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)

Fluorogenic fluorescent probe for imaging lipid droplets; suitable for use with two-photon microscopy

Novel Allosteric Inhibitor of p97

Novel enhancer of the clearance of mutant aggregate-prone proteins by autophagy in mammalian cell models of Huntington's and Parkinson's disease, independent of rapamycin

Novel strathclyde minor groove binder (S-MGB), curing animal African trypanosomiasis (AAT)

Novel enhancer of the cyclin-dependent kinase (CDK) inhibitor p27(Kip)

Novel TLR2 agonist, promoting cross-presentation by mouse and human antigen presenting cells

Novel highly hydrophilic and non-ATP-competitive MEK1/2 inhibitor

Selective, direct-acting covalent inhibitor of the K-Ras G12C mutant relative to wild-type Ras

Novel Active Site Inhibitor of Oncogenic K-Ras G12C

Novel Stablizer of Survival of Motor Neuron 2 (SMN2) , Post-Translationally Stablizing SMN Protein for the Treatment of Spinal Muscular Atrophy (SMA)

Novel specific splicing enhancer, targeting RNA for a specific splicing correction, recognizing the interface between U1 snRNP and the SMN2 E7 5ʹ SS, promoting the U1-C zinc finger RNA duplex binding activity

Second-generation modulator of utrophin, increasing utrophin expression in skeletal, respiratory and cardiac muscles

Novel dual inhibitor of thrombolysis and soluble epoxide hydrolase

Novel Smurf1 inhibitor, promoting bone formation in mouse models of distinctive age-related osteoporosis

Novel potent TLR1/2 Specific Agonist, Suppressing Leukemia Cancer Cell Growth by Stimulating Cytotoxic T Lymphocytes

Selective ligand of GC-rich sequences in DNA

Novel potent DNA-binding topoisomerase II-directed antitumor agent.

Novel specific inhibitor of Aldo-keto reductase 1C3 (AKR1C3, EC 1.1.1.188)

Novel Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency In Vivo

Potent and selective GAL3 antagonist

Highly selective alpha1A-adrenoceptor antagonist

Specific and Nongenetic IAP-dependent Protein Eraser (SNIPER), acting as a protein degradation inducer of oncogenic BCR-ABL protein

Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Eraser (SNIPER), acting as a a protein degradation inducer of bromodomain-containing protein 4 (BRD4)

Novel fused proteins degrader of the His-tagged CRABP-II and Smad2 in cells

Novel potent degrader of the mitochondrial CRABP-II protein

Novel potent and selective degrader of the ERα protein

Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Eraser (SNIPER), acting as a a protein degradation inducer of phosphodiesterase-4 (PDE4)

Novel potent serotonin and noradrenaline reuptake inhibitor (SNRI) with moderate 5-HT2A antagonist activity for anti-depression

Inducer of apoptosis in neuroblastoma cells through inhibition of AKT signaling pathway

Novel agonist of PPAR-gamma, inhibiting lipopolysaccharide (LPS)-induced NO production and pro-inflammatory cytokines, potentiating interleukin-4-induced arginase-1 expression, promoting microglial polarization toward to an M2 anti-inflammatory phenotype

Highly selective inhibitor of CDK8 and its isoform CDK19

Novel macrophage modulator, inhibiting inflammation and M1 polarization of macrophages, restoring the balance between M1-polarized and M2-polarized macrophages in high fat diets (HFD)-induced obese mice resulting in the improvement of adipose inflammation

Inhibitor of tubulin polymerization, resulting in cell cycle arrest and induction of apoptosis

Orally available active prodrug of ICRF-154, interferring with topoisomerase II activity prior to the formation of intermediate cleavable DNA-enzyme complexes during the catalytic cycle resulting in tumor cell growth inhibition

Novel potent inhibitor of SOD1-Derlin-1 interaction

Novel potent inhibitor of SOD1-Derlin-1 interaction

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