Novel inhibitor of COX and neutrophil migration

Distinct IKur blocker

Unique topoisomerase inhibitor, showing significant growth-inhibitory effects against large-cell lung cancer (Lu-116) and gastric adenocarcinoma (St-4)

Novel Potent and Selective A3 Antagonist

Novel degrader of CRABP proteins

Novel highly potent (EC 50 = 1.6 nM) aryl hydrocarbon receptor (AhR) agonist with high affinity (K i = 88 nM)

Novel Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitor, showing a remarkably low toxicity both in vitro and in vivo and increasing the function of regulatory T cells (Tregs) at well-tolerated concentrations

Novel selective HDAC6 inhibitor

Novel PP2A ligand, protecting against memory impairment and focal cerebral ischemia in mice

Novel neuroprotective agent

Novel, potent, selective, and BBB-permeable P2X7 antagonist

Novel highly potent, orally bioavailable hepatitis C virus (HCV) entry inhibitor

First-in-class iodothyronine deiodinase type 3 (DIO3) inhibitor, demonstratig attenuated cell counts, induction in apoptosis, and a reduction in cell proliferation in DIO3-positive HGSOC cells (OVCAR3 and KURAMOCHI)

Selective inhibitor of the funny channel pacemaker current (If) in the sinoatrial node in a dose-dependent fashion, resulting in a lower heart rate and thus more blood to flow to the myocardium

The first Ang IV-analogue being able to abolish IRAP-availability completely at the cell surface in vitro

Prodrug of QVO, being quickly converted to QVO in mice and rats following administration, ameliorating hyperglycemia, and suppressing hepatic gluconeogenesis and activating AMPK signaling pathway in the liver tissues

Novel, orally available soluble guanylate cyclase (sGC) stimulator with once-daily dosing potential for the treatment of cardiovascular diseases

Novel WNT inhibitor, suppressing cytoplasmic and nuclear biochemical markers of WNT signaling in cultured cells, inhibiting recombinant TNKS activity, or WNT fatty acylation

Novel WNT inhibitor, suppressing cytoplasmic and nuclear biochemical markers of WNT signaling in cultured cells, inhibiting recombinant TNKS activity, or WNT fatty acylation

Novel potent noncleavable proteolysis targeting chimeric (PROTAC) for TrkC degradation in metastatic breast cancer cells

Novel potent and cleavable proteolysis targeting chimeric (PROTAC) for TrkC degradation in metastatic breast cancer cells

Potent and selective agonist of human somatostatin receptor 4 (sst4), reducing mechanosensitivity of peripheral nerve afferents and spinal neurons in an inflammatory pain model

Novel highly potent JAK1-selective inhibitor, exhibiting excellent selectivity over JAK2, JAK3, and TYK2 (IC 50 : JAK1 0.145 nM; JAK2 2.94 nM; JAK3 2.31 nM; TYK2 8.17 nM)

Novel JAK1 inhibitor

Novel selective Jak2 inhibitor, demonstrating a time-dependent knock-down of pSTAT5, a downstream target of Jak2

Novel irreversible selective JAK3 inhibitor through the covalent interaction with a Jak3 active-site cysteine

Novel irreversible selective JAK3 inhibitor through the covalent interaction with a Jak3 active-site cysteine

Novel irreversible selective JAK3 inhibitor through the covalent interaction with a Jak3 active-site cysteine

Novel Selective JAK3 Inhibitor with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

Novel Selective JAK3 Inhibitor with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

Novel potent JAK1/2/3 inhibitor

Novel potent JAK1/3 inhibitor, targeting JAK3 and JAK1 with IC 50 at 3nM and 5nM, respectively

Novel positive allosteric modulator of AMPA receptor

Novel anti-triple-negative breast cancer (anti-TNBC) agent with a high selectivity against BC cells over normal human cells, downregulating phosphatidylinositide 3-kinase (PI3K)/Akt pathway by suppressing protein-tyrosine phosphatase 1B (PTP1B) expression

