PPARdelta receptor agonist

Hepatoprotective and choleretic agent

Narcolepsy agent, being used to treat catalepse and daytime sleepiness in patients with narcolepsy

Natural tumor antagonistic steroidal alkaloid, inducing typical cellular apoptotic hallmarks and cell cycle blockage at S-G2/M phase, activating nuclear import of DFF-40 mediated nucleosomal disruption and cell demise

Novel oral, broad-spectrum matrix metalloproteinase inhibitor (MMPI), being >10-fold more active than marimastat in inhibiting the processing of cell-bound TNF-alpha

Novel long-acting, reversible albumin-binding growth hormone (GH) derivative for treatment of growth hormone dificiency

Unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue, effectively reducing GH secretion in human GH-secreting pituitary adenomas even in Octreotide non-responsive tumours.

Novel potent and selective allosteric modulator of sigma-1 receptor

Novel, selective and orally bioavailable c-Met inhibitor, exhibiting antitumor activity both in vitro and in vivo

A2A adenosine receptor agonist

Natural analgesic, antipyretic, anti-inflammatory, and anti-tumor agent

Inhibitor of constitutive and inducible STAT3 activation through the activation of SHP-2 tyrosine phosphatase

Natural inhibitor of the Kv1.3 channels in a concentration-dependent manner

Human norepinephrine transporter blocker

DAT modulator, being unique in affecting substrate uptake without impacting efflux

Novel partial inhibitor of amphetamine-induced dopamine release

Sorting inhibitor, blocking Vps16 function, one protein in the class C tethering complex, and increasing aflatoxin synthesis and export

Novel Programmed Death Ligand 1 (PD-L1) Binding Peptide (a Peptide Ligand for PD-L1)

Novel telomerase inhibitor

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Novel photo-controllable hydrogen sulfide donor applicable in live cells

Novel anti-tuberculosis agent against intracellular Mycobacterium tuberculosis

Antibiotic, binding to the bacterial 30S ribosomal subunit, interfering with the initiation of protein synthesis and with proper protein elongation and leading to bacterial cell death

Novel gamma-secretase modulator

Novel selective orally bioavailable inhibitor of p300/CBP histone acetyltransferase

Novel p53 Stabilizer for Brain Cell Differentiation

Sterol Biosynthesis Inhibitor, Fungicide

Novel potent sPLA2 inhibitor, selectively targeting hGIIA and hGIID

Novel isosteric charge-deficient spermine analogue

USP7 inhibitor from the marine sponge Stylissa massa

Pivotal intercellular signal transmitter

Novel SPOP inhibitor, suppressing the viability and inhibiting the colony formation of ccRCC cell lines driven by cytoplasmic SPOP

Novel potent serine palmitoyl transferase (SPT) inhibitor

Novel potent and selective binder of small subunit B of the serine palmitoyltransferase complex (SPTSSB)

Novel specific PAK4 inhibitor, effectively inhibiting the invasion of SGC7901 cells without cytotoxicity, regulating the PAK4/LIMK1/cofilin and PAK4/SCG10 signaling pathways

Novel inhibitor of the in vivo aggregation of

Novel NR4A nuclear receptor modulator

Novel NR4A nuclear receptor modulator

Selective neurotensin antagonist

Novel Unc-51-Like Kinase 1 (ULK1)

Novel partial agonist of PPARgamma

Novel NR4A nuclear receptor modulator

Potent inhibitor of both JNK3 and p38

Novel Inhibitor of c-Jun N-terminal Kinase 3 (JNK3)

Novel renin inhibitor

The first selective β3 adrenergic agonist, showing to possess a profile of antidepressant activity in rodents

Novel Selective TBK1/IKK dual inhibitor with anticancer potency

Peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR)

Novel inhibitor of sterol regulatory element-binding protein (SREBP), impairing the SREBP activity by inhibiting glucose transporters and thereby activating AMP-activated protein kinase (AMPK)

Novel mixed μ opioid receptor (MOR) agonist and δ/κ opioid receptor (DOR/KOR) antagonist

Highly blood-brain barrier permeant, potent, and selective for LRRK2 kinase activity, being effective in attenuating pro-inflammatory responses in macrophages and rescuing neurite retraction phenotypes in neurons.

