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

Microtubule stabilzer, potently inhibiting cellular proliferation in cancer cell lines

Natural antifungal and cytotoxic agent

Natural inhibitor of the proliferation of sensitive and resistant human cancer cell lines and this inhibitory activity is strongly increased in the presence of laxaphycin A

Potent, orally active, selective and direct thrombin inhibitor

Prodrug of LB30870 as potent, orally active, selective and direct thrombin inhibitor

Neurotoxic amino acid

Novel antibiofilm coating, covalently bindng to a titanium implant surface (LC0024-Ti)

Novel activator of Lecithin:cholesterol acyltransferase (LCAT) including some familial mutations, by forming a hydrophobic adduct with Cys31

Novel potent angiogenesis inhibitor, inhibiting VEGFR-2 and JAK/STAT3 signalling in primary cultured human endothelial cells and cancer cells

Novel clickable linker for estrogen receptor degraders

Novel potent and selective RON receptor tyrosine kinase inhibitor

Novel potent and selective covalent inhibitor of EGFR and Her2 exon20 insertion mutations, exhibiting selectivity over wild type EGFR and within the kinome

Novel potent inhibitor of the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL) and dampening flux through the pentose phosphate pathway

Novel potent and selective covalent inhibitor of EGFR and Her2 exon20 insertion mutations, exhibiting selectivity over wild type EGFR and within the kinome

Novel dual inhibitor of GSK-3β and aurora kinase A, increasing somatic cell plasticity and inhibiting tumorigenicity

Novel Aurora Kinase A Inhibitor

Novel Src family tyrosine kinase inhibitor with anti-inflammatory effects in response to Aß stimulation of microglia

Novel inhibitor of human lactate dehydrogenase A (LDHA)

Novel Inhibitor of SIRT1; Inhibitor of the human MDM2-p53 interaction

Novel PAK3 kinase inhibitor, inhibiting p53-​inactivated cancers

Novel inhibitor of PERK stress-dependent eIF2α phosphorylation with no toxicity to the cells

Novel TDP-43::GFP aggregation inhibitor

Necroptosis inhibitor

Novel inhibitor of phosphatidylcholine transfer protein (PC-TP)

Potent and metabolically stable inhibitor of necroptosis, a regulated caspase-independent cell death pathway

Novel cdk5/p25 kinase inhibitor

Novel potent tau kinase inhibitor, targeting CDK5​/p25 and GSK3β

Potent haspin kinase inhibitor

Novel ALK2 inhibitor

Competitive LRRK2 kinase inhibitor without affecting the GTPase activity

Precursor of 6-[18F]Fluoro-L-DOPA used for positron emission tomography (PET) scans. References: http://www.hindawi.com/journals/bmri/2014/674063/

Nucleic acid binding fluorescent dye

Highly potent multi-target antagonists of both alpha1A- and alpha1D-adrenoceptors, and also of 5-HT1A receptors

Novel partial agonist of PPARα and PPARγ, providing distinct and favorable gene activation profiles for the treatment of diabetes and obesity

Highly potent multi-target antagonists of both alpha1A- and alpha1D-adrenoceptors, and also of 5-HT1A receptors

Highly potent multi-target antagonists of alpha1A- and alpha1D-adrenoceptors, and 5-HT1A receptors

Novel inhibitor of the LEDGF/p75-IN interaction, potently inhibiting both the early and late stages of HIV-1 replication

Cyclooxygenase-2 (COX-2) inhibitor

Novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist

Novel potent inhibitor for the PLAAT family members, reducing the NAE levels, including anandamide, in cells overexpressing PLAAT2 or PLAAT5

Novel inhibitor of nuclear receptor binding SET domain 2 (NSD2), against H3K36 methylation

Novel inhibitor of T-cell expansion and autoimmune encephalomyelitis

Novel Electrophilic PROTAC that degrades nuclear proteins by engaging DCAF16

Phosphodiesterase inhibitor, acting as a vasodilator and showing antihypertensive effects

Novel non-steroidal glucocorticoid receptor agonist

Novel Soft-Drug Inhibitor of Phosphodiesterase 4 (PDE4) for Topical Treatment of Atopic Dermatitis

Orally bioavailable Smoothened (Smo) antagonist

Leukotriene B4 receptor antagonist

Inhibitor of ERAAP function

Partial agonist (antagonist) at mu and delta opioid receptors.

Watersoluble prodrug of Levcromakalim, being more chemically robust and efficacious at lowering IOP with once daily dosing in a normotensive mouse model.

