Inhibitor of cholecystokinin B receptors (CCK2)

Novel inhibitor of the prostate-specific membrane antigen (PSMA)

Novel inhibitor of the prostate-specific membrane antigen (PSMA)

Novel long-lasting myostatin inhibitor, significantly increasing muscle mass and hindlimb grip strength in Duchenne muscular dystrophic model mice

Novel photoactivatable allosteric ligand for the M1 muscarinic acetylcholine receptor

Novel selective positive allosteric modulator (PAM) at the M1 muscarinic acetylcholine receptor

Novel thapsigargin-based PSMA-activated prodrug, inhibiting the sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump protein

Novel specific and efficient inhibitor of miR-21 expression, inducing a 485% increase in the luciferase reporter signal at 10 μM

Novel inhibitor of microRNA-21 (miR-21)

Novel Miro1 degrader, rescuing dopaminergic neurodegeneration and promoting Miro1 degradation in Parkinson’s Disease fibroblasts

Novel degrader of Miro1 (mitochondrial Rho GTPase 1), reducing Miro1 levels in fibroblasts and stress-induced degeneration of dopaminergic neurons derived from Parkinson's disease (PD) patients, as well as age-dependent neuronal loss and prolongs lifespan

Novel inhibitor of AMA1-RON2 interaction, blocking merozoite invasion from schizont-infected RBCs; Antidepressant; Acetylcholinesterase inhibitor

The first small molecule inhibitor of Mitf-E-box DNA binding with depigmenting activity

Sensitive and specific Raman probe for live cell imaging of mitochondria

Fluorescent probe for measuring the activity levels of erasers of S-palmitoylation, acyl-protein thioesterases (APTs), within mitochondria of live cells

Radiation Mitigator, reducing lipid hydroperoxides and preventing apoptotic cell death

Novel mitochondrial-targeted pan-APT inhibitor

Novel potent antiproliferative mitochondria-targeted OXPHOS inhibitor (IC50=38 nM) in MiaPaCa-2 cells, being more effective than other inhibitors of OXPHOS in MiaPaCa-2 and U87MG cells

Novel selective fluorescent H2O2 probe, tracking the mitochondria of live biological specimens and responds to local fluxes of hydrogen peroxide (H2O2) by a turn-on fluorescence enhancement

Antineoplastic DNA alkylating agent

Specific inhibitor of the cellular inosine-5-monophosphate dehydrogenase (IMPDH); Immunosuppressive agent

Potent and selective PDE4 inhibitor

Novel potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R)

The class III antiarrhythmic agent, blocking HERG, a human cardiac delayed rectifier K+ channel

Novel Dipeptidyl peptidase IV (DPP-4) inhibitor, improving neovascularization by increasing both the number of circulating endothelial progenitor cells and endothelial nitric oxide synthetase expression

Potent and Selective 5-Lipoxygenase Inhibitor

Selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor

Selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor

Novel Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure

Novel renin inhibitor

Potent TRPV1 antagonist

Potent and selective human type-1 5alpha-reductase inhibitor

Novel Selective Androgen Receptor Modulator (SARM)

Novel nonpeptide bombesin receptor subtype-3 agonist

Novel potent muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM)

Novel bombesin receptor subtype-3 (BRS-3) modulator

Novel liver-targeting inhibitor of stearoyl-CoA desaturase (SCD)

Novel agonist of G-protein coupled receptor 40 (GPR40)

Prodrug of raltegravir with enhanced colonic absorption

Novel potent and selective MKK3/6 inhibitor

Novel highly specific, potent, orally bioavailable MKP5 inhibitor

Novel endoplasmic reticulum proteostasis modulator, enhancing insulin production in pancreatic β cells, inhibiting the UPR, alleviating ER stress and protein aggregation, improving intracellular insulin levels and insulin secretion

Novel Inhibitor of Scavenger Receptor BI-mediated Lipid Uptake

Selective inhibitor of Myosin Light Chain Kinase (MLCK)

Novel IKK2 inhibitor, decreasing NF-κB activation and down-regulating the expression of a number of inflammatory proteins

Novel potent DNA binding agent, stabilizing topoisomerase-dependent cleavage, demonstrating exceptional efficacy against a number of murine and human tumor models

Second generation 5-LO inhibitor, blocking the production of leukotrienes

Novel selective and potent inhibitor of recombinant h12/15-LOX and cellular mouse 12/15-LOX (m12/15-LOX)

Potent and selective competitive inhibitor of human epithelial 15-lipoxygenase-2 (15-LOX-2)

