Selective non-peptide vasopressin V2 receptor antagonist

Novel inhibitor of salmonella serine acetyltransferase (SAT), the enzyme that catalyzes the rate-limiting step of L-cysteine biosynthesis

Inhibitor of H274Y and N294S mutants

Subtype-selective α4β2 nicotinic acetylcholine receptor partial agonist

PPARγ covalent ligand

Novel reversible covalent inhibitor of the cyclin-dependent kinase 5 (Cdk5)-mediated phosphorylation of PPARγ at Ser245, a key factor in the insulin-sensitizing effect of PPARγ-targeted drugs

Novel neuroprotective agent, suppressing abnormal tau protein aggregation

Selective, active-site-directed 14 kDa PLA2 inhibitor, totally inhibiting LT and PAF formation, while prostanoid formation was not altered

Dual ETA and ETB receptor antagonist

Potent, specific inhibitor of human p38 mitogen-activated protein (MAP) kinase

Potent and selective agonist for the human ß3-adrenoceptor

Inhibitor of p38 MAPK

Selective 5-HT2C_receptor>5-HT2C inverse agonist

Selective 5-HT7 receptor antagonist

Novel selective mTOR inhibitor

Nonpeptidic antagonist of alpha(v)beta3 and alpha(v)beta5 integrins, reducing angiogenesis and VEGF expression

Selective dopamine D3 receptor antagonist

Selective p38a kinase inhibitor, inhibiting Brd4

AntiMycobacterium tuberculosis agent

Novel TRPV4 blocker

Potent and selective dopamine D3 receptor antagonist

Novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor

Novel CXCR2 selective antagonist, inhibiting ex vivo neutrophil activation and ozone-induced airway inflammation in humans

Novel inhibitor of mitogen and Stress-Activated Kinases 1 (MSK1)

Novel Rho kinase inhibitor

Potent non-cytotoxic inhinitor of Mycobacterium tuberculosis H37Rv

Novel cAMP-independent potentiator of CFTR, synergistically restoring CFTR function

Novel cAMP-independent potentiator of CFTR, synergistically restoring CFTR function

Membrane-permeant, fluorescent, selective Na+ indicator dye

Novel potentiator of metabotropic glutamate receptors for use against neurological and psychiatric disorders

Novel potentiator of metabotropic glutamate receptors for use against neurological and psychiatric disorders

Novel inhibitor of Quiescin Sulfhydryl Oxidase 1 (QSOX1), suppresses tumor cell growth in a Matrigel-based spheroid assay and inhibits invasion in a modified Boyden chamber, but does not affect viability of non-malignant cells

Inhibitor of S100B which selectively kills melanoma; Amoebicidal diamidine

Novel Smac mimetic, demonstrating potent cell-killing effects in several subtypes of breast, ovarian, and prostate cancer cell lines but only when the DR ligand TRAIL or another such apoptosis inducer is co-administered

Novel obatoclax derivative, inducing apoptosis in hepatocellular carcinoma cells through SHP-1-dependent STAT3 inactivation

Potent inhibitor of checkpoint kinase 2 (Chk2)

Matrix metalloproteinase (MMP) inhibitor, also acting as a collagenase inhibitor

Second-generation leukotriene B4 receptor antagonist

Selective COX-2 inhibitor

Potent and selective inhibitor of p38 MAP kinase

Novel selective COX-2 inhibitor

Novel photoswitchable substrate for sphingomyelin synthase 2 (SMS2), enabling optical control of apoptosis and being ready for azide-alkyne click chemistry

Novel photoswitchable substrate for sphingomyelin synthase 2 (SMS2), enabling optical control of apoptosis and being ready for azide-alkyne click chemistry

Natural Potent Inhibitor of Transient Receptor Potential Melastatin 2 (TRPM2) Ion Channels

Natural selective non-peptide antagonist for the receptor GAL-1

Novel Inhibitor of the virus fusion to its cell receptor, targeting SARS-CoV-2 spike protein HR1

Novel Inhibitor of the virus fusion to its cell receptor, targeting SARS-CoV-2 spike protein HR1

Precursor for radioiosotopically labelled R(+)-SCH-23390

D1 dopamine receptor antagonist

Novel, orally active phosphodiesterase 4 (PDE4) inhibitor

Non-​nucleoside antiviral agent, having potent and selective activity against herpes simplex virus type 2 (HSV-​2)

Potent and selective PDE1 and PDE5 inhibitor

Novel Acyl_carrier_protein_synthase>acyl carrier protein synthase inhibitor; Inhibitor of growth of the bacteria Streptococcus_pneumoniae>Streptococcus pneumoniae and Neisseria_gonorrhoeae>Neisseria gonorrhoeae