Natural carnitine derivative, playing a role in mitochondrial metabolism and demonstrating beneficial cardiovascular effects

Respiratory quinolone antibiotic, exhibiting enhanced activity against the important respiratory pathogen Streptococcus pneumoniae

Neuroprotective, anti-inflammatory, and anti-diabetic agent, protecting against DNA damage and apoptosis induced by ultraviolet light

Selective estrogen receptor modulator (SERM)

Hematologic malignancy-selective membranolytic peptide from the antimicrobial core (RRWQWR) of bovine lactoferricin

Novel potent and selective antagonist of exportin-1, attenuating dual NF-κB signaling and the Nrf2 cytoprotection pathway via targeting exportin-1 in colitis mice

Novel non-secosteroidal vitamin D receptor (VDR) ligand

Novel irreversible inhibitor of cell division cycle 25B, inhibiting human cancer cells via ROS generation

Potent and specific pan-PIM inhibitor, inhibiting proliferation of several AML cell lines, showing dual antitumoral and bone antiresorptive effects

Novel S. typhimurium infection inhibitor on the activity of DUSP3, DUSP11, and DUSP27

Novel inhibitor of cystine stone formation for treatment of cystinuria

Natural precursor of histamine; reversible inhibitor of protein synthesis

Serotonin-norepinephrine-dopamine triple reuptake inhibitor (SNDRI); Anti-depressant

Novel inhibitor of AMA1–RON2 interaction, blocking merozoite invasion from schizont-infected RBCs; Cytochrome P450 inhibitor

Inhibitor of cholinephosphotransferase (CPT), phosphatidyl-N-methylethanolamine N-methyltransferase (PME-NMT), and phosphatidyl-N,N-dimethylethanolamine N-methyltransferase (PDE-NMT)

Potent positive inotropic agent, inhibiting myocardial cell apoptosis

Novel inhibitor of the oncogenic Lin28-let-7 interaction

Natural capsid inhibitor

Novel Fused Benzodiazepine Hybrid Payload for Antibody-Drug Conjugate (ADC)

5HT-4 antagonist with moderate 5HT-3 antagonist properties

Lipid II binder, causing specific upregulation of the vancomycin-resistance associated gene vraX which is implicated in the cell wall stress stimulon that confers glycopeptide resistance

The first inhibitor of the catalytic activity of AChE and AChE-induced amyloid-beta aggregation protecting against reactive oxygen species

The first fluorogenic dipeptide probe for

Novel pan-inhibitor of sialyltransferase (ST)

Potent, selective, and orally active inhibitor of semicarbazide-sensitive amine oxidase (SSAO) activity, inhibiting vascular adhesion protein 1 (VAP-1) activity and decreasing the density of macrophages in inflamed atherosclerotic plaques in mice

Highly

Novel selective agonist of the human melanocortin 1 receptor (hMC1R) for sunless tanning and prevention of genotoxicity of UV in melanocytes

Novel inducer of biofilm dispersal, having a slower rate of NO release

Novel inhibitor of kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2)

Novel Modulator of p75NTR-dependent motor neuron death

Negative control for LM11A-24

Novel Probe for Imaging Tau Pathology in Transgenic Mouse and Rat Models

Novel p75NTR antagonist

Novel AI-2 quorum-sensing inhibitor, affecting the starvation response and reducing virulence in several Vibrio species, most likely by interfering with LuxPQ

Novel highly selective inhibitor of the low-molecular-weight protein tyrosine phosphatase (LMPTP), being highly orally bioavailable and reversing obesity-induced diabetes in mice

Novel Two-in-One Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites

Potent and selective ligand of imidazoline 1 receptor (I 1 R)

Novel potent and specific agonist of I 1 imidazoline receptors

Peroxisome proliferator-activated receptor-α/γ (PPAR α/γ) dual agonist

Inhibitor of the Vesicular_monoamine_transporter_2>vesicular monoamine transporter-2 (VMAT2)

Antibiotic for treatment of bacterial infections including bronchitis and urinary tract infections, prevent urinary tract infections prior to surgery

Natural neurotrophic agent

Opioid receptor agonist, acting on the µ-opioid receptors in the myenteric plexus of the large intestine

Lopinavir Secondary Metabolite

Novel LOX-activity sensor for cross-linking with a collagen peptide to chemoselectively target endogenous aldehydes generated by LOX

Potent ligand of the 5-HT7 receptor

Potent antimitotic and oral tubulin binding agent, significantly inhibiting growth of a human non-small-cell lung tumor

Novel potent and selective peripheral AAK1 inhibitor

Novel inhibitor of both renal SGLT1 and SGLT2

Novel LPA 1-3 agonist, inducing a calcium response in hLPA 1-3 cells within a range of 0.4 to 1.5-log lower potency, as compared to LPA

Novel LPA 1-3 agonist, inducing a calcium response in hLPA 1-3 cells within a range of 0.4 to 1.5-log lower potency, as compared to LPA

Novel p53 activator through the inhibition of MDM2

Novel potent and specific inhibitor of O-linked β-N-acetylglucosamine transferase (OGT)

Novel agonist of liver receptor homolog-1 (LRH-1), reducing the expression of lipogenic genes in mouse liver, and inflammation and disease severity in a mouse model of ulcerative colitis

Novel potent agonist of the liver receptor homolog-1 (LRH-1, NR5A2)

The first small molecule antagonist of LRH-1 activity.