Novel fluorogenic yellow fluorescent dye for use in self-labeling tag systems

Novel mitophagy inducer with therapeutic potential for Parkinson's disease, acting as light chain 3 (LC3) interactors, similar to cardiolipin or ceramide, triggering mitophagy via Pink1/Parkin

Novel Inhibitor of Jumonji AT-Rich Interactive Domain 1B (JARID1B) Histone Demethylase

Natural naphthyridine alkaloid

Potent inhibitor of the proliferation of PC3 prostate carcinoma cells

Natural Inhibitor for Protein−Protein Interaction of the Homodimer of Proteasome Assembly Factor 3

Natural radical scavenger, inhibiting L-glutamate toxicity in neuronal hybridoma N18-RE-105 cells

Inhibitor of renal transporters OAT1 and OAT3; Antihepatitis agent as a substrate for intestinal PEPT1

Natural anti-inflammatory agent, showing potential for the treatment of inflammatory bowel disease (IBD)

Metabolite of JBSNF-000088

Novel RORα activator, diminishing diethylnitrosamine-induced acute liver injury and repressing transcriptional expression of APPs such as CXCL1 and LCN2 in mice

Novel dose-dependent inhibitor of ABHD6

JCP174 analog used for affinity purification of labeled targets

Negative control of JCP174

Novel dose-dependent inhibitor of ABHD6

Covalent dual inhibitor of DPAP1 and DPAP3

Covalent dual inhibitor of DPAP1 and DPAP3

Novel potent inhibitor of Mpro

Novel irriversable serine hydrolases inhibitor

Peripheral Selective CB1 Receptor Antagonist

Novel apoptosis inducer, significantly inhibiting tumor growth in the xenograft model

Novel human flap endonuclease 1 (FEN1) inhibitor with in vitro inhibition of flap cleavage activity as well as cytotoxic activity against a colon cancer cell line, DLD-1

Novel inhibitor of the heat shock protein 70 (Hsp70) with anti-proliferative activity in breast and prostate cancer cells

Novel type I Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, binding preferentially to unphosphorylated IRAK4

Novel Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, binding preferentially to unphosphorylated IRAK4

Novel Ras homologous A (RHOA) inhibitor, potently inhibiting cell viability and migration/invasion of gastric cancer (GC) cell lines, and mouse xenografts, diversely expressing RHOA, binding affinity for RHOA was >140-fold greater than Rhosin, a nonclinic

Novel specific dual inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2) and cyclin-dependent kinase 1 (CDK1), targeting cell cycle progression and angiogenesis

Potent non-nucleoside inhibitor of HIV-1 reverse transcriptase (NNRTIs)

Novel potent GHS-R1a agonist (EC50 (Ca ): 1.6 nM), significantly stimulating GH secretion

Novel ghrelin receptor (GHS-R1a) antagonist [IC 50 (affinity): 5 nM IC 50 (Ca ): 60 nM]

Novel partial inverse agonist of GHS-R1a (K i = 3 nM, EC 50 = 70 nM, Emax = −37%)

Novel inhibitor of viral protease function, suppressing Zika virus Infection both In vitro and In vivo

Novel Potent NS4B Inhibitor for the Treatment of Dengue Virus Infection

Novel Potent Human Adenovirus Inhibitor, showing improved anti-HAdV activity (IC50 = 0.27 μM), significantly decreasing cytotoxicity (CC50 = 156.8 μM), and lowering in vivo toxicity (maximum tolerated dose = 150 mg/kg in hamster) as compared with niclosam

Novel potent and selective IRAK1 degrader, effectively degraded cellular IRAK1 protein with a DC50 of 3 nM in HBL-1 cells

Novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase

Vascular endothelial growth factor receptor-2 (VEGF-2) kinase inhibitor

Estrogen receptor ESR1 agonist

Novel Positive Allosteric Modulator of the α7 Nicotinic Acetylcholine Receptor

Selective delta opioid receptor agonist as a potent and efficacious antihyperalgesic agent

Novel EthR inhibitor, boosting antituberculous activity of ethionamide

Selective androgen receptor modulator with minimal prostate hypertrophic activity stimulating sexual behavior in female rats

Histamine H3 receptor antagonist and serotonin reuptake inhibitor

Novel potent, selective, and systemically active positive allosteric modulator (PAM) of mGlu2-receptors

Novel Adenosine A 2A /A 1 Antagonist With Efficacy In Preclinical Models of Parkinson's Disease

Negative control for JNJ-40068782

JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor.

