mCLB073 is an advanced, orally active small molecule agonist specifically designed to target Mtb adenylyl cyclase Rv1625c. As an optimized derivative of V-59, it demonstrates significantly enhanced potency and efficacy for in vivo applications. In cholesterol-based media, mCLB073 shows a remarkable 17-fold increase in activity against Mtb compared to its predecessor, V-59, while retaining favorable pharmacokinetic characteristics and a strong safety profile. In preclinical studies, oral administration of mCLB073 at 30 mg/kg led to a substantial reduction in Mtb colony-forming units (CFUs) in the lungs of mice, accompanied by a 45% decrease in lung pathology severity. These findings highlight its potential as a promising therapeutic candidate for tuberculosis treatment.

PIM1-IN-2 is a highly effective and ATP-competitive inhibitor of Pim-1, demonstrating a Ki value of 91 nM. Unlike traditional inhibitors, it interacts with the ATP-binding kinase hinge region without relying on the formation of standard hydrogen bonds, showcasing a unique mechanism of action. This distinctive approach highlights its potential as a promising therapeutic agent.

ATV006 is a potent, orally active antiviral agent and ester prodrugs of GS-441524. ATV006 inhibits the replication of SARS-CoV-2 and its variants. ATV006 can be used for SARS-CoV-2 research.

Sphingosine-1-phosphate (S1P) functions as a versatile signaling molecule, acting both intracellularly and extracellularly. Within cells, it serves as a secondary messenger, playing a key role in calcium ion (Ca²⁺) mobilization. Externally, S1P acts as a ligand, binding to and activating a range of G protein-coupled receptors, including S1P1-5 receptors as well as GPR3, GPR6, and GPR12. This bioactive lipid is synthesized from sphingomyelin and other membrane phospholipids, highlighting its importance as a critical mediator in various cellular processes.

N-β-alanyldopamine hydrochloride, commonly referred to as NBAD hydrochloride, stands as the primary dopamine derivative found in haemolymph.

Alagebrium Chloride, identified as ALT711, emerged as a pioneering pharmaceutical candidate developed by Alteon, Inc. It marked the first clinical attempt to address the crosslinks formed by advanced glycation endproducts (AGEs), a key factor in the aging process. By targeting and disrupting these crosslinks, Alagebrium aims to counteract the stiffening of blood vessel walls, a condition linked to hypertension, cardiovascular disorders, and various age-related degenerative issues caused by protein crosslinking. Clinical studies have demonstrated its efficacy in lowering systolic blood pressure and offering therapeutic advantages for individuals with diastolic dysfunction.

Pemvidutide is a dual agonist targeting both GLP-1R and GCGR, demonstrating significant efficacy in reducing body weight, liver fat content, and serum lipid levels. Its unique mechanism of action makes it a promising candidate for research and therapeutic development in conditions such as non-alcoholic steatohepatitis (NASH) and obesity. This innovative compound offers potential for addressing complex metabolic disorders with a multifaceted approach.

JNJ-28583113 (JNJ28583113) a potent, selective, brain penetrant TRPM2 antagonist with IC50 of 126 nM (hTRPM2).JNJ-28583113 shows similar potency against species chimpanzee and rat TRPM2 with IC50 of 100 and 25 nM, respectively.JNJ-28583113 shows no significant (IC50>10 uM) reactivity towards PARP or PARG and a panel for multiple known kinases GPCRs and ion channels, nine other TRP channels with exception of TRPM5 (IC50<1 uM).Blocking TRPM2 via JNJ-28583113 caused phosphorylation of GSK3α and β subunits in cell assays.JNJ-28583113 also protected cells from oxidative stress induced cell death as well as morphological changes induced by non-cytotoxic concentrations of H2O2。JNJ-28583113 blunted cytokine release in response to pro-inflammatory stimuli in microglia.JNJ-28583113 was brain penetrant but not suitable for systemic dosing as it was rapidly metabolized in vivo, but the in-vitro pharmacology of JNJ-28583113 is the best in class.

Idoxuridine is an anti-herpesvirus antiviral and anticancer drug. It is a nucleoside analogue, a modified form of deoxyuridine, similar enough to be incorporated into viral DNA replication, but the iodine atom added to the uracil component blocks base pairing. It is used only topically due to cardiotoxicity. It was synthesized by William Prusoff in the late 1950s. Initially developed as an anticancer drug, idoxuridine became the first antiviral agent in 1962.

Pinostrobin is a flavonoid with diverse biological activities, including antioxidant, anti-inflammatory, and anticancer properties. Pinostrobin is a dietary bioflavonoid discovered more than 6 decades ago in the heart-wood of pine (Pinus strobus). Pinostrobin has depicted many pharmacological activities including anti-viral, anti-oxidant, anti-leukaemic, anti-inflammatory and anti-aromatase activities. It is an inhibitor of sodium channel and Ca(2+) signalling pathways and also inhibits intestinal smooth muscle contractions.