Novel selective and reversible LSD1 inhibitor (IC50 value of 60 nM), exhibiting the antiproliferative activity against HTB5, HTB3, HT1376, and HTB1 cells with IC50 values of 1.87, 0.18, 0.09, and 0.93 μM, respectively

Novel selective inhibitor of histone lysine specific demethylase 1 (LSD1/KDM1A), displaying FAD-competitive binding to LSD1, concentration-dependently inducing accumulation of H3K4me1/me2 and H3K9me2, increasing expression levels of epithelial cell marker

Novel prodrug of Lisofylline, maintaining a steady fasting blood glucose level with a significant increase in insulin level

Novel prodrug of Lisofylline, maintaining a steady fasting blood glucose level with a significant increase in insulin level

First-in-class inhibitor of NF-κB signaling pathway by preventing the maturation of a rate-limiting multiprotein complex necessary for IKK activation

Novel positive allosteric modulator (PAM) of the GLP-1R, enhancing insulin secretion in a glucose-, ligand- and GLP-1R-dependent manner

Precursor for 11C-radiolabelling LSN3172176 PET scan

Selective inhibitor of P-glycoproteins (P-gp)

Novel potent xanthine oxidase inhibitor

Novel potent inhibitor of FLT3 mutations, also inhibiting CDK2 and CDK6

Novel inhibitor of the interactions of CFTR-associated ligand (CAL) and PSD-95/Dlg1/ZO-1 (PDZ) domain

Peptide metabolite

Novel PI 3-kinase delta inhibitor

Brain penetrant high affinity α1A-adrenoceptor ligand

Novel potent and selective hA2A receptor antagonist

Novel potent and selective inhibitor of LRRK2, inhibiting LRRK2 WT, the overactive variant G2019S, and the resistant mutant A2016T56 at 12 nM, 19 nM and 93 nM, respectively

Novel, potent, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors

Novel potent and selective LMP2 inhibitor, also inhibiting mouse 20S proteasomes

Novel β2-specific inhibitor, potently targeting both β2c and β2i, displaying moderate trypanocidal activity

Novel potent β2c-specific inhibitor, displaying moderate trypanocidal activity

Novel β2i-specific inhibitor, displaying moderate trypanocidal activity

Potent and selective adenosine A2A receptor antagonist

Potent mGlu5 receptor positive allosteric modulator (PAM)

A1 adenosine receptor antagonist

Human adenosine A1 receptor antagonist

Hybrid ortho/allosteric ligand of the adenosine A(1) receptor

Thiazolidine-containing cyclic peptide antibiotic, suppressing growth of species of disease-causing bacteria in that part of the human microbiome

Novel inhibitor of heat shock protein 90 (Hsp90)

Immune modulator with SARS-CoV-2 antiviral activity via a multi-target mechanism including localized, self-limiting reactive oxygen species (ROS) scavenging activities that were demonstrated in a model of lipopolysaccharide (LPS)-induced joint inflammatio

Novel Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma

Novel selective LXRβ agonist, reducing total brain Aβ

Novel Manassantin A Derivative, Inhibiting Hypoxia-Inducible Factor 1 and Tumor Growth

Novel potent HIF-1 inhibitor, also downregulating the protein level of HIF-1alpha, which depended on von Hippel-Lindau for proteasome degradation, showing in vivo anticancer efficacy by decreasing the HIF-1alpha expression in nude mice bearing MX-1 tumor

Novel LRRK2 kinase inhibitor against the wild-type and G2019S mutant LRRK2 kinase being 424.40 ± 1.31 nM, 378.80 ± 1.20 nM, respectively

Novel LRRK2 kinase inhibitor against the wild-type and G2019S mutant LRRK2 kinase being 1526.00 ± 0.87 nM, 1165.00 ± 1.18 nM, respectively

Novel, potent, orally-bioavailable kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders

Novel glucokinase activator (GKA)

Novel mGlu2/3 receptor agonist; Prodrug of LY-404039

Potent antioxidant, being cytoprotective in models of focal and global cerebral ischemia

Selective negative allosteric modulator of mGlu3

Potent 5-HT3 serotonin receptor antagonist

Orally active cell-permeable inhibitor of human

Novel, potent, and systemically bioavailable mGlu2/3 receptor agonist, exhibiting both antipsychotic and analgesic properties in vivo

Selective cell permeable phosphatidylinositol 3-kinase (PI3K) inhibitor

Novel highly potent and selective agonist of metabotropic glutamate (mGlu) receptors 2 and 3

Potent and selective inhibitor of PKCβI and PKCβII

Potent GluR5 kainate receptor agonist

Selective GluR5 kainate receptor antagonist

AMPA receptor potentiator

Allosteric modulator of AMPA receptors

Orally active ghrelin agonist, bindjng with high affinity to and being a potent activator of the growth hormone secretagogue receptor 1a (GHS-R1a) receptor

AMPA receptor potentiator

Selective mGlu1 receptor antagonist

Novel potent and selective dual PPARalpha/gamma agonist

Novel competitive GLUK5 receptor antagonist