Negaive control for JNJ-42396302

Novel potent, orally active LTA4H inhibitor

Novel inhibitor of PDE10A

Novel ago-PAM for the metabotropic glutamate receptor subtype 2 (mGluR2)

Novel inhibitor of respiratory syncytial virus (RSV), binding the RSV F glycoprotein and inhibiting membrane fusion

Negative control for JNJ-54119936

Novel TARP γ-8 Selective AMPAR Negative Modulator

Selective DGAT1 inhibitor

Selective DGAT2 inhibitor

Novel cysteine-reactive covalent ligand, selectively targeting C377 of PPP2R1A to impair breast cancer signaling, proliferation, and in vivo tumor growth

Novel SMAC mimetic, sensitizing non-small cell lung cancers to multiple chemotherapy agents in an IAP-dependent but TNF-α-independent manner

Non-toxic radioprotector GS-nitroxide, improving hematopoiesis in long-term bone marrow cultures (LTBMCs)

Non-toxic anti-relapse agent, acamprosate

Novel selective inhibitor of nuclear translocation of IKKα as the most potent synthetic gibberellin against cancer-derived cell lines, displaying no cytotoxicity in cells derived from noncancerous sources (HEK 293T, HS 578BST, HS 888Lu, HS 895Sk, HUVEC)

Novel inhibitor of CD4-gp120 binding, blocking the binding of the HIV-1 envelope glycoprotein gp120 to the CD4 receptor

Novel specific inhibitor of Fusarium myosin I; Fungicide

Novel antitubercular agent, inhibiting InhA and FAS-II pathway

Novel potent antitubercular agent, inhibiting InhA and FAS-II pathway

Novel ERK inhibitor, alleviating IMQ-induced mice skin lesions through ERK/IL-17 signaling pathway

Novel RORγ

Cytokine release inhibitor, inhibiting production of IL-1ß, IL-8, IL-6, IL-10 and TNFalpha

Novel nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase

Novel orally active and selective transient receptor potential vanilloid 1 (TRPV1) antagonist

Novel inhibitor of urate transporter 1 (URAT1)

Novel K(ATP) channel opener

Specific inhibitor of factor Xa

Novel live-cell peobe of voltage-dependent structural changes of voltage-gated Kv2.1 channels

Novel neuroprotective agent, improving cognitive performances in a transgenic mouse model of AD

Novel BET selective inhibitor, targeting BRD4

Potent cannabinoid (CB) receptor agonist

Novel potent stimulator of glucagon-like peptide-1 (GLP-1) secretion in vitro, also potently stimulating Ca(2+) influx through TRPA1 cation channels, being one of the most potent non-electrophilic TRPA-1 channel agonists

Novel potent mitochondrial pyruvate carrier (MPC) inhibitor to treat hair loss

Novel BH3 α-helix mimetic, inducing apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak

High-affinity partial agonist of the vanilloid receptor

Potent TRPV1 agonist

Potent vanilloid receptor (VR1) agonist

Selective modulator of GABAA receptors containing the α5 subunit

Novel β-Glucocerebrosidase modulator, promoting dimerization of β-glucocerebrosidase and revealing an allosteric binding site, stabilizing wild-type and N370S mutant GCase and increases GCase abundance in patient-derived fibroblast cells