Potent DAT allosteric modulator, partially inhibiting DAT uptake without altering DAT-mediated reverse transport and with minimal inhibition of DAT binding

Novel inhibitor of thrombospondin 1 activation of TGF-β, blocking TGF-β activation (pIC50 = 8.12 nM) and has a plasma half life of 1.8 h (iv)

Novel potent inhibitor of Wn/ß-catenin signaling in cancer cells

Novel GLUT inhibitor, preferentially inhibiting the growth of GBM cells with minimal toxicity to non-neoplastic astrocytes and neurons, also inhibiting glucose uptake and decrease the glycolytic capacity and glycolytic reserve capacity of GBM patient-deri

Novel GLUT inhibitor, preferentially inhibiting the growth of GBM cells with minimal toxicity to non-neoplastic astrocytes and neurons, also inhibiting glucose uptake and decrease the glycolytic capacity and glycolytic reserve capacity of GBM patient-deri

Novel MOR agonist/DOR antagonist that produced systemically active potent antinociceptive activity in tail-flick assay in mice

Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss

Novel potent SIRT1 activator

Novel selective CXCR2 antagonist

Novel potent inhibitor of Staphylococcus aureus sortase A (SrtA)

Novel antiestrogen, lacking estrogenic and genotoxic actions

Potent ß-amyloid aggregation inhibitor; Antioxidant

Potent competitive inhibitor of indoleamine 2,3-dioxygenase (IDO)

Non-selective potent dopamine reuptake inhibitor

Non-selective potent dopamine reuptake inhibitor

Novel inhibitor of Pak1 activation, anti-cancer ingredient isolated from the Chinese traditional herb Curcuma wenyujin

The first selective inhibitor of Histone Deacetylase 2 (HDAC2)

Novel antimalarial agent

Elongation factor P (EF-P) fuction modifier

Potent furin inhibitor, blocking furin-dependent cell surface processing of anthrax protective antigen-83 in vitro.

Novel chimeric degrader against cellular retinoic acid binding proteins (CRABPs), inducing the AhR-dependent degradation of CRABP-1 and CRABP-2 via the ubiquitin-proteasome pathway

Novel chimeric degrader against bromodomain-containing (BRD) proteins, inducing the interaction of AhR and BRD proteins and displaying effective anticancer activity that correlated with protein knockdown activity

Cofactor for mitochondrial deacetylase sirtuin-3 enzyme, regulating energy metabolism and immunity and modulating inflammasome assembly

Novel Selective and Orally Active Oxytocin Receptor Antagonist for the Prevention of Preterm Labor

SSR-180,575 is a drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO. It has been shown to have neuroprotective and cardioprotective effects and to stimulate steroidogenesis of pregnenolone in the brain, which may be linked to its neuroprotective action.

Inhibitor of the replication of herpes simplex viruses 1 and 2 (HSV-1 and HSV-2)

Novel non-peptidic highly potent somatostatin receptor 3 (SSTR3) agonist

Novel potent sstr3 antagonist, showing to reduce glucose excursion in a mouse oGTT assay

Novel somatostatin receptor subtype 5 antagonist, stimulating glucoseinduced GLP-1 secretion, reducing blood glucose in a gut- and GLP-1R-dependent manner

Novel potent mast cell (MC) activator, promoting de novo synthesis of cytokines and inducing the release of eicosanoids from human and mouse MCs

Novel potent mast cell (MC) activator, promoting de novo synthesis of cytokines and inducing the release of eicosanoids from human and mouse MCs