Inhibitor of p21-hRas nucleotide exchange in vitro

Novel histamine H3-receptor antagonist

Novel potent and selective glucagon receptor antagonist

Novel inhibitor of SARS-CoV-2 main protease (MPro)

Novel inhibitor of vanilloid receptor subtype 1 (VR1)

Novel Lysine-Specific Demethylase 1 (LSD1) Inhibitor (IC50: 20nM)

Novel glucose transport inhibitor

Novel inhibitor of SARS-CoV-2 main protease (MPro)

Novel inhibitor of SARS-CoV-2 main protease (MPro)

Selective, ATP-competitive p38

Novel Inhibitor of p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs) with the IC50 values of 140, 910 and 17.5 nmol/L against MDM2, HDAC1, and HDAC6, respectively, showing the tumor growth inhibition (TGI) in the A549 xenograf

Novel dual acetylcholinesterase inhibitor (AChEI) and a calcium channel blocker (CCB)

Novel inhibitor of nNOS-PSD-95 interaction, exhibiting neuroprotective activities in NMDA-induced or Oxygen and glucose deprivation (OGD)-induced neuronal damage in primary cortical neurons cultures, and ameliorating focal cerebral ischemic damage in rats

NRTI-drug pair of zidovudine (AZT)-didanosine (ddI), being highly cytotoxic and mutagenic

Novel irriversible selective PDI inhibitor, selectively labeling protein disulfide isomerase and inhibiting its enzymatic activity, showing unique cytotoxicity in cells derived from multiple myeloma

Potent inhibitor of MMP-2, -3, -9, -8, -13, and -14

Selective, surmountable antagonist for 5-HT4 receptors

Novel inhibitor of the Golgi complex (Vrg4); Antifungal

Novel immunostimulatory monosaccharidic lipid A analog, down-regulating TNF-alpha and IL-6 production and priming secretion of G-CSF and IL-1 beta

Selective 5-HT2B/2C receptor antagonist

Novel inhibitor of sterol 14a-demethylases (CYP51)

Potent antiproliferative agent, binding to the “colchicine binding site” on tubulin and inhibiting tubulin polymerization in vitro

Highly selective human tachykinin NK1 receptor antagonist

Natural plant growth inhibitor

Novel open-ring metabolite of rapamycin derivative

Antagonist of gamma-aminobutyric acid A (GABA A ) receptor and cholinergic agent

Novel Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease

Novel potent inhibitor of the enzyme soluble epoxide hydrolase (sEH)

Novel AkaLumine analog, acting asa NIR emission luciferin with the enhanced solubility in water

Novel S100B inhibitor

Novel Wnt inhibitor/Axin stabilizer

Novel potent antagonist of the Hedgehog pathway

Sentrin-specific protease 1 (SENP1) inhibitor

Novel selenium-nonsteroidal anti-inflammatory drug (Se-NSAID), inhibiting colorectal cancer (CRC) growth via the inhibition of the cell cycle in G1 and G2/M phases and reduces the cell cycle markers like cyclin E1 and B1 in a dose dependent manner

Selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A) that prolong the benefit of eIF2α phosphorylation, thereby protecting cells from proteostatic defects

Novel mitochondrial KIM-1 receptor modulator to be specifically internalized by renal tubular epithelial cells via KIM-1 receptor-mediated endocytosis and then actively distributed in mitochondria under the effect of TPP, effectively ameliorating injured

Novel serotonin reuptake inhibitor

Cytochrome P450 14α-demethylase inhibitor, also acting as a BuChE-IDO1 inhibitor

Highly selective H1 receptor antagonist

The first-in-class triple-site aaRS inhibitor, targeting Salmonella enterica threonyl-tRNA synthetase (SeThrRS) with IC 50 = 19 nM and K d = 35.4 nM

The most potent inhibitor of Set7, inhibiting the KMTase G9a

Novel inhibitor of Mycobacterium marinum MelF (Rv1936), exhibiting bacteriostatic/bactericidal activity against M. marinum and M. tuberculosis in vitro

Novel potent CYP17 lyase inhibitor, inhibiting androgen production without mineralocorticoid excess or cortisol depletion

Novel telomerase inhibitor

The First potent SecA inhibitor

Potent and selective STAT5 inhibitor

Potent, selective, and highly brain-penetrant NPY Y2 receptor antagonist

Novel dual inhibitor of BRD4 and PI3K, inhibiting BRD4, PI3Kα, PI3Kδ, and PI3Kγ with IC 50 values of 277, 714, 27, and 1170 nM, respectively

Novel anticancer agent, arresting cell cycle in S-phase and causes DNA replication stress leading to the phosphorylation of H2AX into gamma-H2AX

