Novel blocker of the interaction between FGF1 and FGFRD2 to inhibit cell proliferation, showing potent antiproliferent with less cytotoxicity.

Novel NO-donor, suppressing inflammatory and nociceptive responses

Novel HMG-CoA reductase inhibitor and nitric oxide donor

Cyanogen Bromide adduct of (R)-SCH-12679, a D1 antagonist

Tricyclic antidepressant (TCA), acting as a serotonin–norepinephrine reuptake inhibitor (SNRI) and also having other activities including antihistamine, antiadrenergic, antiserotonergic, anticholinergic, and sodium channel-blocking effects

Novel degrader of steroid receptor co-activator 1 (SRC-1)

Novel potent and highly specific IRAK4 inhibitor

Selective water-soluble gelatinase inhibitor

Potent and selective inhibitor for gelatinases, matrix metalloproteinase 2 (MMP2) and matrix metalloproteinase 9 (MPP9)

Inhibitor of Phosphodiesterase (PDE)-2

Precursor for radiolabeled diltiazem

Major metabolite of loperamide, also used as the precusor for radiolabelled loperamide

Novel G4-DNA ligand, promoting transcription in Gram-positive bacteria and repressing transcription in Gram-negatives

Novel Inhibitor of New Delhi Metallo-β-lactamase-1 (NDM-1)

Negative control compound for Necrostatin-1 related assays

Novel necroptosis inhibitor

Novel inhibitor of caspase-independent cell death with necrotic morphol, distinctly different from apoptosis, autophagy, and necroptosis, displaying strong mitochondrial reactive oxygen species and ONOO- scavenging activity

Non-narcotic analgesic for the relief of acute and chronic pain

Novel Inhibitor of DNA Glycosylases, inhibiting NEIL1 activity

Novel ATP-competitive inhibitor of Nek2 and Nek7

Natural inhibitor of tumor metastasis by upregulating the RNA-binding-protein MBNL2, inducing cell cycle arrest through multiple signaling pathways including RNA binding protein CELF6

Inhibitor of the formation of

Potent natural anti-tumor agent against metastatic colorectal cancer, resulting in cell cycle arrest at the G2/M phase and inducing apoptosis through the dysfunction of mitochondria to trigger intrinsic apoptotic pathway by untargeted metabolomic method,

Natural inducer of autophagy and apoptosis, inhibiting glutamate overexcitation and upregulation of the Wnt/β-catenin signaling pathway

Novel AR inhibitor, being selective for the testosterone stimulated AR-dependent prostate cancer cell

The first potent NAD-driven small molecular inhibitor of TcGAPDH (Trypanosoma cruzi glyceraldehyde 3-phosphate dehydrogenase)

Novel non-peptidic, non-covalent cruzain inhibitor

Human B-type natriuretic peptide, facilitating cardiovascular fluid homeostasis through counterregulation of the renin-angiotensin-aldosterone system, stimulating cyclic guanosine monophosphate, leading to smooth muscle cell relaxation

Anti-inflammatory, antibronchospastic agent

Novel dual Rho Kinase and norepinephrine transporter (ROCK/NET) inhibitor

Novel fluorescent RXR antagonist

Lidocaine metabolite, showing antinociceptive effects, inhibiting GlyT1-mediated glycine uptake

Modulator of the T1007 site, resulting in rapid activation of this transporter and potentiating KCC2 activity

Ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth

Novel potent Trypanosoma brucei Inhibitor

Novel inhibitor of the growth of protozoan parasites, against T. brucei bloodstream proliferation

Novel inhibitor of TbrPDEB1, showing modest inhibition of T. brucei proliferation

Novel neurogenic inducer for converting pluripotent P19 cells into electrophysiologically active neurons

Novel neuroprotectant for Alzheimers disease, showing significant neuroprotection and antioxidative properties, crossing the blood-brain barrier (BBB)

The neurotensin active fragment, eliciting behavioral responses typical of clinically used antipsychotic drugs when administered directly to the brain

Novel potent HDAC6 degrader with promising antiproliferation activity in multiple myeloma (MM) cells

Inhibitor of NFAT-mediated transcription, leading to the suppression of interleukin-2 expression and T cell proliferation, showing immunosuppressive, antidiabetic, and antitrypanosomal activities

First-in-class inhibitor of NF-κB signaling pathway by preventing the maturation of a rate-limiting multiprotein complex necessary for IKK activation

Neutrophil Dysfunction Test Peptide

Novel inhibitor of human cytomegalovirus (HCMV) infection

New generation, topology 2 selective orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist

Novel TRPV1 Antagonist

New generation, topology 2 selective corticotropin releasing factor-1 (CRF-1) receptor antagonist

Brain-permeable dual blocker of neuronal voltage- and ligand-operated calcium channels, acting as chemosensitizer and circumvent the resistance of the plasmodia parasite against chloroquine (CQ) by inhibiting the p-glycoprotein efflux pump and enabling th

Novel cell-permeant probe for the super-resolution imaging of the endoplasmic reticulum in live cells

Novel luciferin analog, enabling both sensitive and highly resolved imaging in vivo

UAMC1110 Conjugate Linker

Selective Inhibitor of Human Lactate Dehydrogenase Isoform A (LDH-A)

Novel inhibitor of the sterol regulatory element binding protein (SREBP)

Antilipidemic agent

Novel fluorescent probe for imaging α4β2* nAChRs

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