Highly selective α4β2 subtype nicotinic receptor agonist

Novel potent Liver Receptor Homolog-1 (LRH-1) modulator

Novel inhibitor of dengue virus NS5 RNA-dependent RNA polymerase (RdRp), inhibiting the DENV type 2 (DENV2) RdRp activities

Natural selective inhibitor of protein tyrosine phosphatases (PTPases)

Novel potent and selective SIRT2 inhibitor, increasing the acetylation level of eukaryotic translation initiation factor 5A (eIF5A) and reducing cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression

Novel selective inhibitor of activated fibroblasts, inhibiting the enhanced migration of fibroblasts cocultured with cancer cells by binding to β-arrestin1 and interfering with β-arrestin1-mediated cofilin signaling pathways

Novel potent and highly selective GPR6 inverse agonist, inhibiting GPR6 cAMP signalling in TR-FRET assays with a EC50 = 16 nM and >100 fold selectivity against GPR3 and GPR12

Novel gastrocolokinetic ghrelin agonist, approximately sixfold greater potency than natural ghrelin

Promising pro-apoptotic agent, showing activity on various cancer cell lines

Novel MOR agonist

Novel Fluorescent ER-Tracker dye, showing potent cytotoxic activity on several types of cancer cells, being accumulated into the endoplasmic reticulum (ER) as highlighted by its colocalization

The first irreversible covalent MPS1 inhibitor, targeting a poorly conserved cysteine in the kinase's hinge region

Potent, reversible, non-carbonyl inhibitor of fatty acid amide hydrolase (FAAH)

Novel potent and specific RNA-binding ligand, targeting riboswitches and other RNAs at proximal subsites

Selective antagonist of NMDA receptors NR2B subunits

Selective alpha1A/1L-adrenoceptor partial agonist

Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit

Potent protein kinase C (PKC) inhibitor

ADAM17-selective inhibitor

Competitive AMPA receptor antagonist

Selective, non-competitive Metabotropic_glutamate_receptor>mGlu2 antagonist

Novel NR2B selective, non-competitive, voltage-independent antagonist

NMDA receptor antagonist , specifically suppressing the severe autoimmune phenotypes of chs3-2D (chilling sensitive 3, 2D), including the arrested growth morphology and heightened PR (Pathogenesis Related) gene expression

Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor

Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor, exhibiting antifungal activity in vivo

Vitamin D analogue, showing significant in vitro and in vivo antitumor activity.

Novel reversible inhibitor of interleukin-2 (IL-2)

Dual inhibitor of HDAC and MMP

Potent and selective inhibitor of the p38 MAPK catalytic domain

Beta(1) adrenoceptor-selective agonist

Novel mGlu2/3 negative allosteric modulator (NAM)

Selective negative allosteric modulator of mGlu3

Novel highly potent dual NK1/NK3 receptor antagonist

Novel Glucokinase Activator for the Treatment of Type 2 Diabetes

Orally active chemokine receptor CCR2 antagonist preventing glomerulosclerosis and renal failure in type 2 diabetes

Novel potent, orally available GPBAR1 agonist

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

Potent γ-secretase modulator (GSM)

Novel potent and selectve LPA1 antagonist, attenuating NHLF human lung fibroblast cell proliferation and contraction in vitro, reducing plasma histamine levels in mouse LPA-challenge model

Novel potent γ-secretase modulator (GSM) with high solubility, balanced lipophilicity, and showing no phototoxicity and PIK4CB side bing activity

Selective antagonist at the 5-HT1A receptor

Platelet-activating factor (PAF-R) antagonist, selectively for intracellular PAF binding sites

Novel potent competitive inhibitor of Rho-associated coiled-coil-containing protein kinase 2 (ROCKII)

Novel potent ROCK inhibitor

Potent Rho--​kinase (ROCK) inhibitor

Novel potent and selective ROCK inhibitor

Novel potent and selective ROCK inhibitor

Novel potent and selective ROCK inhibitor

Anti-cancer agent, acting through gastrin antagonism and H /K -ATPase inhibition, modulating apoptosis pathways, antidyslipidemic, antiadipogenic, gastroprotective, antifertility, and antileishmanial

Lipid modifying agent; Antihyperlipidemic and antiarteriosclerotic

Novel p38α kinase inhibitor; Antioxidant

Allosteric modulator of dextromethorphan binding to high-affinity sigma receptors

