Novel inhibitor of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter (PCFT) over the reduced folate carrier (RFC)

Novel inhibitor of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter (PCFT) over the reduced folate carrier (RFC)

Novel broad-spectrum antifungal agent, also exhibiting good fungicidal activity against both fluconazole-sensitive and -resistant Candida albicans cells and having potent inhibition activity against Candida albicans biofilm formation and hyphal growth, in

Novel antifungal agent, inhibiting C. neoformans growth at submicromolar levels, being effective against fluconazole-resistant C. neoformans and a clinical strain of C. gattii, and being not antagonistic with currently approved antifungal

Novel antileishmanial agent against L. amazonensis promastigotes (IC 50 = 15.52 ± 3.782 μM) and intracellular amastigotes (IC 50 = 4.10 ± 1.136 μM), 50% cytotoxicity concentration at 84.01 ± 3.064 μM against BALB/c peritoneal macrophages, and 20.49-fold s

Novel antileishmanial agent, strongly inhibiting recombinant CYP51 from L. donovani, displaying activity against L. donovani intracellular amastigotes with an IC50 value of 0.53 μM

Novel idebenone analog, demonstrating significantly higher potency ex vivo, and significantly lower cytotoxicity, than idebenone in the treatment of Leber's Hereditary Optic Neuropathy (LHON)

Novel anti-MERS-CoV agent against virus-infected Huh7 cells

Novel antioxidant, binding copper in a unique manner compared to other chelates proposed to treat Alzheimer's disease and protecting HT-22 neuronal cells from cell death induced by Aβ + copper(II)

Novel anti-SARS-CoV-2 agent, displaying in vitro antiviral activity with IC 50 0.016 µM and Mpro inhibition activity with IC 50 0.013 µM, showing potent activity against human TMPRSS2 and furin enzymes with IC 50 0.05, and 0.08 µM, respectively

Novel antitubercular agent, exerting growth inhibition of Mtb during parasitism of host macrophages

Novel cellular anticancer agent, exhibiting 7.9-341.7-fold antiproliferative activities against four cell lines, Aspc-1 (human colon adenocarcinoma cells), H358 (human nonsmall cell lung cancer cells), HCT116 (human colorectal adenocarcinoma cells), and S

Novel anticancer agent, targeting PPARγ and HDAC4, being cytotoxic to CCRF-CEM cells (CC50 = 2.8 μM), inducing apoptosis, and causing DNA fragmentation, modulating the expression of c-Myc, cleaving caspase-3, and causing in vivo tumor regression in CCRF-C

Novel tumor-targeting cytotoxic agent

Cyclooxygenase inhibitior

AP1510 is a potent cell-permeable ligand for human FKBP12. AP1510 regulates protein-protein interactions through dimerization.

Novel highly potent and selective α4β2 nAChR antagonist

Inhibitor of both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation

Novel highly potent and selective Src_%28gene%29>Src kinase inhibitor

Novel inhibitor of the gatekeeper mutant of BCR-ABL, suppressing in vitro resistance

Potent and selective antitumor agent, effectively depleting cellular Fe, resulting in transferrin receptor-1 up-regulation, ferritin down-regulation, and increased expression of the potent metastasis suppressor, N-myc downstream regulated gene-1

Novel inhibitor of the Ap4A phosphorylase (Rv2613c) of Mycobacterium tuberculosis (Mtb)

Novel inhibitor of PCAF bromodomain/Tat-AcK50 association

Selective A2a adenosine receptor agonist

Novel inhibitor of PCAF bromodomain/Tat-AcK50 association

Novel potent and selective oxytocin receptor antagonist

N-Type calcium channel inhibitor

Histamine H3 receptor antagonist

Potent aminopeptidase N/CD13 (APN) inhibitor

Novel extremely potent inhibitor of APN activity in vitro, selective against other zinc-dependent enzymes such as matrix metalloproteases, and possessed limited cytotoxicity against Ad293 cells and favorable physicochemical and metabolic stability propert

