JCP174 is an inhibitor of a depalmitoylase that enhances Toxoplasma host-cell invasion by targeting TgPPT1.

KV2 channel inhibitor-1 demonstrates selective blockade of KV2.1 (IC50 = 0.2 μM) and KV2.2 (IC50 = 0.41 μM) channels while exhibiting minimal activity against KV1.2 (IC50 >10 μM). The compound shows >10-fold selectivity over NaV channels and other KV subtypes, with only weak effects on CaV channels.

PH-064 (also known as BIM-46187) functions as a potent inhibitor targeting the heterotrimeric G-protein signaling complex.

GSK5182 is a potent, orally bioavailable inverse agonist that selectively targets ERRγ (IC50 = 79 nM) without affecting ERRα or ERα nuclear receptors. Additionally, it stimulates ROS production in hepatocellular carcinoma cells.

CE3F4 is a potent, noncompetitive EPAC1 inhibitor that blocks EPAC1-induced Rap1 activation both in cell-free systems and in intact cells and did not influence protein kinase A holoenzyme activity.

RBC10 demonstrates anticancer properties by disrupting the Ral-RALBP1 protein interaction. This compound additionally suppresses Ral-dependent cellular processes, including fibroblast spreading in murine models and colony formation of human tumor cells in soft agar assays.

PSB-SB-487 demonstrates dual receptor activity, functioning as a potent GPR55 antagonist (IC50 = 113 nM) while also acting as a CB2 receptor agonist (Ki = 292 nM at human CB2). This compound shows therapeutic potential for investigating metabolic disorders, neurodegenerative conditions, pain pathways, and oncological applications.

ML-211 is a carbamate-containing small molecule that potently inhibits both APT1/LYPLA1 (IC50=17 nM) and LYPLA2 (IC50=30 nM). While it also blocks ABHD11 activity (IC50=10 nM), it maintains >50-fold selectivity for LYPLA enzymes over 20 other tested serine hydrolases.

HS-1793, a structural analog of Resveratrol (HY-16561), demonstrates broad-spectrum antitumor effects across multiple cancer cell lines by triggering apoptotic cell death.

VPC 23019 is an aryl amide-based S1P receptor modulator that demonstrates receptor subtype selectivity. It functions as a competitive antagonist at S1P1 (pKi=7.86) and S1P3 (pKi=5.93), while acting as an agonist at S1P4 (pEC50=6.58) and S1P5 (pEC50=7.07) receptors.

SW155246 is a selective DNA methyltransferase 1 (DNMT1) inhibitor, demonstrating potent activity against human DNMT1 (IC50 = 1.2 μM) while showing weaker inhibition of murine DNMT3A (IC50 = 38 μM). This compound holds potential for cancer research and other therapeutic applications.

ML298 demonstrates potent and selective inhibition of phospholipase D2 (PLD2), exhibiting an IC50 of 355 nM while showing minimal activity against PLD1 (IC50 >20 μM), representing >53-fold selectivity.

YM-26734 acts as a competitive antagonist of secretory phospholipase A2 (PLA2), demonstrating broad-spectrum inhibitory activity against multiple PLA2 isoforms.

CYM2503 is a potential positive allosteric modulator of the galanin receptor subtype 2 (GalR2). Preclinical studies indicate that CYM2503 prolongs the onset of electrographic seizures and reduces overall seizure duration. Additionally, it exhibits protective effects against electroshock-induced seizures in murine models. Both GalR1 and GalR2 receptors are considered promising therapeutic targets for investigating seizure disorders and epilepsy.

Atglistatin is a potent and selective inhibitor of adipose triglyceride lipase (ATGL), effectively suppressing lipolysis activity. In vitro studies demonstrate its inhibitory effect with a half-maximal inhibitory concentration (IC50) of 0.7 μM.

The small molecule ML336 demonstrates specific antiviral activity against the TC-83 strain of Venezuelan equine encephalitis virus (VEEV) by functioning as a potent inhibitor.

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.

4'-bromo-resveratrol, a brominated analog of resveratrol, shows significant anticancer properties through its unique capacity to inhibit SIRT1 and SIRT3 simultaneously. In melanoma models, it alters cellular metabolism by targeting mitochondrial function, leading to cell cycle arrest and induction of programmed cell death. This multimodal mechanism suggests potential applications in overcoming treatment resistance.

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.

OS-3-106 represents a blood-brain barrier permeable compound demonstrating exceptional selectivity and potency as a dopamine D3 receptor (D3R) agonist. With an impressive binding affinity of Ki = 0.2 nM for D3R, this compound shows particular promise for investigating potential therapeutic interventions in psychoactive substance addiction disorders. Its unique pharmacological profile makes it a valuable research tool for studying reward system modulation.

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.

VK-II-36, a structural analog of carvedilol, selectively suppresses sarcoplasmic reticulum Ca²⁺ release without exhibiting β-receptor blocking activity. It effectively inhibits both early and delayed afterdepolarizations, thereby preventing triggered arrhythmias. This unique pharmacological profile makes VK-II-36 a promising candidate for antiarrhythmic therapy.

Galloflavin is a strong inhibitor of lactate dehydrogenase (LDH), effectively targeting both LDH-A and LDH-B isoforms with calculated inhibitory constants (Ki) of 5.46 μM and 15.06 μM, respectively, for pyruvate. By disrupting LDH activity, galloflavin suppresses glycolysis and reduces ATP generation, leading to the inhibition of cancer cell proliferation. This mechanism highlights its potential as an anticancer agent targeting metabolic pathways.

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

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

TAE-1 is a AChE inhibitor. TAE-1 inhibits acetylcholinesterase (AChE; IC50 = 0.465 µM for the human erythrocyte 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.