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

Highly potent and selective antagonist for the AMPA receptors, exhibiting good neuroprotective effects in vivo

Novel highly selective β3-adrenoceptor agonist being developed for the treatment of diabetes and obesity

Novel Potent and Selective VIPR2 Antagonist, Counteracting Cognitive Decline in a Mouse Model of Psychiatric Disorders

Novel inhibitor of the permeability transition pore (PTP)

Selective ligand of the sigma-1 receptor

Ligand of the sigma receptor

Ligand of the sigma receptor

Novel inhibitor of transcriptional activity in Chlamydia trachomatis

Novel, highly potent, and metabolically stable peptide inhibitor of syntenin, Inhibiting Glioblastoma

Novel modulator of kinesin spindle protein (KSP)/Eg5, activating KSP-catalyzed ATP hydrolysis in the absence of microtubules yet inhibiting microtubule-stimulated ATP hydrolysis by KSP

Potent and selective inhibitor of ABHD6

TXA2/prostaglandin endoperoxide receptor antagonist

Thyroid hormone receptor β (TRβ) selective agonist

Hypoxic cell radiosensitizer

Novel selective DYRK1A inhibitor

Novel potent and selective inhibitor of Hsp90β

Novel protein farnesyltransferase inhibitor

Potent Kv1.5 inhibitor

Novel neuroprotectant, inhibiting Kv2.1-syntaxin molecular interaction

Novel Preferable Phosphodiesterase 4B (PDE4B) Inhibitor, Decreasing Cocaine-Mediated Reward Properties in Vivo

Ras destabilizer, targeting the Wnt/ß-catenin pathway and inhibiting development of metastatic colorectal cancer

Novel inhibitor of the Wnt/ß-catenin pathway, binding directly to the regulators of G-protein signaling domain of axin, initiating ß-catenin and Ras degradation through enhancement of the ß-catenin destruction complex activating GSK3ß, effectively suppres

Selective T-type Ca(2+) channel blocker with anti-proliferative effects against various cancer cells

Potent inhibitor of LpxC and lipid A biosynthesis

Nonpeptide agonist of angiotensin AT1 receptor

Novel cell-permeable attenuated cationic amphiphilic lytic (ACAL) peptide, efficiently bring immunoglobulin G (IgG) and other functional proteins into cells

Novel Migration Inhibitory Factor (MIF) inhibitor, binding at the allosteric and tautomerase sites, blocking MIF's tautomerase CD74 receptor binding, and pro-inflammatory activities

Novel γ-secretase modulator photoaffinity probe, identifying distinct allosteric binding sites on presenilin that can be exploited to reduce levels of pathogenic Aβ species

Novel inhibitor of α-synuclein amyloid aggregation for the treatment of Parkinson's disease

Novel inhibitor of the TWEAK-Fn14 signaling cascade

Novel potent inhibitor of human pancreatic cancer cells

Potent leukotriene inhibitor

Blocker of the activity of human neutrophil elastase (NE), human proteinase-3, human macrophage metalloelastase, mouse macrophage metalloelastase and Pseudomonas aeruginosa elastase

Novel partial agonist of the benzodiazepine receptor

Potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase (PMNL-E)

HIV protease inhibitor

Novel partial agonist of muscarinic M1 receptors

HIV-1 non-nucleoside reverse transcriptase inhibitor

Inhibitor of Human Immunodeficiency Virus Type 1 (HIV-1)

Inhibitor of Strand Transfer, Preventing Integration and Inhibiting HIV-1 Replication in Cells

Inhibitor of the KCNQ1 channel

Potent glycoprotein IIb/IIIa inhibitor

Ras farnesyltransferase inhibitor, inhibiting in p70(s6k) phosphorylation in mammary tumors, inducing tumor regression in transgenic mice by mediating alterations in both cell cycle control and apoptosis

Dual ET(A)/ET(B) endothelin receptor antagonist

Class III antiarrhythmic agent, selectively blocking the slowly activating cardiac delayed rectifier potassium current Iks

Potent and selective agonist of the human beta3 adrenergic receptor

L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively.

Novel HIV-1 integrase strand transfer inhibitor (INSTI), stabilizing an integrase-single blunt-ended DNA complex

Chemically-modified forskolin with greater stability and water solubility than the parent compound

Novel inhibitor of HIV-1 and SIV integrase

The first organ-selective thyromimetic, lowering plasma low density lipoprotein (LDL) cholesterol and raising plasma high density lipoprotein (HDL) cholesterol levels

Adenosine A1 receptor antagonist, reducing allergic responses to house dust mite in an allergic rabbit model of asthma, improving survival and protecting the kidney in a rat model of cecal ligation and puncture induced sepsis, also improving survival and

Top1mt inhibitor, targeting mitochondrial DNA

Glutamate receptor antagonist and radical scavenging agent

Novel Peptide Deformylase Inhibitor against Streptococcus pneumoniae, Haemophilus influenzae, and Staphylococcus aureus

Novel Modulator of autoimmune demyelination

Potent inhibitor of histone deacetylase

Novel, potent and selective CRTh2 antagonist

Natural fungal phytotoxin, activating the plant jasmonic acid pathway

Lipopeptide antibiotic with activity against a range of Gram-positive bacteria including drug-resistant pathogens

Novel dual TRPV1 antagonist and TNF-alpha production inhibitor

Novel adenosine receptor agonist, inducing relaxation of corpus cavernosum; Novel selective phosphodiesterase-​4 (PDE4) inhibitor associated with anti-​TNF-​α properties

Novel Adenosine A2a Receptor Agonist, Attenuating the Progression of Monocrotaline-induced Pulmonary Hypertension

Novel IKK-β inhibitor, reducing the secretion of TNF-α, IL-1β, IL-6, IL-12, IFN-γ and increased secretion of IL-10, protecting gastrointestinal homeostasis

Novel orally active IKK2 inhibitor

Novel Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitor

Natural F508del-CFTR corrector, inhibiting both PARP-3 and -16, regulating the activity of the unfolded protein response activator inositol-requiring enzyme (IRE-1) via modulation of the level of its ribosylation by PARP-16

Natural F508del-CFTR trafficking corrector, targeting poly(ADP-ribose) polymerase (PARP)

Disruptor of microfilament-mediated processes