Potent and selective mixed-type inhibitor of human epithelial 15-lipoxygenase-2 (15-LOX-2)

Novel potent inhibitor of EBOV infection

Novel Inhibitor of Human Cytomegalovirus

Potent inhibitor of STAT3 and Akt signaling

Novel dual JAK/Src kinase inhibitor, suppressing growth of diverse cancer cells

Novel inhibitor of human cytomegalovirus (HCMV) infection

Potent agonist of TRPML channels specifically activating lysosomal ML1 currents

Novel potent and selective MALT-1 protease inhibitor, showing improved solubility and permeability in comparison with MLT-748

Novel potent IDO1 inhibitor, showing low cytotoxicity and higher selectivity for IDO1 over TDO enzyme

Novel potent and selective HDAC8 inhibitor

Novel potent and selective HDAC8 inhibitor

Novel potent and selective HDAC8 inhibitor

Novel highly potent and selective MMP13 inhibitor

Negative allosteric modulator (NAM) ligand for the mGlu5 receptor

Novel Mmpl3 inhibitor, indirectly blocking translocation of Trehalose Monomycolates across the IM

Highly water-soluble antifibrotic agent, reducing the profibrotic phenotype induced in vitro in primary human fibroblasts and ameliorating bleomycin-induced pulmonary fibrosis in vivo

Novel inhibitor of lanosterol-14-alpha-demethylase (TcCyp51)

The first small-molecule anti-plasmodial agent, disrupting rosetting, simultaneously restoring microcirculation and reduce parasite load

Novel antimalarial agent against asexual stages of P. falciparum

Novel potent Plasmodium lactate transporter PfFNT

Novel MEP pathway-targeting antimalarial agent

Novel antimalarial agent with increased efficacy against one or more pfatp4 mutated clones

Novel Inhibitor of Plasmodium falciparum

Novel antischistosomal agent against chronic S. mansoni infection

Novel antischistosomal agent against chronic S. mansoni infection

Novel antimalarial agent with increased efficacy against one or more pfatp4 mutated clones

Novel inhibitor of Plasmodium falciparum, killing both blood- and sexual-stage P. falciparum parasites

Novel antimalarial agent against Plasmodium falciparum

Novel antimalarial agent, targeting P. falciparum farnesyltransferase PfFT, showing remarkable growth inhibition with EC50 value of 0.4 µM and presenting good selectivity index (SI > 250)

Selective allosteric inhibitor of Plasmodium Kinesin-5

Novel potent inhibitor of P. falciparum asexual blood stages, inhibiting heme detoxification

Novel potent broad antiparasitic agent against intracellular Leishmania amastigotes, Trypanosoma brucei, and Plasmodium falciparum

First-in-class acetyl-CoA synthetase (AcAS) inhibitor, showong single digit nanomolar in vitro activity against P. falciparum and P. vivax clinical isolates, and potently blocking P. falciparum transmission to Anopheles mosquitoes

Novel anticancer agent, inducing apoptosis, inhibiting migration and invasion

Novel highly potent and selective MNK1/2 kinases inhibitor

Potent and selective Mnk2 inhibitor

Cell-permeable superoxide dismutase (SOD) mimetic

Novel inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity

Momelotinib (dihydrochloride) is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of Hepcidin expression and increased availability of iron for erythropoiesis. Momelotinib (dihydrochloride) can reduce transfusion burden and spleen enlargement caused by myelofibrosis, showing potential value in research and application within the field of myelofibrosis.

Natural antioxidant and antidiabetic agent

Novel iminosugar, downregulatiing the interferon γ receptor by dengue virus

Natural potent antioxidant agent

Natural analogue of (-)-gambogic acid acting as a potent inhibitor of global predominant MRSA USA300

Potent dopamine antagonist with high affinity to the D2, D3, and D4 receptors, and with moderate affinity for the 5-HT2 receptors

Natural antibacterial, antileishmanial, and antifungal agent

Potent and Specific PDE10A inhibitor

Novel mixed kappa-delta opioid receptor agonist with anti-cocaine properties and reduced side-effects in rats

Novel potent and selective microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor

Novel anti-cancer agent, being more potent and safer than conventional indomethacin

Novel selective class IIb histone deacetylase inhibitor (HDACi), dose-dependently decreasing the viability of Acanthamoeba trophozoites

Potent and selective COX-2 inhibitor

Specific estrogen receptor α (ERα) antagonist

Novel main protease (Mpro) inhibitor, inhibiting MHV-A29, HCoV-229E, FOPV replication, and SARS-CoV-2 viral cell entry