Novel inducer of endogenous ApoA-I, protecting against atherosclerotic lesion development in ApoE-/- mice, upregulating the apolipoprotein A-I gene expression, enhancing its function of promoting cholesterol efflux, ABCA1 expression and activation of PPAR

Novel apolipoprotein E4 (apoE4) stabilizer, showing activity in an IL-6 and IL-8 cytokine release assay

Potent inhibitor of Bcl-2 and Mcl-1, acting as a BH3 mimetic

Inhibitor of HMG-CoA-reductase, promoting apoptosis of myeloma cells in vitro

Novel inducer of cell death by activating apoptosis in cancer cells

Novel anticancer agent, arresting MCF-7 cell growth at G2/M phase and S phase, dose dependent increasing in the mitochondrial membrane potential (ΔΨm) and ROS levels, decreasing in Gal-1 protein levels

Aminoglycoside antibiotic used in veterinary medicine

Marine-Derived Peptidic Stimulator of VEGF-A and Other Growth Factors with Potential Application in Wound Healing

Novel tumor calibrated inhibitor, showing unique polypharmacology and strongly improved therapeutic index in fly and human MTC xenograft models

First-in-class inhibitor of APS reductase (APSR), a critical enzyme in the assimilation of sulfate for the biosynthesis of cysteine and other essential sulfur-containing molecules

Prodrug of APX-001A, the first-in-class inhibitor of the fungal protein Gwt1

Inactive analog of pyrabactin used as the negative controller

Selective blocker of the Aquaporin-1 ion channel conductance, slowing cancer cell migration

Novel agonist of the water channel aquaporin-1 (AQP1)

Novel SH2-​containing inositol 5-​phosphatase (SHIP 1) modulator

Novel Antiandrogen, Suppressing Castration-Resistant and MDV3100-Resistant Prostate Cancer Growth

Novel AR antagonist, targeting the AR AF2, showing excellent AR antagonistic activity (IC 50 = 0.47 μM) and peptide displacement activity (IC 50 = 18.05 μM)

Novel potent androgen receptor (AR) degrader, exhibiting excellent AR binding affinity (85%) and AR degradation efficacy at 30 μM

Novel Rho kinase inhibitor

Novel inverse agonist of Mas G-protein signaling, dose-dependently inhibiting inositol 1,4,5-trisphosphate accumulation in AdMas-infected cells, and attenuating the sarcomeric organization and cell enlargement observed in Mas overexpressing myocytes

Novel 5-hydroxytryptamine 1B (5-HT 1B ) autoreceptor antagonist

Novel immunosuppressant and monocarboxylate transporter inhibitor, reducing immune responses both in vitro and in vivo, maintaining long-term graft survival, and inducing operational tolerance

Novel inhibitor of lactate transporters (monocarboxylate transporters; MCTs)

Highly potent CK2α inhibitor (K(i) = 0.5 nM), revealing high selectivity for CK2α in a panel of 140 protein kinases

Highly potent and selective fluorescent probe of Rho kinase (ROCK)

Anticancer agent, inducing apoptosis mediated at least in part by the ERS pathway and inhibiting hepatoma tumor growth

Negative control for ARCC-4, binding androgen receptors (AR) without inducing degradation.

Long-acting beta-2 adrenergic agonist

Long-acting beta-2 adrenergic agonist

Potent tumor-homing tripeptide, targeting heat shock protein 70 (HSP70)

Novel selective inhibitor of PREP, displaying great selectivity over FAP, while also not inhibiting the DPPs.

Novel inhibitor of Ark1, the fission yeast member of the conserved Aurora kinase family

P2T (P2YADP) purinoceptor antagonist

Selective ecto-ATPase inhibitor, preventing metabolism of P2 purinoceptor agonists

Natural inhibitor of recombinant purified ClpXP and ClpYQ AAA+ proteases, exhibitung potent antibacterial activity against H. pylori, including multidrug-resistant strains

Regulator and promotor of immune functions, enhancing the role of macrophages, inhibiting bacteria growth, improving the protein metabolism, and regulating liver function

Novel dual inhibitor of the fatty acid amide hydrolase (FAAH) and the cyclooxygenase (COX) enzymes

