Potent and selective NOP receptor antagonist

Cyclophilin inhibitor, showing reduction in interleukin-2 expression and reduction in CNS inflammatory infiltrates, inhibiting HCoV-229E replication

Novel potent tyrosine kinase inhibitor (TKI), targeting c-Met, VEGFR2 and Axl

Novel potent PARP1 inhibitor

Novel self-immobilizing near-infrared (NIR) fluorogenic probe that can be activated by senescence-associated ß-galactosidase (SA-ß-Gal), the most widely used senescence marker

Novel highly selective and sensitive near-infrared fluorescent probe for imaging of hydrogen sulphide in living cells and mice

Novel precursor of bright-emission NIR-II fluorophores for in vivo tumor imaging and image-guided surgery

NIR emitting firefly luciferin analogue, displaying dose-independent improved NIR emission even at low concentrations where the native d-luciferin substrate does not emit

Novel NIR NIR O2˙– probe, displays superior sensitivity to NIR O2˙– and having the capability to monitor trace amounts of intracellular NIR O2˙– in AKI in vivo

Antiviral agent against KFDV, AHFV, OHFV, as well as tick-borne encephalitis virus (TBEV) and mosquito-borne flaviviruses

Selective modulator of amyloid-beta peptide degradation, regulating Abeta levels

Novel pan-caspase inhibitor, potently reducing not only inflammasome-mediated interleukin-1β (IL-1β) secretion but also osteoclast differentiation in BMMs

Neuroprotective, protecting neurons from death following cerebral anoxia (interruption of oxygen supply to the brain).

Topoisomerase I inhibitor prodrug, slowly hydrolyzing and releasing irinotecan, increasing drug penetration into tumors and decreasing drug clearance

Novel Enterovirus 71 Inhibitor, binding to the hydrophobic pocket in VP1 to block viral infection, exhibiting excellent antiviral activity (with an EC50 of 5.056 nM and a 100% protection rate for mice at a dose of 20 mg/kg) and low toxicity

Novel NLRP3 inhibitor, reducing caspase-1 activation, oligomerization of ASC, and therefore, IL-1β processing, showing a significant anti-inflammatory effect and reduced mechanical hyperalgesia at 3 and 10 mg/kg (i.p.) in an in vivo mouse of gout

Novel Nm23-H1 activator, exerting cytotoxic effects on metastatic breast cancer cells by inducing mitochondrial dysfunction only under glucose starvation

Novel inhibitor of the Gli1 transcription, inducing apoptosis in cancer cells but not in non-cancerous cells

Novel inhibitor of glioma-associated oncogene homologue 1 (Gli1) mediated transcription

Novel Inhibitor of Nonsense-Mediated RNA Decay, Suppressing Nonsense p53 Mutations

Potent and state-dependent Nav1.7 antagonist

Novel Mdm2 inhibitor, acting as a negative regulator of p53, reducing viability in cell culture and suppressing tumor growth

Novel Microtubule Modulator, Blocking Mitosis and Inducing Apoptosis in HeLa Cells by Binding to Tubulin

Covalent and allosteric inhibitor of the ATPase VCP/p97, inducing cancer cell death

Novel selective and orally bioavailable MPS1 inhibitor

Novel JAK2 inhibitor, displaying significant tumor growth inhibition in SET-​2 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favorable pharmacokinetic and safety profile

Novel Potent and Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor (CCK-1R) Agonist

Novel inhibitor of autophagy, protecting cardiomyocytes against hypoxia/reoxygenation injury

Novel selective histamine H3 antagonist

Iminosugar, binding to the active site of lysosomal beta-glucosidase and stabilizing the proper folding for the catalytic form, acting as a chemical chaperone that facilitate transport and maturation of acid beta-Glu

Novel potent alkynyl bisubstrate inhibitor of nicotinamide N-methyltransferase (NNMT)

Novel non-nucleoside reverse transcriptase inhibitor (NNRTI)

Moderate antibiotic agent against a broad spectrum of gram-negative bacteria

The universal precursor of the nocardicins

Natural Inhibitor of an Oncogenic RNA, targeting RNA folds in the nuclease processing site in the oncogenic, noncoding microRNA-18a, selectively inhibiting nuclease processing in vitro and in prostate cancer cells and triggering apoptosis

Nocazine family member

Marine natural nocazine family member; Standard used in nocazine biosynthetic parthway studies

Neuropeptide, acting as a endogenous ligand for the nociceptin receptor (NOP, ORL-1)

PPARalpha agonist and EC 3.5.1.23 (ceramidase) inhibitor

Steroidal progestin

Neutral, nonandrogenic, progesterone-like profile progestin

Novel human epidermal growth factor receptor-2 (HER2) inhibitor; Spermatocide

Novel red-light-controllable nitric oxide (NO) releaser

FAUC-365 analog

Steroidal progestin used in veterinary medicine to control estrus and ovulation in cattle