Novel Mps1 Kinase Inhibitor

Novel inhibitor of MPS1

Novel tubulin polymerization inhibitor

Novel Dual HDAC6 and Tubulin Inhibitor, Displaying Anti-tumor Ability in Human Cancer Cells

Novel mitochondrial permeability transition pore (mPTP) inhibitor

Novel potent and selective antagonist of GluN2A-containing NMDA receptors

Novel highly potent and selective 5-HT2C agonist

Novel, potent inducer of apoptosis via the MAP kinase pathways. Inhibitor of several kinases including the tyrosine kinase FLT3-ITD

Novel inhibitor of the main protease (Mpro) of SARS-CoV-2

Novel positive allosteric modulator (PAM) of mas-related G protein-coupled receptor X1 (MRGPRX1), reducing behavioral heat hypersensitivity in humanized MRGPRX1 mice, demonstrating the therapeutic potential in treating neuropathic pain

Activator of MrgX1 receptor signaling

Novel peripheral CB1R antagonist, being highly biased toward inhibiting CB1R-induced β-arrestin-2 (βArr2) recruitment over G-protein activation

Novel potent and selective RORγT inhibitor, showing no appreciable activity against a panel of related nuclear hormone receptors

Novel potent RORγT inhibitor

Novel potent and selective RORγT inhibitor, showing no appreciable activity against a panel of related nuclear hormone receptors

Novel selective and reproducible inhibitor of DNA synthesis in E. coli JL553

Selective enhancer of the ATP effects at fast desensitizing P2X (P2X1 and P2X3) receptors

Potent P2Y14 receptor agonist

Selective P2Y6 agonist

Selective P2Y2 agonist

Potent P2Y6 agonist

Potent and selective P2Y6 receptor agonist

Novel highly potent human CD73 inhibitor (K i = 0.673 nM)

Novel potent antagonist of P2Y 14 receptor (P2Y 14 R) (IC 50 ~20 nM at hP2Y 14 R/mP2Y 14 R)

Novel potent P2Y14 Receptor Antagonist (IC 50 , 15 nM)

Bitopic fluorescent antagonist of the A2A adenosine receptor

Novel highly selective A1 adenosine receptor (A1AR) agonist

Novel Partial Agonist of Human and Mouse A3 Adenosine Receptors (Ki = 10.9/17.8 nM, at human/mouse A3AR)

Novel highly potent A3 adenosine receptor (A3AR) antagonist with Kd values (nM): 0.55 (human), 3.74 (mouse), and 2.80 (rat)

Potent inhibitor of TANK-binding kinase-1 (TBK1)/IKKepislon kinases

Novel inhibitor of Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor

Novel, selective, orally bioavailable, negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5)

Inhibitor of DNA damage repair

Novel inhibitor of DNA damage repair

Novel inhibitor of Human p53 and CREB Binding Protein (CREBBP) interaction

Novel potent and selective SETD8 inhibitor

Mitochondrial tRNA-specific modification, regulating efficient mitochondrial translation and energy metabolism in mammals

Novel potent tankyrase (TNKS) inhibitor (EC 50 : 2 nM)

Novel inhibitor of SLC16A3

Novel potent and selective PI3Kδ inhibitor

Potent TRPV1 agonist

Novel potent broad-spectrum metallo-β-lactamase (MβL) inhibitor, inhibiting the MβLs NDM-1, VIM-2, ImiS, and L1

Novel BBB permeable potent MT1 and MT2 ligand (MT1, Ki = 0.031 nM; MT2, Ki = 0.070 nM) with good metabolic stability in human hepatic microsomes

Novel antituberculosis agent. targeting the respiratory chain of Mycobacterium tuberculosis (Mtb) and being effective against multi drug resistant (MDR) Mtb

Novel minimized theta-defensin, being highly effective against CRE pathogens K. pneumoniae and E. coli in vivo, significantly enhancing survival by promoting rapid host-mediated bacterial clearance and by modulating pathologic cytokine responses, restorin

Novel resveratrol-based multitarget-directed ligand, cellularly activating the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibiting both hMAO-B and QR2 (IC 50 s = 8.05 and 0.57 μM), and promoting hippocampal neurogenesis

Selective antagonist of melanocortin-4 receptor (MC4R)

Novel Mithramycin A (MTM) 2'-oxime (MTMox) conjugate, displaying an 11-fold increase in plasma exposure and improved efficacy in an Ewing sarcoma xenograft

Novel, potent, and selective brain-penetrant ATP-competitive mTOR inhibitor

Novel potent dual inhibitor of mTOR and HDAC1

Novel selective inhibitor of mTORC1, yielding potent inhibition of glucose uptake