Novel selective estrogen receptor degrader (SERD), inducing regression in a tamoxifen-resistant breast cancer xenograft

Novel potent and selective BRAF inhibitor

Selective alpha-7 agonist

The first human arylsulfatase A reversible inhibitor, impairing mouse oocyte fertilization

Inhibitor of the inflammatory responses via NF

Non-steroidal selective estrogen receptor modulator (SERM)

Novel Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers

Inhibitor of D-amino acid oxidase (DAAO)

Inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake, significantly restoring decreased insulin-like growth factor 1 and fibroblast growth factor 2 mRNA levels in dorsal root ganglion and spinal cord, respectively

Potent factor Xa inhibitor with significant oral anticoagulant activity

Novel GPR119 agonist, potentiating insulin secretion from rat islets and having potent anti-diabetic effects in ICR and diabetic db/db mice

Second-generation potent orally-active thrombopoietin (TPO) receptor agonist

Novel Foxo1 inhibitor, exerting anti-diabetic and anti-hypertriglyceridemic effects by improving blood glucose and triglyceride metabolism at the gene expression level

Novel SHIP2 inhibitor, increasing Akt phosphorylation, glucose consumption, and glucose uptake in L6 myotubes, specifically upregulating the GLUT1 gene

Novel GPR40 agonist

Novel Receptor-interacting Protein Kinase 2 (RIP2) Inhibitor

Selective inhibitor of aurora kinases (AKs)

Novel angiogenesis inhibitor, directly binding to acid ceramidase 1 (ASAH1)

Novel inhibitor of inositol-requiring enzyme 1 (IRE-1), also inhibiting G protein-coupled receptor kinase 6 (GRK6)

Natural Suppressor of MMP-2-Mediated Migration and Invasion by Targeting FAK and JAK-STAT Signaling Cascades

Novel, Potent, Selective, and Brain-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitor, Modulating Brain Inflammation In Vivo

Novel modulator of acetylcholine receptor function, promoting the in vitro relaxation of β2-adrenoreceptor desensitized tracheas

Novel, Potent, Selective, and Direct Acid Sphingomyelinase (ASM) Inhibitor with Antidepressant Activity

Novel Permanently-charged Sodium Channel Blocker, Showing Robust Efficacy, a Rapid Onset and Long Duration of Action

Novel potent GPR17 agonist

Novel slow-onset, tight binding, potent asparagine synthetase (ASNS) inhibitor

Selective progesterone receptor modulator

Novel antifungal agent against Aspergillus isolates

Novel dual A2A/A1 AR antagonist

Novel tropomyosin-related kinase A (TrkA) inhibitor for the oral treatment of pain due to osteoarthritis of the knee

Novel long-acting muscarinic antagonist (LAMA), showing more selective inhibition of bronchoconstriction against salivation and more rapid onset of action than tiotropium bromide

Novel potent Aspergillus hyphal growth inhibitor

Selective antagonist for the cholecystokinin receptor CCKA

Novel cholecystokinin antagonist

Novel cholecystokinin antagonist

Natural antineoplastic agent, targeting cathepsin and inducing autophagy effects in breast cancer cells

Natural inhibitor of pollen development in Arabidopsis thaliana, also inhibiting dihydroxy-acid dehydratase (DHAD)

Natural luciferase inhibitor

Natural inhibitor of glutamic oxaloacetate transaminase 1 (GOT1), suppressing glutamine metabolism, making PDAC cells sensitive to oxidative stress and inhibiting cell proliferation, exhibiting potent in vivo antitumor activity in an SW1990-cell-induced x

Novel potent anticancer agent, inhibiting the growth of CRC bulk and sensitized FOLFOX-resistant cells

Novel near-infrared (NIR) probe for imaging β-amyloid (Aβ) plaques or Tau tangles

Novel anti-Alzheimer’s agent, inhibiting amyloid β aggregation, β-secretase, and tau aggregation

Novel AKAP1/PKA modulator, inducing UCP1 expression and thermogenesis

Inhibitor of HIV-reverse transcriptase activity

Natural endogenous inhibitor of nitric oxide synthases (NOS), also inhibiting arginine transport and increasing oxygen free radicals, mitochondrial dysfunction and transforming growth factor beta (TGFβ) expression, exhibiting a strong association with car

Novel inhibitor of αSyn fibrillization, blocking fibril growth and suppressing A53T αSyn neurotoxicity

The First Small-molecule Opioid Pan Antagonist with Nanomolar Affinity at Mu, Delta, Kappa and Nociceptin Opioid Receptors.