Secondary metabolite from the myxobacterium Sorangium cellulosum, acting as a potent HCV inhibitor, Ebola virus (EBOV) entry inhibitor, and a potassium channel inhibitor

Controllable nitric oxide (NO) donor, releasing NO triggered by photoinduced electron transfer (PeT)

Natueal sigma receptor agonist, attenuating cytokine release associated with SARS-CoV-2, also being used as anti-malarial, anti-stroke and cough-suppressant

Novel potent inhibitor of notum carboxylesterase activity

Novel potent notum inhibitor (OPTS IC50 3.6nM; TCF-LEF EC50 220nM), showing good plasma exposure and reasonable CNS penetration

Novel potent LRRK2 inhibitor

Natural inhibitor of the allosteric regulation of Hsp70

Natural inhibitor of jasmonate signaling targets JAR1 in Arabidopsis thaliana

Second-Generation RET/VEGFR2 Inhibitor

Novel stabilizer of long noncoding RNA (lncRNA) GAS5, binding to GAS5 with high affinity, and increasing GAS5 levels and glucose uptake in diabetic patient adipocytes

Novel Inhibitor of Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1)

Novel Inhibitor of Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1)

Novel inhibitor of Trypanosoma brucei PDEB1 (TbrPDEB1)

Novel selective SIRT2 inhibitor, creating a hydrophobic cavity behind the substrate-binding pocket after a conformational change of the Zn-binding small domain of SIRT2

Novel activator of 15-ADON production, significantly increasing the transcription of Tri6, a transcription factor gene necessary for trichothecene biosynthesis, in both trichothecene-inducing and noninducing culture conditions

Novel biomediator, inducing reveromycin production in Streptomyces sp. SN-593

Novel tubulin inhibitor

Novel competitive MTH1 inhibitor

Novel tubulin inhibitor

Novel heterotrimeric G-protein Gi modulator, inhibiting GDP/GTP exchange on a Gαi subunit induced by a G-protein-coupled receptor agonist, but not on another G-protein from the Gαs family, regulating Gβγ-dependent cellular processes, most likely by causin

Novel inhibitor of TGF-β1 signaling pathway, inhibiting the upregulation of MAT2A mechanistically, dose-dependently activating PP2Cα and efficiently alleviating liver fibrosis

Novel potent activator of the natriuretic peptide receptor C (NPR-C) with EC 50 ~1 μM

Calcilytic negative allosteric modulator of calcium-sensing receptor (CaR)

Novel substrate for NAD(P)H: quinone oxidoreductase 1 (NQO1), acting as an effective intracellular ROS generator for the treatment of drug-resistant non-small-cell lung cancer

Novel NMDA/NR2B Antagonist

Novel activator of the Nrf2/HO-1 pathway, upregulating heme oxygenase-1 (HO-1) via promoting nuclear translocation of nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) to regulate LPS‐induced oxidative stress in macrophages

Nrf2-Activator is a potent Nrf-2 activator.

Novel inhibitor of CDK5 translocation, increasing CDK5 accumulation in the nucleus, suppressing both cancer cell proliferation and xenograft tumorigenesis.

Potent, non-selective partial agonist at GABAA receptors with little efficacy at the alpha1 subtype and more at alpha2 and alpha3

Novel Inhibitor with Activity against NS3/4A proteases from Multiple Hepatitis C Virus Genotypes

Novel allosteric inhibitor of HCV NS3 protein function

Novel molulator of SK-IK channels [small- and intermediate-conductance Ca2(+) -activated K(+) channels]

Novel potent α7 nAChR partial agonist

Novel α7 nAChR agonist at human and rat receptors

Novel potent growth inhibitor for gammaherpesvirus-associated B-lymphomas through activation of both the NF-κB and c-Myc-mediated signaling pathways

Novel Inhibitor of the Ras Converting Enzyme 1 (Rce1) Protease, Disrupting Ras Membrane Localization in Human Cells

Novel antagonist of the Grb7 SH2 domain; Antitumor Agent

Ras converting enzyme 1 (Rce1) inhibitor

Novel inhibitor of ABCG2 transporter function

Ligand of the Grb7 SH2 domain, inhibiting the growth of MDA-MB-468 cancer cells

Novel substrate of ABCG2

Inhibitor of human tyrosyl-DNA phosphodiesterase 1 (TDP1)

Novel potent inhibitor of Huntington's disease (HD) pathogenesis via targeting CAG repeats RNA and Poly Q protein

Novel selective inhibitor of JAK3

Selective inhibitor of shp2 protein tyrosine phosphatase (PTP)