Novel inhibitor of the c-di-AMP synthetase DNA integrity scanning protein (DisA) in vitro

Novel potent mast cell (MC) activator, promoting de novo synthesis of cytokines and inducing the release of eicosanoids from human and mouse MCs

Novel histamine H3 receptor ligand

Potent, direct, non-cytotoxic Arachidonate_5-lipoxygenase>5-lipoxygenase (5-LO) inhibitor

Antiviral agent against LASV and a number of other viruses in the Arenaviridae family

Novel histamine H3 receptor ligand

Novel highly potent and soluble partial FXR agonist

Seletive dopamine D3 receptors

Novel potent A 1 R/A 2A R/H 3 R multitargeting ligand (MTL)

Novel potent A 1 R/A 2A R/H 3 R multitargeting ligand (MTL)

Novel selective NaV1.7 inhibitor, blocking the extracellular vestibule of the channel with an IC50 of 72 nM and greater than 200-fold selectivity over off-target sodium channel isoforms, NaV1.1-1.6 and NaV1.8

Highly selective FAAH>fatty acid amide hydrolase (FAAH) inhibitor

Novel PARP-1 inhibitor, showing significant in vitro target inhibition and capability to substantially bypass the multidrug resistance mediated by Pgp

Novel tubulin-binding vascular disrupting agent (VDA)

Cell permeable AKAP disruptor, selectively binding to PKA-RII and blocking the interaction of PKA-RI with AKAP

Novel Lipopeptide Antibiotic with Potent Antibacterial Activity against Multidrug-Resistant Bacteria

Anabolic-androgenic steroid (AAS), acting as an agonist of the androgen receptor (AR)

Novel STAT3 inhibitor, selectively inhibiting STAT3 phosphorylation and exhibiting potent antitumor activity

Novel inhibitor of STAT3 signaling pathway

Novel inhibitor of STAT3, targeting SH2 domain

Novel potent and selective inhibitor of STAT3

Novel inhibitor targeting the DNA-binding domain of STAT3, suppressing tumor growth, metastasis and STAT3 target gene expression in vivo

Novel inhibitor of signal transducer and activator of transcription 3 (STAT3), inhibiting the proliferation of tumor cells harboring abnormal activation of STAT3, such as, MDA-MB-468, MDA-MB-231 and DU145

Novel cell-permeable selective STAT5a inhibitor prodrug, inhibiting tyrosine phosphorylation of STAT5a with selectivity over STAT5b in cultured human leukemia cells, and representing a valuable tool to define the non-redundant molecular functions of the t

Highly Potent and Selective Inhibitor of the Transcription Factor STAT5b

Novel human stem/progenitor cells proliferation activator, promoting survival and preserving stemness in human embryonic stem cells

Natural inducer of G1 arrest in primary human esophageal epithelial cells but G2 arrest in immortalized cells

Novel inhibitor of expression from canonical CREB response element-containing promoters

Novel RBP4 antagonist for treatment of Stargardt disease

Natural anti-feline infectious peritonitis virus (FIPV) agent, specifically targeting the 3CLpro of FIPV and inhibiting its replication

Novel non-nucleotide STING agonist, demonstrating antitumor activity when dosed intratumorally in a syngeneic mouse model

Novel covalent antagonist of hsSTING

Novel Fatty Acid Binding Protein 5 (FABP5) Inhibitor

Novel Fatty Acid Binding Protein 5 (FABP5) Inhibitor

Dual inhibitor of topoisomerase 1 and 2, inducing G(2) arrest in the absence of DNA damage. Inhibitor of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay

Novel inhibitor of the heterogeneous ribonuclear protein A18 (hnRNP A18)

Novel blocker of IL-17A binding to the IL-17A receptor (IL-17RA)

Novel activator of cellular ATG4B activity

Potent natural modulator of human Toll-like receptor 7 (TLR7)