Novel NOP receptor-mu opioid receptor ligand

Novel potent and selective partial agonist of human and rat α3β4 nicotinic cholinergic receptors

High affinity, selective alpha3beta4 nAChR ligand

Novel dual μ-opioid and nociceptin receptor partial agonist (K i = 16.49 and 3.67 nM, respectively)

Nucleosidic antibiotic

Novel selective nociceptin receptor (NOP) agonist

Novel inhibitor of cyclin-dependent kinases 1, 2, 4, 5, and 9 with in vitro activity against lymphoid malignancies

Novel degrader of MTH1 fusion proteins for use within the aTAG system

aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC50 value of 0.28 nM and Ki value of 1.8 nM. degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader .

Hydrogen sulfide-releasing cyclooxygenase inhibitor

Potent cytotoxic agent for both prostate cancer and melanoma

Novel ROS generator, permeating mycobacteria to reliably enhance endogenous ROS including superoxide radical

Selective ß1 receptor antagonist

Potent JAK2 inhibitor

Novel selective A2BR antagonist

Novel inhibitor of the cancer-associated tropomyosin 3.1 (Tpm3.1), suppressing glucose-stimulated insulin secretion (GSIS) from the pancreatic islets

Novel non-toxic contrast agent for micro-CT imaging

Novel potent inhibitor of nucleotide pyrophosphatase/phosphodiesterase-1 (NPP1)

Novel antitimor agent, exhibiting superior anti-proliferative activity, excellent chemo-sensitizing activity against pancreatic cancer in vitro and in combination with Gemcitabine

Natural potent apoptosis inducer in U937 cells, inducing caspase-3 processing, PARP, and DNA fragmentation

Novel Potent Dual Inhibitor of MDM2 and MDMX (Ki =1 nM)

Novel potent and selective dual inhibitor of MDM2 (Ki = 0.9 nM) and MDMX (Ki = 7 nM)

Novel potent, highly selective, orally bioavailable CDK9/P-TEFb inhibitor

Novel Potent Autotaxin (ATX) Ligand

Novel selective Autotaxin (ATX) inhibitor

Novel inhibitor of JAK/STAT signaling, inhibiting both constitutive and interleukin-6-induced STAT3 phosphorylation, selectively affecting cell viability only of cancer cells harboring aberrant JAK/STAT signaling

Potent inhibitor of HCV RdR

Novel AURKA inhibitor, reducing clonogenicity, arresting the cell cycle at the G2/M phase, and inducing caspase-mediated apoptotic cell death in HCT116 human colon cancer cells

Natural antibiotic

Novel inhibitor of AChE, suppressing Aβ aggregation, protecting Caenorhabditis elegans against Aβ- and 6-OHDA-induced neurotoxicities dose-dependently

Potent inhibitor of HCV RdR

Novel small 4 integrin antagonist, preventing the development of experimental colitis in mice.

Novel potent ATP-competitive inhibitor of Aurora A/B/C (5.6/18.4/24.6 nM)

Novel DNA damage inducer during G0/G1, S, and G2 cell cycle phases via a mechanism unique from other DNA damaging agents

Novel autophagy inhibitor, targeting mitochondrial complex I directly, leading to the potent inhibition of mitochondrial respiration as well as autophagy

Unique signaling molecule used in quorum sensing

Novel inhibitor of autophagy, promoting metabolic stress within the tumour microenvironment and potentiating the effect of cytostatics in combination therapy

Novel anticancer agent, exhibiting potential cytotoxicity and inhibiting autophagy in hepatocellular carcinoma (HCC) cells

Monoselective agonist of the S1P(1) receptor

Novel USP30 inhibitor

Novel USP28 inhibitor

Novel, highly potent p53-MDM2 inhibitor with an IC50 value of 0.08 nmol/L, displaying excellent oral efficacy in the human SJSA1-based xenograft model.

