response regulator).

Hydrangetin is a bioactive compound that has been identified as having antiplatelet aggregation properties, meaning it can help prevent blood clots by inhibiting the clumping together of platelets. This compound can be isolated from Zanthoxylum schinifolium, a plant commonly known as the Sichuan pepper or Korean pepper, which is used in traditional medicine and culinary practices in East Asia.

Ricinine is a pyridine alkaloid found in the seeds and leaves of the castor oil plant (Ricinus communis). While Ricinus communis is primarily known for producing ricin, a highly toxic protein, ricinine itself is a less toxic compound and has been studied for its potential pharmacological properties, including hepatoprotective effects.

Oxypalmatine is a bioactive alkaloid compound isolated from Phellodendron amurense, a plant commonly known as Amur cork tree. Phellodendron amurense is a traditional medicinal plant widely used in East Asian medicine, particularly in China, Japan, and Korea, for its anti-inflammatory, antimicrobial, and antipyretic properties. Oxypalmatine is one of the many alkaloids found in this plant, contributing to its pharmacological effects.

N-Desmethyl Galanthamine is indeed a metabolite of Galanthamine, a well-known acetylcholinesterase (AChE) inhibitor. Galanthamine is a natural alkaloid originally derived from plants such as Galanthus (snowdrop) and is widely used in the treatment of Alzheimer's disease and other cognitive disorders due to its ability to enhance cholinergic neurotransmission.

Ethacizine hydrochloride (Ethacizin; NIK-244) is a Class Ic antiarrhythmic agent, which means it is part of a group of drugs that primarily act by blocking sodium channels in the heart. This class of antiarrhythmic agents is known for their potent effects on slowing conduction in the heart, particularly in the atria, ventricles, and the His-Purkinje system.

AZD2461 is indeed a novel poly (ADP-ribose) polymerase (PARP) inhibitor that has been investigated for its potential to overcome resistance mechanisms associated with other PARP inhibitors, such as Olaparib. One of the key resistance mechanisms to Olaparib is mediated by P-glycoprotein (Pgp), an efflux pump that can reduce intracellular concentrations of the drug, thereby diminishing its efficacy.

AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.

Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4

Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.

GSDMD agonist DMB is a direct and selective gasdermin D (GSDMD) agonist, activates GSDMD pore formation to trigger liposome leakage with EC50 of 0.7 uM, activates GSDMD pore formation and pyroptosis without cleaving GSDMD. DMB directly binds to GSDMD by microscale thermophoresis (MST) with a dissociation constant (KD) of 1.1 uM. DMB induces pyroptosis in immortalized and primary cells in a GSDMD-dependent and cleavage-independent manner. DMB binds to GSDMD and induces cleavage-independent GSDMD oligomerization and pore formation. activated human GSDMD but not other human gasdermins, also activates mouse GSDMD in the liposome leakage assay, albeit with ∼5-fold reduced efficacy. GSDMD agonist DMB modifies GSDMD at C191, which is conserved in GSDMD from different species but not in other gasdermin family members. DMB induces tumor regression and enhances antitumor immunity that depends on GSDMD expression in the tumor.

Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo.

Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.

Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.

Ganirelix acetate is an antagonist of GnRH that competitively antagonizes the gonadotropic GnRH receptor, thereby mutating the pathway and causing rapid and reversible inhibition of gonadotropin (luteinizing hormone LH and follicle stimulating hormone FSH) secretion. Ganirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion. The suppression of pituitary LH secretion by Ganirelix Acetate is more pronounced than that of FSH.

Agonist of sst2, sst3 and sst5 somatostatin receptors

Somatostatin is a tetradecapeptide which can suppress the growth hormone (GH) secretion and control the pituitary hormone secretion in human CNS.

Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation. Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation. It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma). Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention.

Terlipressin is a potent vasoconstrictor that acts via V1 receptors on arteriolar smooth muscle cells. Terlipressin can result in splanchnic vasoconstriction augmenting systemic arterial blood pressure with beneficial circulatory and renal effects that would be expected to also ameliorate the key pathophysiological changes responsible for the development of refractory ascites

Teriparatide Free Base is a biologically active form of teriparatide, a recombinant human parathyroid hormone (PTH) analogue. It is used to treat osteoporosis in both men and postmenopausal women who are at high risk of fractures. Teriparatide works differently from most other osteoporosis medications, as it stimulates bone formation rather than just slowing bone loss.

LY3437943 is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). LY3437943 inhibits for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. LY3437943 can be used for the research of obesity.

An immunoactive peptide that has been shown to inhibit cell proliferation and induce apoptosis in human leukemia, non-small cell lung cancer, melanoma, and other human cancers.

Carbetocin (marketed under brand names such as Lonactene and Duratocin) is a synthetic analogue of oxytocin, specifically designed for use in obstetrics to prevent and manage postpartum hemorrhage (PPH), a leading cause of maternal mortality worldwide. It is a long-acting agonist of peripheral oxytocin receptors, making it highly effective in inducing uterine contractions and reducing bleeding after childbirth.

Cetrorelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist. Cetrorelix inhibits the endogenous luteinizing hormone surge during ovarian stimulation. Cetrorelix reduces cyclophosphamide induced ovarian follicular destruction in mice.

A peptide hormone and neuropeptide that is released into the bloodstream as a hormone in response to stretching of the cervix and uterus during labor and with stimulation of the nipples from breastfeeding.

Atosiban (RW22164; RWJ22164) is indeed a nonapeptide and a competitive antagonist of the vasopressin and oxytocin receptors. It is structurally similar to oxytocin but lacks the amino group at the N-terminus, making it a desamino-oxytocin analogue. Atosiban is primarily used as a tocolytic agent, which means it helps to inhibit premature labor by blocking the action of oxytocin on the uterus. This makes it particularly valuable in the management of spontaneous preterm labor, as it can help delay delivery, providing critical time for administering corticosteroids to enhance fetal lung maturity or for transferring the mother to a facility with appropriate neonatal care.

CMP05-7 (Endosomolytic compound CMP05-7) is a novel endosomolytic small-molecule compound that exhibits higher transfection efficiency/ability to induce endosomal escape of oligonucleotides (ONs) than current compounds such as chloroquine.