Cell-permeable antagonist of secreted frizzled related protein-1(sFRP-1), inhibiting Wnt-3/frizzled interaction and restoring cellular response to Wnt-3 stimulation

Highly Potent and Selective Plasmin Inhibitor, Attenuating Fibrinolysis in Plasma

Novel probe for CAMKK2/CAMKK1

Novel probe for CLK1, CLK2, and CLK4

Negative control for SGC-GAK-1 (GLXC-31266)

Novel potent allosteric modulator of N-methyl-D-aspartate receptors (NMDAR)

PKM2 activator, potently inhibiting proliferation of cancer cells in media lacking serine

PKM2 activator, potently inhibiting proliferation of cancer cells in media lacking serine

Novel highly selective SGK1 inhibitor with a highly optimized profile suitable for oral dosing as a potentially disease-modifying agent for osteoarthritis

Novel Potent SGLT1/2 Dual Inhibitor

Novel inhibitor of the CML mutant Bcr-AblT315I, preempting in vitro resistance when combined with nilotinib or dasatinib.

Selective agonist of GABA A receptors α5 subunit

Potent and selective agonist of GABAA receptors α5 subunit

Novel potent sEH inhibitor, effectively blocking key angiogenic properties of human retinal endothelial cells (HRECs), inhibiting choroidal sprouting and significantly suppressing CNV lesion volume

Novel inhibitor of endothelial cell growth

Novel selective inhibitor of the generation of IL-5-producing Th2 cells and induction of active histone modifications at the IL5 gene locus during Th2 cell differentiation

Stable and ROS-free antagonist against anti-apoptotic Bcl-2 proteins, bypassing drug resistances and synergizing cancer therapies in human leukemia cell

First in Class Hypoglycemic Agent with Extra-Strong Action, increasing insulin sensitivity, improving glucose tolerance, reducing fasted insulin level and insulin sensitivity, decreasing total body and interscapular fat mass and also increasing the activi

Novel Selective Human ER Partial Agonist (ShERPA)

Selective inhibitor of cancer cell growth, exerting chemoprevention activity without evidence of toxicity

Novel Inhibitor of Phospho-STAT3 Through Induction of Protein Tyrosine Phosphatase PTPN6

Novel potent stabilizing ligand for FKBP-derived destabilizing domains

Cystathione gamma lyase (CSE) inhibitor, inhibiting H2S production and L-cysteine-induced relaxation of rat aortic rings ex vivo

Antineoplastic antibiotic

Inhibitor of shp2 protein tyrosine phosphatase (PTP)

Highly Potent and Peripheral Nervous System-Restricted KOR Agonist

Novel cognitive enhancer; Nootropic agent

Novel direct HIV-1 Nef antagonist with antiretroviral activity

Novel Complement Factor C1 Inhibitor

Silicon-Containing GABA Derivative, Treating Neuropathic Pain without Central-Nervous-System-Related Side Effects

Silicon-Containing GABA Derivative, Treating Neuropathic Pain without Central-Nervous-System-Related Side Effects

Novel COX-I and COX-II inhibitor with four times higher solubility in physiological media and a lower melting enthalpy than ibuprofen

Peroxisome proliferator

Antioxidant and antimicrobial agent, counteracting mitochondrial oxidative stress in cardiomyocytes

Novel D2/5-HT2A Receptor Dual Antagonist

Novel farnesoid X receptor antagonist

Novel SIRT1 Activator

First-in-class apolipoprotein E4 (ApoE4)-targeted sirtuin1 (SirT1) enhancer, normalizing sirtuin 1 levels and improving cognition in an Alzheimer's disease mouse model

Novel SIRT1 Inhibitor, showing potent effect on prostate cancer cell line

Novel SIRT1 inhibitor, inducing apoptosis in HCT116 human colon carcinoma cells partially by activating p53

Potent and selective inhibitor of SIRT2

Novel selective SIRT3 inhibitor, exhibiting SIRT3 inhibitory selectivity with IC50 value of 7.2 µM over SIRT1 (32.6 µM) and SIRT2 (33.5 µM), showing potent inhibitory activity against a group of MLLr leukemic cell lines

Novel in situ tetrazine ligation reactive silicon-rhodamine dye

Potent broad spectrm fluoroquinolone antibiotic

Fluoroquinolone antibiotic, acting as antibacterial, antineoplastic, anti-Infective agents, Inhibiting DNA-gyrase and topoisomerase

Novel inhibitor of lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF)-α and interleukin (IL)-6 on microglia, exhibiting anti-inflammatory activity through ER-stress-mediated autophagy, significantly inducing the conversion ratio of LC3 II/I and