Novel selective mTORC1 inhibitor, directly targeting class I glucose transporters

Novel mTOR inhibitor, exhibiting potent anticancer activities against four tumor cell lines, including MCF-7, HeLa, MGC-803, and C6, inducing cell death via apoptosis by targeting both mTORC1 and mTORC2 within cells and arrests the cell cycle of HeLa at t

Novel mitochondria-targeted photoactivatable real-time probe, being phototriggered by either UV (one-photon) or NIR (two-photon) light to form a fluorescent coumarin product and facilitate the release of drug payload

Useful probe in the mapping of membrane proteins, such as ion channels and transports proteins, as well as enzymes and receptors.

Useful probe in the mapping of membrane proteins, such as ion channels and transports proteins, as well as enzymes and receptors.

Novel potent multitarget ligand

Novel potent MurA inhibitor

Novel potent and selective MCL-1 inhibitor

Novel potent mutant IDH1 R132H inhibitor

Novel potent and selective cathepsin K (Cat K) inhibitor

CNS-penetrant, selective restorer of injury- or disease-induced overproduction of proinflammatory cytokines towards homeostasis. Selective suppressor of beta amyloid (Aβ)-induced glia proinflammatory cytokine production

Novel GPR119 agonist with Anti-Diabetic Efficacy in db/db Mice

Novel mitophagy activator

Major thiol in most actinomycetes involved in mycothiol biosynthesis and mycothiol-dependent enzymes such as mycothiol-dependent formaldehyde dehydrogenase and mycothione reductase

Novel inhibitor of the protein-protein interactions between the bHLHZip proteins c-Myc and Max

Novel inhibitor of the protein-protein interactions between the bHLHZip proteins c-Myc and Max

Novel inhibitor of zinc finger DHHC domain-containing (zDHHC) enzymes

Myotoxin II fragment

Novel potent, reversible and uncompetitive inhibitor of actin-stimulated ATPase activity of myosin V

Novel inducer of apoptosis in a Myc-dependent manner, inhibiting Myc-driven transformation and disrupting MYC-Max interaction

Inhibitor of the chaperonin activity of HSP60, correlating to LONP and LRP130 aggregation

Bacterial RNA polymerase (RNAP) inhibitor

Novel potent and selective PROTAC degrader of BRD3/4

Competitive inhibitor of both SPHK1 and SPHK2

Glucokinase activator (GKA)

Novel RNA labeling probe through both metabolic and enzyme-assisted manners

Deuterium labeled m6A used in important m6A physiological pathways related studies

Alkylating agent, forming DNA adducts at the C-8 position in guanine, resulting in single strand breaks, demonstrating carcinogenic action

Delta-9-tetrahydrocannabinol (THC)/cannabidiol (CBD) combination for the treatment of multiple sclerosis (MS)-related moderate to severe spasticity

Derivative of loline

Novel antiviral agent against the replication of influenza virus A/H3N2 subtype in Madin-Darby canine kidney (MDCK) cells

Coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage

Electron donor and cofactor for many redox enzymes including nitric oxide synthetase

Partial estrogen antagonist, inhibiting angiogenesis in some tissues by blocking the effects of fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF), inducing oxidative stress, protein kinase C and calcium signaling

Novel potent full agonist for orexin receptor

Novel highly selective antibacterial agent against Propionibacterium acnes

Mixed agonist/antagonist opioid modulator, binding with high affinity to the MOR and KOR, and having relatively low affinity for the DOR

Novel fluorescent probe for detection of endogenously produced Naph-O2˙– in living cells and tissues

Novel repeat-structure-specific DNA ligand, specifically binding slipped-CAG DNA intermediates of expansion mutations

Triple reuptake inhibitor

Novel Gut-Restricted Inhibitor of Intestinal Sodium-Dependent Phosphate Transport Protein 2b (NaPi2b) for the Treatment of Hyperphosphatemia

Antagonist of alpha-2 adrenergic receptors and inhibitor of the neuronal uptake of norepinephrine

Inhibitor of extrinsic and intrinsic thrombin generation, inhibiting clot-bound and free (fluid-phase thrombin)

Activator of the transient receptor potential vanilloid (TRPV) channels TRPV1 and TRPV4

Natural DnaE1 blocker, inducing a DNA damage response in Mycobacterium tuberculosis (Mtb) and inhibiting growth by blocking the replicative DNA polymerase, DnaE1

Potent suppressor of inducible nitric oxide synthase (iNOS; NOS II)

Novel selective NaV1.1 inhibitor, reducing visceral hypersensitivity