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).

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.

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.

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.

Agonist of sst2, sst3 and sst5 somatostatin receptors

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.

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.

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.

CDD-1281 (CDD1281) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.2 nM and Kiapp value of 8 nM.

XST-20 is a small molecule that selectively targets the DNA-binding domain (DBD) of FOXM1, atranscription factor involved in cell cycle progression, proliferation, and cancer development. Witha surface plasmon resonance (SPR)-derived binding affinity (Kd) of 20 uM, XST-20 effectivelysuppresses FOXM1's transcriptional activities, making it a promising candidate for targetingFOXM1-driven cancers, such as ovarian cancer.

ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα. ODH-08 reduces hepatic collagen deposition and expression levels of fibrogenic markers such as α-smooth muscle actin and collagen type I alpha 1 chain in Western diet-fed mice. ODH-08 suppresses the expression of fibrogenic proteins in hepatic stellate cells (HSCs). ODH-08 suppresses the activity of SMAD2 and 3, which are the primary downstream proteins of transforming growth factor β.

JNJ525 is a small molecule inhibitor that targets tumor necrosis factor alpha (TNFα), a cytokine involved in inflammation and immune regulation. TNFα exerts its biological effects by binding to its receptors, TNFR1 (TNF receptor 1) and TNFR2 (TNF receptor 2). JNJ525 works by preventing the formation of TNFα complexes with these receptors, thereby inhibiting TNFα-mediated signaling pathways.

aNDR1 (NDR1 agonist) is a specific small-molecule agonist of Nuclear Dbf2-related kinase 1 (NDR1, STK38), specifically inhibits CRPC cells and promotes kinase activity of NDR1.

BU99008 is non-radiolabled compound. 11C-BU99008 is a PET Ligand for the imidazoline2 Binding Sites in Rhesus Brain.

NCGC00161856 is identified as the first small-molecule ligand and inverse agonist of the thyroid-stimulating hormone receptor (TSHR). It inhibits basal cAMP production in HEK-EM 293 cells that stably express TSHRs, with a half-maximal inhibitory concentration (IC50) of 3.0 µM. This means that NCGC00161856 effectively reduces the constitutive activity of TSHR, which is the receptor's activity in the absence of its natural ligand (thyroid-stimulating hormone, TSH).

PRLX 93936 is a structural analogue of erastin with potential antineoplastic activity. Erastin analogue PRLX 93936 appears to inhibit mitochondrial outer membrane protein VDACs (voltage-dependent anion channels) 2 and 3, resulting in an oxidative, non-apoptotic cell death. Erastin analogue PRLX 93936 exhibits greater lethality in cell lines harboring mutations in the GTPase protein oncogenes HRAS and KRAS or the serine-threonine protein kinase oncogene BRAF than in non-tumorigenic cell lines. VDACs 2 and 3 are up-regulated in a wide variety of tumor cell lines.

OAT-177 is a potent, selective, orally active acidic mammalian chitinase (AMCase) inhibitor with IC50 of 14 and 19 nM against human and mouse AMCas, respectively, >150-fold selectivity over mCHIT1.

VU 0606170 (also referred to as VU0606170) is a selective inhibitor of the sodium-activated potassium channel KNa1.1, also known as Slack or Slo2.2. This compound has shown specificity for Slack channels over other related potassium channels, making it a valuable tool for studying the physiological and pathological roles of KNa1.1.

MG-002 is a second-generation, orally bioavailable inhibitor of eIF4A, a key RNA helicase involved in the initiation of cap-dependent mRNA translation. By targeting eIF4A, MG-002 effectively disrupts the translation of certain mRNAs, particularly those with complex 5' untranslated regions (UTRs) that are highly dependent on eIF4A activity. This mechanism of action makes MG-002 a promising candidate for targeting cancers and other diseases driven by dysregulated translation.

Novel potent broad-spectrum metallo-β-lactamase (MβL) inhibitor, inhibiting the MβLs NDM-1, VIM-2, ImiS, and L1

Novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupting Warburg metabolism and inducing context-dependent cytostasis in cancer cells