Novel irreversible β-Glucocerebrosidase modulator

Inhibitor of all three monoamine transporters

Potent, highly selective, and irreversible ABHD6 Inhibitor

Novel potent and selective inhibitor of PIM kinases

Novel dual CLK1 and CLK3 inhibitor

Novel inhibitor of peptidoglycan synthesis targeting the lipid II precursor

Novel antagonist for proteinase-activated receptor 2 (PAR2)

Novel norditerpenoid inhibitor of testosterone-5α-reductase

Novel inhibitor of the interaction of the N-terminally truncated RXR

Novel inhibitor of the interaction of the N-terminally truncated RXR

Natural anti-inflammatory agent, inhibiting the NF-κB-mediated transactivation of a luciferase reporter gene, IL-6 production, and COX-2 expression

Natural anti-inflammatory agent, inhibiting the NF-κB-mediated transactivation of a luciferase reporter gene, IL-6 production, and COX-2 expression

Novel mGlu4 ligand

Novel antimalarial agent, providing protection to malaria-infected mice

Antibiotic, binding within the mRNA channel of the 30S subunit and inhibiting protein synthesis

Novel activator of hERG1 potassium channels, blocking native and recombinant hERG1 channels at high voltages, but activating them at low voltages

Novel histone deacetylase inhibitor

Novel Plk1 PBD inhibitor, showing a remarkable in vitro anticancer effect by inducing Plk1 delocalization, mitotic arrest, and apoptosis in HeLa cells

Selective inhibitor of Protein_kinase_D1>protein kinase D (PKD); Inhibitor of cell adhesion and HIV; Inhibitor of herpes simplex virus type 1 replication

Novel highly potent dual amylin and calcitonin receptor agonist (DACRA), showing long-lasting improvement of food preference and body weight loss

Novel ADAM12 and MMP inhibitor, ameliorating cardiac function in a transverse aortic constriction (TAC) model by inhibiting the proteolytic activation of HB-EGF signaling, exerting its antidiabetic effect by ameliorating insulin sensitivity through the in

LTB4 inhibitor for the treatment of b-cell leukemias and lymphomas, potently inhibiting histamine, platelet activating factor,and 5-lipoxygenase

Highly specific transglutaminase 2 (TG2) inhibitor

Dual PDE3/4 inhibitor

Novel potent and Subtype-Selective Positive Modulator of KCa2 Channels

Potent PDZ domain peptide inhibitor that rescues CFTR activity

Novel selective KDM4C inhibitor

Novel KDM4 inhibitor

Potent and selective KDM5 inhibitor

Potent and selective KDM5 inhibitor

Phosphate acceptor peptide substrate for cAMP-dependent protein kinase

Potent and selective adenosine A1 antagonist with renal protective and diuretic activities

Novel and potent factor Xa inhibitor

Novel potent peptide dual agonist of opioid/neurokinin 1 receptor

Novel Pim-1 kinase Inhibitor, dose-dependent decreasing the viability of LS174T and HCT-116 cells

Inhibitor of Aβ-induced inflammation

Novel anti-inflammatory and antioxidant agent, significantly decreasing blood glucose, triglycerides, and cholesterol and increased insulin

Novel FGFR2 inhibitor, enhancing the chemosensitivity of drug-resistant gastric cancer cell lines

Novel KIF18A inhibitor, causing significant mitotic arrest in vivo, binding at the interface of KIF18A and tubulin

Novel Max-binding modulator, attenuating Myc-driven transcription and stabilizing the Max homodimer

Novel inducer of the ISG54 promoter, causing IRF-3 translocation

Novel potent and selective inhibitor of kir1.1 channels

Novel ROS1 kinase inhibitor

Novel ROS1 kinase inhibitor

Novel TRPV1 antagonist

Novel specific inhibitor of MYC

Potent D3 receptor antagonist with high 5-HT1A receptor affinity

Novel NF-κB inhibitor and lipopolysaccharide (LPS)-induced nitric oxide production inhibitor