The first potent inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt

Novel potent and selective RORγt agonist, showing robust antitumor efficacy in syngeneic tumor models and improving the efficacy of anti‑PD‑1 in a murine lung cancer model

Novel RORgammaT inhibitor

Novel RORγt agonist

Novel potent RORγt inverse agonist

Novel potent and selective CB2 probe (Ki for CB2: 0.8 nM and >12000 selectivity over CB1)

Novel P2X3 antagonist

Photosensitiser for the treatment of age-related macular degeneration

Novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor

Prodrug of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148

Specific and competitive H2 receptor antagonist

Potent agonist of S1P1 receptors

Novel non-peptidic RANTES antagonist

Novel stimulator of autophagy, inhibiting Mycobacterium tuberculosis survival in macrophages, and targeting Pik1

Novel stimulator of host immune defenses, Inducing the transcription of putative immune effectors in C. elegans

Novel inhibitor of β-amyloid-induced cytotoxicity

Selective collagenase inhibitor, inducing the conformational change in the side-chains of the S1 pocket of MMP-1

Potent and selective competitive antagonist of 5-HT4 receptors

Selective phosphodiesterase-4 (PDE4) inhibitor

Selective and reversible Monoamine_oxidase_A>monoamine oxidase A (MAO-A) inhibitor

Specific ligand to CB2-positive spleen tissue of rats and mice

Potent indirect activator of AMPK

Novel allosteric RORγt inverse agonist

Selective inhibitor of the dopamine transporter (DAT), blocking cocaine-induced locomotor stimulation and acting as a positive allosteric modulator of the human CB1 (hCB1) receptor

Novel potent and selective KOR antagonist

Novel Potent and Selective Orexin-1 Receptor Antagonist

Novel Potent Dual Orexin Receptor Agonist

Novel allosteric inhibitor of soluble adenylyl cyclase (sAC)

Potent serotonin SR-1A/SR-1B and moderate SR-2C agonist

Potent vertebrate GABAa antagonist

Novel non-steroidal antiandrogen, downregulating c-myc messenger RNAs

Potent non-steroidal antiandrogen

Novel DNA gyrase B inhibitor

Novel inhibitor of Src protein tyrosine kinase SH2

PKCβ-selective inhibitor

The first small molecule inhibitor of ThiD; IkB kinase (IKK) inhibitor; antibiotic

Novel Ricin Inhibitor, Targeting Ribosome Binding

Novel Ricin Inhibitor, Targeting Ribosome Binding

Novel Ricin Inhibitor, Targeting Ribosome Binding

Novel Ricin Inhibitor, Targeting Ribosome Binding

Inhibitor of Adipogenesis/Lipogenesis with AMPK Activation and UPR Suppression, Reducing Lipid Accumulation in Adipocytes

Novel specific RUVBL1/2 ATPase inhibitor, radiosensitizing NSCLC, but not normal lung epithelial cells

Natural potent macrophage uptake enhancer of S. aureus and zymosan A bioparticles

Inhibitor of LFA-1/ICAM-1 Mediated Cell Adhesion

Potent and selective of the benzodiazepine site on GABA(A) receptors

Selective antagonist of protease activated receptor-1

Novel CD45 phosphatase inhibitor

Novel small molecule inhibitor of protein interaction with glycosaminoglycans (SMIGs), exercising broad spectrum anti-inflammatory activity by inhibition of protein binding to the cell surface GAG, heparan sulfate

The first Small Molecule RXFP3/4 Agonist, Increasing Food Intake in Rats Upon Acute Central Administration

Novel potent broad-spectrum antiviral inhibitor, showing excellent broad-spectrum inhibition activity against various pathogenic viruses, including hepatitis c virus (HCV), dengue virus (DENV), zika virus (ZIKV), Chikungunya virus (CHIKV), enterovirus 71

Partial 5-HT1A serotonin receptor agonist

Selective D2 dopamine receptor antagonist; Precursor to radiolabeled S-(-)-raclopride

The most viable GPVI modulator, acting as a potent antithrombotic agent

Novel highly effective tyrosinase inhibitor with great potential to be utilized in anti-Parkinsonian syndrome

Highly Potent and Selective Butyrylcholinesterase (BChE) Inhibitor for Cognitive Improvement and Neuroprotection

Highly Potent and Selective Butyrylcholinesterase (BChE) Inhibitor for Cognitive Improvement and Neuroprotection