Metablite of the Streptomyces antibiotics streptothricin and streptolin

Antibiotic, being used as an antineoplastic agent and to induce diabetes in experimental animals

The first nonpeptidyl, selective activator of the tissue-protective EPOR/CD131 receptor

Novel agonist of the tissue-protective erythropoietin (EPO) receptor, increasing FXN expression and EPOR phosphorylation

Inhibitor of 17β-hydroxysteroid dehydrogenases (17β-HSDs)

Novel Nonsteroidal Inhibitor of Carbonic Anhydrase IX

Novel dual Inhibitor of repair enzymes 8-oxoguanine DNA glycosylase (OGG1) and human MutT Homolog 1 (NUDT1 or MTH1), increasing sensitivity of tumor cells to oxidative stress

Novel potent c-MET inhibitor

Potent c-MET inhibitor

Sunitinib analog, acting as a potential inhibitor for nucleoside diphosphate kinase (NDK) from Leishmania major (LmNDK)

Agonist of TRPV1

Novel potent and selective inhibitor of the cellular PDGF receptor kinase and PDGF receptor-induced cell proliferation

Natural immunosuppressive agent, effectively blocking T cell proliferation and survival while profoundly inhibiting pro-inflammatory IFNγ and IL-17 production by fully differentiated effector Th1 and Th17 cells, also acting as an estrogen receptor antagon

Fluorescent substrate which can be hydrolyzed by the proteasome to release free AMC and the fluorescence of which is proportional to the proteasome activity

Novel antagonist of G-protein-coupled receptor SUCNR1 (succinate receptor 1 or GPR91)

Novel potent inhibitor of osteoclastogenesis, suppressing both equilibrative nucleoside transporters and concentrative nucleoside transporters

Novel inhibitor of airway inflammation and hyperresponsiveness in experimental models of chronic obstructive pulmonary disease (COPD)

Antibacterial, inhibiting bacterial folic acid synthesis by competing with para amino benzoic acid

β-Lactam antibiotic against multi-drug resistant pathogens

Novel inhibitor of RhoG-hepcidin uptake

Neuroprotective agent, alleviating stroke-induced neuroinflammation

Peripheral vasodilator

Novel, potent, selective, and competitive antagonist of LTD4 and LTE4

D2 selective dopamine agonist, showing anxiolytic and anti-parkinsonian activities

Novel fibroblast growth factor receptor modulator for treating neurodegenerative diseases

5-HT2 antagonist

Potent Inhibitor of Plasmodium FK506 Binding Protein 35 (FKBD35), also act as a HIV inhibitor

Antagonist of the mammalian bile acid sensor farnesoid-X-receptor (FXR)

Selective D2 dopamine receptor antagonist

D2 dopamine receptor partial agonist in adenylyl cyclase inhibition assay and antagonist in the GIRK and phospho ERK1/2 assays

Novel clickable tumor-specific irreversible inhibitor of stearoyl CoA desaturase (SCD)

Natural potent alpha-mannosidase inhibitor, exhibiting antimetastatic, antiproliferative, and immunomodulatory activities

Potent differentiating agent

Novel selective OXE receptor antagonist

Novel highly potent and selective CDK7 inhibitor, demonstrating broad anti-tumor activity in vivo

Novel universal opioid receptor agonist

Novel inhibitor of the Syk kinase (spleen tyrosine kinase)

Novel potent and specific inhibitor of syncytin-mediated cell fusion, completely blocking cell fusion at 1.6 μg/ml

Negative control of Syn-1 peptide, having the same amino acid composition as Syn-1 peptide, but a scrambled sequence

Novel Mycobacterium tuberculosis growth inhibitor

Novel microtubule-stablizer

K+ channel blocker

Novel TLR7 agonist via immune response induction and tumor microenvironment modulation

Potent inhibitor of both rodent and human MAO-B, proved to be safe in high doses with no hERG and mutagenic activities and demonstrated neuroprotection in an in vivo chronic model of PD