First-in-class allosteric inhibitor of respiratory syncytial virus (RSV), blocking RNA elongation by the respiratory syncytial virus polymerase complex

Novel USP28 inhibitor

Novel selective USP7 inhibitor (USP7 IC50 9 μM; USP8 >50μM)

Novel USP28 inhibitor

The fifth-generation fluoroquinolone with in vitro coverage of community-acquired bacterial pneumonia (CABP) pathogens, atypical respiratory pathogens, multidrug-resistant Streptococcus pneumoniae and methicillin-resistant Staphylococcus aureus

Novel non-peptide Ang-(1-7) mimetic, inhibiting perivascular inflammation, through the reduction of chemokine expression in pVAT, as well as through direct actions on monocytes/macrophages inhibiting their activation

Novel angiotensin-(1-7) Mas receptor agonist

Novel antistaphyloccocal agent, attenuating inhibition of hERG potassium channel current

Cancer chemoprevebtive agent

Natural potent antienterovirus D68 (anti-EV-D68) agent

Novel cytosolic phospholipase A2 group IVA (cPLA2α) inhibitor, displaying potent anti-inflammatory activity and disease-modifying properties in cellular and in vivo models

Potent broad spectrum antibacterial agent, particularly against drug-resistant Staphylococcus pathogens

Novel potent and selective αvβ3 integrin inhibitor

The first potent and selective αvβ5 integrin inhibitor

Novel PDE4 inhibitor

Novel specific inhibitor of HIV-1 entry through interaction with the Env spike by virtue of the incorporation of a guandinium group

Novel potent dual inhibitor of Ax1 and Mer

Zn -dependent inhibitor of human plasma Lp-PLA2

Highly specific JNK inhibitor #212121; font-style: normal; font-variant-ligatures: normal; font-variant-caps: normal; font-weight: 400; letter-spacing: normal; text-align: start; text-indent: 0px; text-transform: none; white-space: normal; word-spacing: 0

Novel dual ERK5 and BRD4 inhibitor

Novel potent and selective ERK5 inhibitor

Novel potent dual ERK5 and BRD4 inhibitor

Novel highly potent and orally bioavailable Axl inhibitor

Novel integrin-binding peptide, inhibiting hepatocyte growth factor (HGF) signaling through Met-integrin interactions, also being an antiangiogenic agent by reducing phosphorylation of VEGR2, IGFR, and PDGFR, stabilizing vessels by disrupting α5β1 signali

Cyclooxygenase Inhibitor;

Second Generation

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel orally bioavailable inhibitor of Hedgehog signaling

Novel transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist

Novel potent EphB4 inhibitor

Novel tankyrase inhibitor, enhancing irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance

Novel covalent ERK1/2 inhibitor

Novel weak PAR2 antagonist

Novel selective Cdc42 inhibitor, suppressing primary colon cancer growth and prolonging survival in a preclinical mouse xenograft model by downregulation of PAK1 activity

Near-IR probe for detecting conformational changes of Aβ1-42 soluble oligomers in vitro

Inducer of Death Receptors and Sensitizer of Human Cancer Cells to TRAIL through a p53-Independent Mechanism

Inhibitor of hepatic cholesterol biosynthesis, inhibiting the cytochrome P450 enzyme lanosterol 14alpha-demethylase

Novel selective GABA-C antagonist

Novel CXCR2 antagonist with 200 times improvement in solubility than AZD8309

Selective alpha7 nicotinic receptor activator

Novel transient receptor potential vanilloid 1 (TRPV1) antagonist

AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways.

Novel peroxisome proliferator-activated receptor alpha (PPARalpha) agonist, inducing alanine aminotransferase-1 gene and protein expression in human, but not in rat hepatocytes