Inverse agonist of the constitutive androstane receptor (CAR)

FP receptor agonist

Novel HIV-1 integrase inhibitor

Novel inhibitor of D-cyclin transactivation via phosphoinositide 3-kinase pathway

Potent 5-HT1A receptor agonist, also acting as a 5-HT2A and 5-HT2C receptor antagonist

Potent, orally active, partial 5-HT1A receptor agonist

Inhibitor of NADPH oxidase, preventing the structural and functional sequelae of diet-induced metabolic heart disease

Potent and selective thrombin inhibitor for the treatment of thromboembolic disorders

Novel, Potential Antipsychotic Displaying Marked Antagonist Properties at α1- and α2-Adrenergic Receptors

Selective and highly potent alpha2-adrenoceptor agonist

Novel potent and selective agonist activity for S1PR4

Novel selective sigma 1 receptor (S1R) antagonist, exhibiting potent binding affinity for S1R, high selectivity over S2R and 87 other human targets, acceptable in vitro metabolic stability, slowing clearance in liver microsomes, and excellent blood-brain

Potent and selective ligand of imidazoline 1 receptor (I1R)

Potent and selective ligand of imidazoline 1 receptor (I1R)

Potent activator of the AMP-activated protein kinase (AMPK)

Potent quinone reductase 2 (QR2) inhibitor

alpha2-Adrenoceptor Antagonist, Norepinephrine Transporter (NET) Inhibitor, Serotonine Transporter (SERT) Inhibitor

Potent and selective inhibitor of constitutive Stat3 DNA-binding and transcriptional activities

Novel modulator of the retrograde signaling including cellular responses to hypoxic and oxidative stress, selectively eliminating superoxide production by complex III without altering oxidative phosphorylation

Potent inhibitor of glucose-6-phosphate translocase (G6P T1)

Novel glucokinase (GK) activator

Novel glucokinase (GK) activator

Dual PPARα/γ agonist

Novel Analogue of SUN-B8155, acting as a cell active and functionally-relevant agonist of calcitonin receptor (CTR), inducing different Gs or arrestin activities through CTR

Partial benzodiazepine inverse agonist, showing antidepressant-like pharmacological activity and acting as a cognitive enhancer

Novel ileal Na /bile acid cotransporter inhibitor

Peripherally restricted cannabinoid CB1/CB2 receptor agonist, inhibiting gastrointestinal motility with no effect on experimental colitis in mice

Irreversible and nonselective Monoamine_oxidase_inhibitor>monoamine oxidase inhibitor (MAOI)

Novel Smoothened receptor agonist

Novel clickable HDAC inhibitor, selectively labeling HDAC complex proteins

Novel Endogenous Reactive oxygen species (ROS)-activated HDAC inhibitor prodrug, demonstrating selective activity against multiple cancer cell lines such as HeLa, MCF-7, MDA-MB-231 and B16-F10, while remaining benign to non-cancer cells

Natural α-glucosidase inhibitor

Natural α-glucosidase inhibitor, potently modulating Nrf 2 , NF-κB and STAT3 pathways

ß2-adrenoceptor agonist

Antibiotic, Inhibiting CD44 expression in breast cancer cells and mammary tumor growth

Novel potent V-ATPase inhibitor, blocking viral entry

Opioid receptor antagonist for the treatment of alcoholism and cocaine addiction

Natural antimicrobial and antitumor agent, inducing reactive oxygen species (ROS), and alterating heme biosynthesis

Vasopeptidase or dual inhibitor of ACE and neutral endopeptidase with potential application in the treatment of hypertension and congestive heart failure

Uridyl peptide antibiotic, exhibiting antibacterial activity against Mycobacterium tuberculosis H(37)Ra and Pseudomonas aeruginosa with MIC values of 10 and 12.5 mug/ml, respectively

Novel potent inhibitor of Shh signaling pathway

Novel Potent Non-peptidic Inhibitor of Secreted Aspartic Protease 2 (SAP2) for the Treatment of Resistant Fungal Infections

Broad-spectrum antifungal agent, selective inhibiting the cytochrome P-450-dependent ergosterol synthesis in Candida albicans, Aspergillus fumigatus and Trichophyton mentagrophytes, in vitro and in vivo activity against F. pedrosoi

Novel inhibitor of TAFIa (activated thrombin-activatable fibrinolysis inhibitor)

