rac-NBI-74330 is a potent and selective CXCR3 antagonist.

Inhibitor of Janus kinases

Novel potent selective androgen receptor modulator (SARM)

Potent anti-free radical agent, elevating glutathione peroxidase (GSH-PX) and super oxide dismutase (SOD) levels and lowering malonaldehyde (MDA) level in vivo in the Alzheimer's model

Hsp90 N-terminal inhibitor

Novel inhibitor of the tyrosine kinase BCR-ABL and platelet-derived growth factor receptor, inhibiting mitosis entry in acute myeloid leukemia cells via suppression of Aurora kinase A expression

Novel potent inhibitor of p38 MAPK

Novel inhibitor of geranylgeranyl diphosphate synthase (GGDPS), showing significant reduction in tumor growth in mice

Novel inhibitor of geranylgeranyl diphosphate synthase (GGDPS)

Novel metabotropic glutamate type 5 (mGlu5) receptor negative allosteric modulator (NAM)

Potent fluorescent α4β1/α9β1 inhibitor

Novel dual inhibitor of dihydroceramide desaturase (dhCerDS) and acid ceramidase (ACDase)

Novel dual inhibitor of dihydroceramide desaturase (dhCerDS) and acid ceramidase (ACDase)

Selective inhibitor of poly(ADP-Ribose) glycohydrolase (PARG)

Novel highly potent, selective, and metabolically stable σ1 receptor agonist potentiating NGF-induced neurite outgrowth

Novel Potent Broad-Spectrum Inhibitor of Influenza A Virus RNA-Dependent RNA Polymerase (RdRp)

Novel HIV-1 Integrase Inhibitor

Novel HIV-1 Integrase Inhibitor

Novel potent inhibitor of RECQL5-helicase activity, and stabilizing RECQL5-RAD51 physical interaction, leading to impaired HRR and preferential killing of RECQL5-expressing breast cancer

Novel Prenyltransferase Inhibitor with In Vitro and In Vivo Antibacterial Activity

Novel potent inhibitor of the supercoiling and ATPase reactions of DNA gyrase, inhibiting gyrase by preventing the binding of ATP

Novel inhibitor of the supercoiling and ATPase reactions of DNA gyrase, inhibiting gyrase by preventing the binding of ATP and showing selectivity against M. smegmatis.

Novel specific inhibitor of the ability of RegA to activate its target promoters, reducing expression of a number of proteins required for virulence

Novel selective antagonist of the mGlu5 receptor

Potent ultra short-acting synthetic unique opioid analgesic

5-HT3 antagonist and 5-HT4 agonist, also acting as a 5-HT2B antagonist

Novel bacterial methionyl t-​RNA synthetase (MRS) inhibitor, hampering Plasmodium growth very effectively

Selective 5-HT1A receptor agonist

Oxidation-reduction indicator in cell viability

Potent VR1 vanilloid receptor agonist, activating protein kinase C

Angiotensin-converting enzyme 2 (ACE2) activator, acting as a modulator on RAAS and KKS activation during COVID-19

Red-absorbing, water-soluble, and iodinated resorufin derivative, being selectively activated with a monoamine oxidase (MAO) enzyme, showing high 1O 2 generation yields in aqueous solutions upon addition of MAO isoforms

Metabolite of Resveratrol

Metabolite of Resveratrol

Novel potent inhibitor of EBOV infection and entry

Novel inhibitor of the REV1/UbPCNA interaction, directly binding to REV1 UBM2 and preventing DNA damage tolerance (DDT)

Novel phosphodiesterase IV (PDE4) inhibitor for the treatment of Asthma and Rheumatoid Arthritis

Novel biomediator that induces reveromycins production at the wide range of concentrations without affecting cell growth

Novel TLR2 activator

Novel Highly Selective Neuropeptide FF1 Receptor Antagonist, Potently Preventing Opioid-Induced Hyperalgesia

Novel fluorescent D-amino acid for labeling peptidoglycans (PG) in live bacteria

Gene switch ligand as a transcription inducer for use in induceable gene expression systems

Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition

Potent, selective & ATP-competitive inhibitor of Cdks

Novel avß6 selective arginyl-glycinyl-aspartic acid (RGD)-mimetic, demonstrating to bind with extremely high affinity and selectivity for the alphavß6 integrin and having the potential as a clinical tool and therapeutic for investigating the role of avß6

Novel peptide-drug conjugate, inducing significant tumor growth suppression with negligible toxicity

Orally active, selective dopamine D3 receptor partial agonist

Novel Potent and Stable Antagonist of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain

Potent inhibitor of Kv1.5 potassium channel

Novel inhibitor of the human papillomavirus (HPV) E6 oncoprotein

Novel Insect growth regulator, as potential insecticide to control olive fruit fly (Bactrocera oleae Rossi)

Potent tubulin assembly and cancer cell growth inhibitor

Quorum sensing modulator as a RhlR agonist

Novel potent and selective RhlR antagonist, strongly inhibiting biofilm formation, and reducing production of virulence factors in P. aeruginosa

Quorum sensing modulator as a RhlR antagonist

Selective sigma-2 ligand, inducing apoptosis in EMT-6 breast cancer cells

Potent inhibitor of the Rho pathway

Selective antagonist of the serotonin 5-HT3 receptor

Antibiotic for tuberculosis (TB) treatment

Natural antibiotic, inhibiting prokaryotic DNA-dependent RNA synthesis and protein synthesis; blocking RNA-polymerase transcription initiation, modulating ß2m aggregation

Water-soluble benzodiazepine prodrug, as a sedative and hypnotic neuropsychiatric agent

HIV-1 reverse transcriptase inhibitor, also acting as an EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor

Novel antidiabetic agent, impairing glucose uptake by muscle tissue, excessing hepatic gluconeogenesis, and increasing beta-cell apoptosis

Natural inducer of apoptosis by significantly upregulating Bcl-2, mitigating expression of Bcl2 in HCT 15 cells and attenuating the apoptotic markers and cell cycle regulatory proteins

First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific inhibitor

Novel IAP-based selective RIPK2 degrader

Novel peroxisome proliferator-activated receptor gamma (PPARgamma) agonist

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