Self-assembling peptide, forming a hydrogel matrix to support growth of cells in the presence of an ionic solution, enhancing chondrogenic differentiation of bone marrow stromal cells (BMSCs)

Novel inhibitor of 70S ribosome by obstructing the peptide exit tunnel

First-in-class inhibitor of Kallikrein-related peptidase 6 (KLK6), promoting the differentiation of OPCs into mature oligodendrocytes in vitro

First-in-class inhibitor of Kallikrein-related peptidase 6 (KLK6), promoting the differentiation of OPCs into mature oligodendrocytes in vitro

Novel antibiotic sensitizer, promoting the rearrangement of the bacterial membrane that enables hydrophobic antibiotics to permeate, strongly sensitizing Gram-negative bacteria to linezolid (Lzd), rifampicin (Rif), or clarithromycin (Clr)

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CDK9 inhibitor, inhibiting transcription of GAPDH

Selective S1P3 agonist

Novel inhibitor of the BfrB-Bfd complex, binding BfrB in the P. aeruginosa cytosol, blocking the BfrB-Bfd interaction and inhibiting iron mobilization from BfrB, resulting in cytosolic iron limitation that is manifested in a pyoverdine hyperproduction phe

Novel inhibitor of the BfrB-Bfd complex, binding BfrB in the P. aeruginosa cytosol, blocking the BfrB-Bfd interaction and inhibiting iron mobilization from BfrB, resulting in cytosolic iron limitation that is manifested in a pyoverdine hyperproduction phe

Novel BACE1 inhibitor with a non-acidic heterocycle at the P1' position

Novel Potent Hematopoietic Prostaglandin D2 Synthase (H-PGDS) Inhibitor

Novel Potent and Selective EP4 Agonist

Novel inhibitor of amyloid-

Novel inhibitor of amyloid-β aggregation, ameliorating the neurodegenerative disorder

Novel enhancer of cGMP activity; Aortic smooth muscle relaxant

Novel enhancer of cGMP activity; Aortic smooth muscle relaxant

Natural anti-TNBC agent, significantly suppressing the triple-negative breast cancer (TNBC) tumor growth without causing side effects

Novel non-chain terminating nucleoside analog anti-HIV inhibitor

Novel selective, orally bioavailable, PAK4 allosteric modulator against triple negative breast cancer

Novel potent antimicrotubule agent, exhibiting potent cytotoxicity against HT-29 cells by strongly binding to tubulin and inducing microtubule depolymn.

Potent antimicrobial peptide against gram-positive and gram-negative bacteria and relatively high LPS-neutralization activity

Novel enteroviral replication inhibitor through a non-capsid binding mode with EC 50 values of 2.5, 2.2, and 3.7 μM against hRV B14, A21, and A71, respectively, targeting the replication stages in the virus

Novel KATP channel opener, exerting cardioprotective effects by opening SarcKATP channels in rat models of ischemia/reperfusion-induced heart injury

Novel irreversible inhibitor of KRAS(G12C)

Novel specific inhibitor of oncogenic KRAS4b signaling, stabilizing the KRAS4b-PDEδ complex and remarkably decreasing tumor size and triggered apoptosis of tumor cells

Novel stabilizer of the KRAS4b-PDEδ complex, decreasing the proliferation of colorectal cancer cells, and increasing apoptosis via decreased activation of oncogenic KRAS4b signaling

Novel potent multi-kinase inhibitor, targeting Ron, Flt3 and TrkA as well as c-Met

Selective novel inhibitor of c-Met receptor tyrosine kinase with anticancer activity.

Novel potent, non-toxic, blood-brain barrier crossing, α5-GABA A R preferring ligand, enhancing a chloride-anion efflux that induces mitochondrial membrane depolarization and in response, TP53 upregulation and p53, constitutively phosphorylated at S392, c

Potassium channel opener

Topo II inhibitor, exhibiting cytotoxic effects against tumour cells

Novel neutrophil elastase (NE) inhibitor, decreasing expression of TGF-ß Signal Related Genes