GSK 2830371 is a selective inhibitor of the WiP1 phosphatase that demonstrates potent antitumor activity in both lymphoma and neuroblastoma preclinical models by suppressing malignant cell proliferation.

5F-203 (NSC-703786) exhibits its anticancer properties through a multimodal mechanism of action. As a DNA-damaging agent, it creates stable adducts while arresting cell cycle progression. The compound's ability to strongly activate AhR signaling results in marked CYP1A1 induction. Additional effects include ROS generation and concurrent activation of multiple stress-responsive kinase pathways (JNK, ERK, and p38), collectively contributing to its cytotoxic profile.

Mps1-IN-3 is a selective and highly potent Mps1 kinase inhibitor with IC50 of 50 nM.

Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.

Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.

A small molecule that promotes differentiation of iPS-derived hepatocytes.

Fluxapyroxad is a broad-spectrum fungicide which inhibits the succinate dehydrogenase (SQR) enzyme.

AV-412, also known as MP-412, is a second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. This agent may be active against EGFR/HER2-expressing tumor cells that are resistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization.

AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.

​​Jarin-1​​ represents a breakthrough in plant hormone modulation as the pioneering small-molecule inhibitor of jasmonoyl-L-isoleucine synthetase (JAR1).

​​MEK-IN-4​​ is a novel small-molecule inhibitor targeting the MAPK/ERK kinase (MEK) pathway with therapeutic potential across multiple disease areas.

​​Dafadine-A​​ represents a novel class of cytochrome P450 inhibitors with unique species-specific activity.

​​TI17​​ represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.

​​B355252​​ is a novel neuroprotective compound that demonstrates dual mechanisms of action to support neuronal survival and regeneration.

​​MK-0343 (MRK-409)​​ represents a novel class of benzodiazepine-site ligands with unique GABAA receptor subtype selectivity.

​​CDE-096​​ is a highly effective plasminogen activator inhibitor-1 (PAI-1) antagonist with broad-spectrum inhibitory activity.

​​2-Hydroxysaclofen​​ is a selective and pharmacologically active antagonist of the GABAB receptor subtype, demonstrating multiple functional effects in neuropharmacological studies.

​​GB1107​​ is a novel small-molecule inhibitor specifically designed to target galectin-3 (Gal-3), demonstrating high binding affinity and oral bioavailability.

​​RO5263397​​ is a novel, orally active trace amine-associated receptor 1 (TAAR1) agonist demonstrating high potency and species-specific activity.

A competitive inhibitor of HMG-CoA reductase that acts as a lipid-lowering agent for prevention of events associated with cardiovascular disease..

Magnesium ionophore III is an onophore used in solvent polymeric membrane electrodes for the assay of Mg2+ activities in blood serum in vitro.

ICA135 (ICA-135, ICA 135) is a broad-spectrum inhibitor against human enteroviruses that inhibits Coxsackievirus A10 (CV-A10) replication in RD cells with IC50 of 1.446 uM.

ZHAWOC8697 is a small molecule dual inhibitor of sentrin-specific protease SENP1 and SENP2 with IC50 of 8.6 and 2.3 uM, respectively, a valuable tool for the study of SUMOylation processes.

EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.

HC-258 is a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. Co-crystallization with hTEAD2 confirmed that HC-258 binds within TEAD’s PA pocket, where it forms a covalent bond with its cysteine.

Oligopeptide-10, also known as granactive oligopeptide-10, is a synthetic bio-active peptide composed of 15 amino acids. it can help manage acne-causing bacteria, both on its own and in conjunction with anti-acne superstar exfoliant salicylic acid.

FDW028 is a potent and highly selective small-molecule inhibitor of fucosyltransferase 8 (FUT8) with binding KD value of 5.486 uM, displays no affinity against other FUTs, shows potent anti-CRC activities.

GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation.

ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.

ML162 is a covalent inhibitor that specifically targets ​glutathione peroxidase 4 (GPX4), a key regulator of ferroptosis. This compound exhibits ​selective cytotoxicity against cancer cell lines harboring ​mutant RAS oncogenes, making it a promising candidate for precision oncology.