Novel selective and potent dual inhibitor of thrombin and factor Xa

Broad spectrum antibiotic

Regulator of the sarco-endoplasmic reticulum Ca -ATPase (SERCA1a), significantly slowing down the E2 to Ca2.E1 transition of SERCA1a while it affects neither phosphorylation nor dephosphorylation

Regulator of the sarco-endoplasmic reticulum Ca -ATPase (SERCA1a), significantly slowing down the E2 to Ca2.E1 transition of SERCA1a while it affects neither phosphorylation nor dephosphorylation

Novel Highly Potent Selective Androgen Receptor Degrader (SARD)

Novel Potent Selective Androgen Receptor Degrader (SARD)

Covalent Antineoplastic Agent

Novel potent SARS-CoV-2 3CLpro inhibitor with IC 50 value of 73 nM

Novel SARS-CoV-2 Main Protease (Mpro) Inhibitor, inhibiting viral replication with a nanomolar EC 50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells, impairing SARS-CoV-2 replication in human lung epithelial cells and human-induced pluripotent stem ce

Novel SARS-CoV-2 nsp14 Methyltransferase inhibitor

Novel potent SARS-CoV-2 MTase Nsp14 and Nsp16 inhibitor

Selective non-peptide vasopressin V2 receptor antagonist

Selective non-peptide vasopressin V2 receptor antagonist

Novel inhibitor of salmonella serine acetyltransferase (SAT), the enzyme that catalyzes the rate-limiting step of L-cysteine biosynthesis

Inhibitor of H274Y and N294S mutants

Subtype-selective α4β2 nicotinic acetylcholine receptor partial agonist

PPARγ covalent ligand

Novel reversible covalent inhibitor of the cyclin-dependent kinase 5 (Cdk5)-mediated phosphorylation of PPARγ at Ser245, a key factor in the insulin-sensitizing effect of PPARγ-targeted drugs

Novel neuroprotective agent, suppressing abnormal tau protein aggregation

Selective, active-site-directed 14 kDa PLA2 inhibitor, totally inhibiting LT and PAF formation, while prostanoid formation was not altered

Dual ETA and ETB receptor antagonist

Potent, specific inhibitor of human p38 mitogen-activated protein (MAP) kinase

Potent and selective agonist for the human ß3-adrenoceptor

Inhibitor of p38 MAPK

Selective 5-HT2C_receptor>5-HT2C inverse agonist

Selective 5-HT7 receptor antagonist

Novel selective mTOR inhibitor

Nonpeptidic antagonist of alpha(v)beta3 and alpha(v)beta5 integrins, reducing angiogenesis and VEGF expression

Selective dopamine D3 receptor antagonist

Selective p38a kinase inhibitor, inhibiting Brd4

AntiMycobacterium tuberculosis agent

Novel TRPV4 blocker

Potent and selective dopamine D3 receptor antagonist

Novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor

Novel CXCR2 selective antagonist, inhibiting ex vivo neutrophil activation and ozone-induced airway inflammation in humans

Novel inhibitor of mitogen and Stress-Activated Kinases 1 (MSK1)

Novel Rho kinase inhibitor

Potent non-cytotoxic inhinitor of Mycobacterium tuberculosis H37Rv

Novel cAMP-independent potentiator of CFTR, synergistically restoring CFTR function

Novel cAMP-independent potentiator of CFTR, synergistically restoring CFTR function

Membrane-permeant, fluorescent, selective Na+ indicator dye

Novel potentiator of metabotropic glutamate receptors for use against neurological and psychiatric disorders

Novel potentiator of metabotropic glutamate receptors for use against neurological and psychiatric disorders

Novel inhibitor of Quiescin Sulfhydryl Oxidase 1 (QSOX1), suppresses tumor cell growth in a Matrigel-based spheroid assay and inhibits invasion in a modified Boyden chamber, but does not affect viability of non-malignant cells

Inhibitor of S100B which selectively kills melanoma; Amoebicidal diamidine

Novel Smac mimetic, demonstrating potent cell-killing effects in several subtypes of breast, ovarian, and prostate cancer cell lines but only when the DR ligand TRAIL or another such apoptosis inducer is co-administered

Novel obatoclax derivative, inducing apoptosis in hepatocellular carcinoma cells through SHP-1-dependent STAT3 inactivation

Potent inhibitor of checkpoint kinase 2 (Chk2)