Selective non-lipid agonist of LPA2/3

Apoptosis inducer; Antitumor agent

Novel inhibitor of the second bromodomain (BD2) of the BET family protein BRD2

Novel potent SHP2 Inhibitor with Anti-Proliferative Activity in Breast Cancer Cell Lines

HIF-pathway inhibitor

Novel inhibitor of Nef-calnexin interaction

Inhibitor of the RUNX1-CBFβ interaction

Specific inhibitor of ERCC1-XPF with no effect on both HhaI and XPG

Novel potent and selective serotonin reuptake inhibitor (SSRI)

Selective G-quadruplex inducer of the human telomeric sequence; Stabilizer of the G-quadruplex formed by the MYC promoter sequence; Anti-neoplastic effects in wild-type p53, p53-mutant or p53-deficient human colon cancer cells.

Non-nucleoside reverse transcriptase inhibitor

Novel inhibitor of growth of intracellular Mycobacterium tuberculosis, inducing autophagy in differentiated THP-1 macrophages

Capturer of kinase-insertion domain receptor (KDR) from a solution, while allowing the captured KDR to bind with the solution-phase vascular endothelial growth factor (VEGF)

Novel inhibitor of ABCG2 transporter function

Novel potent SHP2 Inhibitor with Anti-Proliferative Activity in Breast Cancer Cell Lines

Novel 3C-like protease inhibitor of SARS-CoV-2

Novel Rho-Kinase-II Inhibitor with Vasodilatory Activity

Specific Ligand for Stem Loop 3 Ribonucleic Acid of the Packaging Signal Ψ of Human Immunodeficiency Virus-1

Novel substrate of ABCG2

Novel Inhibitor of the p53-mdm2 Interaction, Activating p53-Dependent Transcription in mdm2-Overexpressing Cells

Novel Rho-Kinase-II Inhibitor with Vasodilatory Activity

Novel potent gonist of Human G Protein-Coupled Receptor-35 (hGPR35) (EC50 8 nM)

Novel inhibitor of Chk1 pathway in 5-FU-resistant CRC bulk and stem cell populations

Novel selective inhibitor of TET1 transcription and 5-hydroxymethylcytosine (5hmC) modification, effectively inhibiting cell viability in AML with high expression of TET1

Potent inhibitor of the AcrAB-TolC efflux pump in Escherichia coli, potentiating the antibacterial activities of novobiocin and erythromycin upon binding to the membrane fusion protein AcrA

Novel potent Mycobacterium tuberculosis DHFR inhibitor

Selective potentiator at GluN1/GluN2C and GluN1/GluN2D receptors

DT-diaphorase inhibitor

Novel Rho-Kinase-II Inhibitor with Vasodilatory Activity

Potent apoptosis inducer in pancreatic cancer cells

Novel potent inhibitor of Huntington's disease (HD) pathogenesis via targeting CAG repeats RNA and Poly Q protein

Novel antagonist of the Grb7 SH2 domain; Antitumor Agent

Novel specific inhibitor of EGF receptor autophosphorylation and cell proliferation in HeLa cells by disrupting allosteric activation of EGF-stimulated dimer

Novel antagonist of the Grb7 SH2 domain; Antitumor Agent

Novel potent SHP2 Inhibitor with Anti-Proliferative Activity in Breast Cancer Cell Lines

Novel non-peptide disruptor of IKKß/NEMO complex

Novel efflux pump inhibitor (EPI)

Novel activator of lanthionine synthetase C-like 2 (LANCL2), down-modulating pulmonary inflammation through the downregulation of TNF-α and MCP-1 and reduction in the infiltration of neutrophils, accelerating recovery and inducing IL-10-mediated regulator

Novel DNA repair inhibitor

Novel inhibitor of ABCG2 transporter function

Novel selective non-zinc-binding MMP-2 inhibitor

Novel dual inhibitor of viral and Streptococcus pneumoniae neuraminidase

Novel potent inhibitor of Huntington's disease (HD) pathogenesis via targeting CAG repeats RNA and Poly Q protein

IκBα phosphorylation inhibitor

Toxitant of Saccharomyces_cerevisiae>Saccharomyces cerevisiae

Potent CDC25A>Cdc25A inhibitor; Vitamine K3 analogue

Potent and selective nociceptin opioid receptor (NOP) agonist

Novel NF-κB inhibitor

Novel inhibitor of the Skp2-Cks1 protein-protein interaction and p27(Kip1) ubiquitination in vitro

Novel inhibitor of the Skp2-Cks1 protein-protein interaction and p27Kip1 ubiquitination in vitro

Novel Inhibitor of HCV NS3/4A Proteinase

Novel selective serotonin reuptake inhibitor (SSRI), exhibiting higher binding affinities in comparison with the paroxetine