Novel COX-2 inhibitor

Potent and selective CCKA receptor antagonist

Novel potent PPARγ antagonist with much improved drug-like properties and promising pharmacokinetic profile

Selective class B inhibitor of the Ca -activated Cl- Channel, Ano1(TMEM16A)

Selective class D inhibitor of the Ca -activated Cl- Channel, Ano1(TMEM16A)

Type-A trichothecene mycotoxin

Novel inhibitor of the type III secretion system (T3SS), acting as a anti-microbial agent against Xanthomonas oryzae pv. oryzae (Xoo)

Novel Inhibitor of Adenovirus Gene Transfer

Novel Inhibitor of Adenovirus Gene Transfer

Inhibitor of HIV-1 Assembly that Targets the Phosphatidylinositol (4,5)-bisphosphate Binding Site of the HIV-1 Matrix Protein

Novel inhibitor of the catalytic functions of peroxiredoxin (Prx) and thioredoxin (Trx) systems

Natural radical scavenger on ABTS

Novel Inhibitor of Parasite Motility and Invasion

Novel Inhibitor of Parasite Motility and Invasion

Novel Irriversible Inhibitor of Parasite Motility and Invasion

Novel Potent Dual AChE/GSK-3 Inhibitor for the Treatment of Alzheimers Disease

Novel potent p53-MDM2/X antagonist, inhibiting MDM2 potently with a Ki value of 58 nmol/L, inducing accumulation of p53, p21 and MDM2, inhibiting cell cycle progression of U-2 OS cells at G1 phase in a p53-dependent manner

Novel inhibitor of the Klebsiella pneumoniae VapBC toxin-antitoxin (TA) system, acting as antimicrobial agents by disrupting the VapBC complex and activating VapC

Novel AMPA receptor potentiator with little agonistic effect, producing antidepressant-like effect without causing psychotomimetic effects

Long-lasting ergosterol biosynthesis inhibitor

Potent FAAH Inhibitor

Novel anti-HIV CCR5 antagonist

Novel selective 5-hydroxytryptamine type 2C (5-HT2C) receptor agonist

Novel inhibitor of the epigenetic modulator lysine-specific demethylase 1A (LSD1)

Natural ferroptosis inducer, killing colorectal cancer cells in vitro and in vivo

CYP26 inhibitor, potentiating the effects of all-trans retinoic acid on cultured human epidermal keratinocytes

Natural neurotrophic agent, promoting neurite outgrowth from neurons through PI3K/Akt pathway

Novel Antibody-Drug Conjugate PBD Dimer Payload

Superagonist at the human thyrotropin-releasing hormone receptor, reversing opioid-induced respiratory depression in isoflurane anesthetized rats

Novel Fluorescent dATP for DNA Synthesis In Vivo, exhibited high brightness, low toxicity, and rapid incorporation and depletion kinetics in both a vertebrate (zebrafish) and a nematode (Caenorhabditis elegans)

Potent and selective non-peptide δ1 opioid receptor agonist

Novel angiogenesis stimulator, promoting multiple key steps of angiogenesis parially via Akt and MAPK signalling pathways, showing anti-ischemic and anti-atherosclerosis activities, also acting as a putative PPARγ agonist

Novel potent Na V -targeting peptide, exhibiting significant increased potency for Na V 1.1, Na V 1.2, Na V 1.3, Na V 1.6 and Na V 1.7 involved in several neurological disorders including acute and chronic pain, motor neuron disease and epilepsy

Novel potent Na V -targeting peptide, exhibiting significant increased potency for Na V 1.1, Na V 1.2, Na V 1.3, Na V 1.6 and Na V 1.7 involved in several neurological disorders including acute and chronic pain, motor neuron disease and epilepsy

ADAM-17 (TACE) and MMP inhibitor, sensitizing cancer stem cells to the lethal effects of 5-FU and blocking shedding of TNF-α from cell membranes