NRF2 inhibitor AEM1 is a specific small molecule inhibitor of Nrf2 transcriptional activity in cancer cells, shows no activity against a panel of >100 kinases (including isoforms of PI3K, AKT, and PKC).

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

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

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.

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.

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.

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.

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.