Novel Inhibitor of HCV NS3/4A Proteinase

Novel Inhibitor of HCV NS3/4A Proteinase

Cytotoxic MDR-selective ligand

Novel anticancer agent, suppressing the growth of several cell lines derived from lung, colon, breast, ovarian, and kidney cancers

Novel down-regulator of EZH2, inducing G2/M cell-cycle arrest of cancer cells and degradating p53 via proteasome-dependent and -independent pathways

Telomerase inhibitor, stabilizing G-quadruplex and suppressing cell growth of A549 human lung cancer cells through activation of the ATR/Chk1-dependent pathway

Telomerase inhibitor, anticancer agent

Novel inhibitor of poly (ADP-ribose) polymerase-1 (PARP-1)

Novel inhibitor of lipid metabolism, disrupting tubulin polymerization,suppressing monoglycerol metabolism depleting lipids and inhibiting the growth of both lymphoma and RCC both in vitro and in vivo

The first reported BoNT/E small molecule inhibitor

Novel inhibitor of nucleoside hydrolase (NH)

Selective inhibitor of HsEg5

Potent inhibitor of endopeptidase activity of botulinum neurotoxin type A light chain (rBoNT/A-LC)

Tyrosyl-DNA phosphodiesterase (Tdp1) inhibitor

First-in-class probe of Rad6 function, inhibiting Rad6 function and Rad6-Rad18 interaction in the PCNA ubiquitination cascade

Novel B-Raf(V600E) inhibitor

Novel stimulator of neurogenesis of human hippocampus-derived neural stem cells in vitro and in vivo.

Novel inhibitor of neutral sphingomyelinase 2 (nSMase2) for the treatment of neurodegenerative diseases

Novel free radical scavenger, against light-induced photoreceptor cell damage

Potent anti-HBV agent, targeting the NTCP-APOA1-HBx-Beclin1-mediated autophagic pathway

Novel nonpeptide selective ligand for NTS2

Novel nonpeptide potent and selective partial agonist of the Neurotensin receptor type 2 (NTS2)

Novel Allosteric Modulator of RNA Binding Targeting the N-Terminal Domain of TDP-43

The first NTR-responsive PROTAC, incorporating the caging group on the Von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand, efficiently degrading the EGFR protein and subsequently exert antitumor efficacy

Novel potent STAT3 inhibitor, exhibiting much improved in vivo pharmacokinetic parameters in rats and efficacies against proliferations in multiple cancer cell lines

Novel potent STAT3 inhibitor

Novel potent and selective non-thiazolidinedione partial Peroxisome_proliferator-activated_receptor>PPARγ agonist, acting as an antibiotic effectively against bacterial persisters

Novel potent CDK2 inhibitor

Novel DNA methytransferase inhibitor, be significantly safer and more effective than decitabine in xenograft models of human leukemia and colon cancer

Novel highly potent and selective MEK4 inhibitor

Novel potent activin antagonist

First-in-class activin antagonist, specifically binding to ALK4, which opens a completely new approach to inhibiting the activity of TGF-beta receptor superfamily members

Nucleosidic antibiotic

Novel inhibitor of Helicobacter pylori , targeting H. pylori's respiratory complex I subunit NuoD

Novel Potent Cell-Active Inhibitor of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition

Novel Inhibitor of the NusB-NusE Protein-Protein Interaction with Antibiotic Activity

Novel modulator of the NusB-NusE interaction

p53-MDM2 binding inhibitor; p-Glycoprotein (p-gp) transport substrate; Antitumer agent

Potent and selective p53-MDM2 binding inhibitor

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel translational readthrough-inducing drug (TRID), rescuing the functional full-length protein expression in genetic diseases, such as cystic fibrosis, caused by premature termination codons (PTCs)

Novel potent, orally bioavailable CXCR2 receptor antagonist

Novel potent, orally bioavailable CXCR2 receptor antagonist

Novel phosphodiesterase 4D (PDE4D) inhibitor

Novel Inhibitor of the Cysteine Protease Cathepsin K

Novel potent and selective antagonist of somatostatin receptor subtype SST(3)

Novel BCR-ABL Kinase Inhibitor

Novel dual inhibitor of TORC1 and TORC2

Novel potent Jak2 type 1 inhibitor

Novel potent and selective p53-HDM2 inhibitor

Potent, orally active dipeptidyl peptidase (DPP)-IV inhibitor

Novel peptide deformylase (PDF) inhibitor; Antibacterial

Novel Syk inhibitor

Novel nonpeptide bradykinin B1 receptor antagonist

The first non-peptide somatostatin sst(1) receptor antagonist

Novel focal adhesion kinase (FAK) inhibitor, potently blocking kinase activity of FAK along with Aurora A, activated Cdc42-associated kinase 1 (ACK1), Met, insulin receptor (IR), TrkA, and IGF-1R