Novel inhibitor of MAGE-A11 with robust activity in TR-FRET for disrupting MAGE-A11:PCF11 interactionm being cell permeable and having improved activity in the TR-FRET assay (IC50 0.13 µM)

Unique and highly potent nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1 (HIV-1), also inhibiting HIV-2

Novel inhibitor of MAGE-A11 with robust activity in TR-FRET for disrupting MAGE-A11:PCF11 interaction (IC50 0.40 μM)

Novel Inhibitor of the Disordered Protein, p27(Kip1)

Novel selective MDMX antagonist

Novel BRAF-targeting PROTAC, inducing efficient and potent degradation of mutant BRAF but sparing BRAFWT, inhibiting cell growth in mutant-BRAF driven cancer cells

Novel selective EGFR degrader

Novel potent EGFR degrader, being capable of penetrating the cell membrane, also degrading an exon-20 insertion mutant form of EGFR (ASV duplication)

Novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity

Novel inhibitor of HIV-1 infection by blocking viral DNA nuclear entry

Highly potent and efficacious proteolysis targeting chimera (PROTAC) degrader of PARP1 for treating cancers, potently inhibiting the growth of cancer cells bearing BRCA1/2 mutations and inducing potent and specific degradation of PARP1 in various human ca

Inhibitor of Aβ self-aggregation

Dopamine D1 receptor agonist

Selective, brain penetrant 5-HT(1B/D) receptor agonist

Novel dual-targeted inhibitor of sphingosine kinase and microtubule polymerization

Potent inhibitor of Dengue viruses (DENV), displaying activities against all four serotypes of DENV, as well as to a related flavivirus, West Nile virus (WNV), and an alphavirus, Sindbis virus (SINV)

Potent influenza A virus (IAV) entry inhibitor, targeting a conserved region of hemagglutinin

Novel inhibitor of NF

Millepachine analog, inhibiting tubulin polymerization by irreversibly binding to the colchicine-binding site in β-tubulin

Biological Active Reagents

Potent anticancer agent, downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK

Novel multikinase inhibitor, potently inhibiting angiogenesis-related kinases including VEGFR1/2/3, and FGFR2, and the Src kinase

Novel FLT3 and Wnt/β-catenin signaling inhibitor, displaying potent activity in models of FLT3-driven AML

Novel inhibitor of cell-cycle progression, inducing G0/G1 phase arrest and apoptosis in human hepatic carcinoma cells

Novel inhibitor of OLIG2 in glioblastoma

Specific Inhibitor of Skp2-Mediated p27 Degradation

Specific Inhibitor of Skp2-Mediated p27 Degradation

First-in-class Specific Inhibitor of Skp2-Mediated p27 Degradation

Novel microtubule-destabilizing agent, exerting potent antitumor activity against esophageal squamous cell carcinoma

Novel microtubule-destabilizing agent, exerting potent antitumor activity against esophageal squamous cell carcinoma

Full agonist of GABAA receptors containing α2 and α3 subunits, and partial agonist of α1 and α5 subunits.

Novel nonpeptide AT1 receptor antagonist, acting as a modulator on RAAS and KKS activation during COVID-19

Potential synthetic lethal lead, targeting E-cadherin-deficient cells

Novel Potent Dual inhibitor of SLK (STE20-like kinase) and STK10 (serine/threonine kinase 10)

Novel highly selective and potent κ opioid agonist (κ, Ki = 0.47 nM, κ/μ = 682, κ/δ = 283)

Novel potent SphK2-selective inhibitor (Ki = 89 nM, 73-fold SphK2-selective) with validated in vivo activity

Novel SphK2-selective inhibitor with improved half-life to 8 h in mice

Novel selective SphK1 inhibitor

Novel SphK2-selective inhibitor

Novel efflux pump inhibitor (EPI)

Novel efflux pump inhibitor (EPI)

Potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue

Novel Potent, Cell-Permeable, Conformationally Constrained Second Mitochondria Derived Activator of Caspase (Smac) Mimetic

Non-peptidic Smac mimetic, binding to XIAP, cIAP-1 and cIAP-2 proteins with higher affinities in cell growth inhibition in the MDA-MB-231 cell line

Novel potent and selective inhibitor of galactokinase (GALK1)

Novel inhibitor of IL-1

Proapoptotic and anti-inflammatory agent, inducing apoptosis by inhibiting apoptosis proteins (IAPs)

Novel activator of PP1, inducing HIV-1 transcription, reactivation of latent HIV-1 in chronically infected cells, and CDK9 phosphorylation

Potent inhibitor of microtubule polymerization

Potent inhibitor of microtubule polymerization

Novel inhibitor of Loxosceles sphingomyelinases D (SMases D)

Novel inhibitor of Loxosceles sphingomyelinases D (SMases D)