Pinocembrin, also known as DL-0108, is an androgen receptor ligand potentially for the treatment of acute stroke.

Sunvozertinib is a potent inhibitor targeting the ErbB family of receptor tyrosine kinases, including EGFR (Epidermal Growth Factor Receptor) and Her2 (Human Epidermal Growth Factor Receptor 2), as well as BTK (Bruton's Tyrosine Kinase). It exhibits particularly strong activity against mutant forms of these kinases, which are often associated with resistance to existing therapies in cancers such as non-small cell lung cancer (NSCLC). The IC50 values (half-maximal inhibitory concentr.

ML316 is a specific antifungal agent that fungal-selectively inhibits the mitochondrial phosphate carrier Mir1, exhibits potent antifungal activity against the moderatelyazole-resistant C. albicans strain CaCi-2 with MIC of 0.05 ug/ml.

NCI-65828 (designated as N 65828，NSC-65828) is a small-molecule inhibitor targeting angiogenin (ANG), a protein critical for angiogenesis and cellular proliferation. Its therapeutic potential stems from selective suppression of ANG's ribonucleolytic function, a biochemical activity essential for mediating downstream biological effects. By disrupting ANG's enzymatic capacity to cleave RNA substrates, NCI-65828 attenuates the protein's pro-angiogenic signaling pathways. Preclinical evaluations highlight its multifaceted antitumor properties. In vitro studies using diverse cancer cell models—including bladder carcinoma (T24; IC₅₀ = 1.3 ± 0.5 μM), cervical adenocarcinoma (HeLa; IC₅₀ = 1.9 ± 0.4 μM), and urothelial carcinoma (UROtsa; IC₅₀ = 3.2 ± 0.8 μM)—demonstrate dose-dependent antiproliferative effects, with potency variations reflecting tissue-specific sensitivity. Parallel experiments in human umbilical vein endothelial cells (HUVECs) reveal significant inhibition of capillary-like tube formation, confirming its antiangiogenic efficacy in disrupting endothelial morphogenesis. Notably, in vivo investigations using transgenic murine models demonstrate that NCI-65828 effectively suppresses the development of prostatic intraepithelial neoplasia (PIN) lesions. Mechanistic analysis indicates this activity arises from direct enzymatic inhibition rather than interference with ANG's intracellular trafficking, as nuclear translocation remains unaffected—a distinguishing feature that differentiates it from other ANG-targeted agents. This selective mode of action positions NCI-65828 as a precision tool for studying ANG-dependent pathologies.

5β-Cholanic acid can be used for 5β-Cholanic acid derivatives synthesis.

PF-04965842 is a selective Janus kinase 1 (JAK1) inhibitor, demonstrating potent activity against JAK1 with an IC50 of 29 nM. Its selectivity is evident from its significantly higher IC50 values for other JAK family members: 803 nM for JAK2, > 10,000 nM for JAK3, and 1,250 nM for TYK2. This selectivity profile suggests that PF-04965842 preferentially targets JAK1 over other JAK isoforms, which could be advantageous in reducing off-target effects and improving therapeutic outcomes in conditions where JAK1 signaling is implicated.

RapiFluor-MS can be used a marker for LC-MS/MS analysis of N-glycans, which provides the highest MS signal enhancement for neutral glycans.

AICP is a highly potent and selective GluN2C-containing NMDA receptor agonist that specifically targets the glycine-binding site of these receptors. It exhibits an EC50 of 1.7 nM at GluN1/GluN2C NMDA receptors, making it a powerful tool for studying the functional roles of GluN2C-containing NMDA receptors in the central nervous system.

UT-59 is a specific inhibitor that targets the cholesterol-sensing membrane protein Scap (SREBP cleavage-activating protein). It functions by binding to Scap's cholesterol-binding site, which prevents Scap from interacting with SREBPs (sterol regulatory element-binding proteins). This inhibition blocks the activation of SREBPs, which are key transcription factors involved in lipid and cholesterol biosynthesis. As a result, UT-59 effectively suppresses lipid synthesis, making it a potential therapeutic candidate for conditions associated with dysregulated lipid metabolism, such as hyperlipidemia, atherosclerosis, or metabolic disorders.

Bexin-1 is a specific inhibitor that targets Munc13-4, a protein critical for regulated exocytosis, particularly in secretory cells such as immune cells (e.g., cytotoxic T lymphocytes, mast cells) and neuroendocrine cells. Munc13-4 plays a key role in vesicle priming and fusion with the plasma membrane, a process essential for the release of secretory granules containing hormones, neurotransmitters, or immune mediators.

Eucatropine is a synthetic anticholinergic agent that acts as a potent inhibitor of muscarinic acetylcholine receptors (mAChRs). These receptors are part of the parasympathetic nervous system and play a key role in mediating the effects of acetylcholine, a neurotransmitter involved in various physiological processes such as smooth muscle contraction, glandular secretion, and heart rate regulation.

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).

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.

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

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