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.

ML-240 functions as a potent ATP-competitive inhibitor targeting the p97 ATPase, demonstrating inhibitory activity with an IC50 value of 110 nM.

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.

CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.

API-1 is a small-molecule Akt inhibitor that triggers Mcl-1 degradation through a GSK3/β-TrCP/FBXW7-dependent mechanism, ultimately promoting apoptotic cell death. In sensitive lung cancer models, API-1 treatment causes rapid Mcl-1 downregulation. Notably, forced Mcl-1 expression confers resistance to API-1-induced apoptosis.

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.

TH588 represents a highly selective and cell-permeable small molecule inhibitor targeting MTH1 (NUDT1), a member of the nudix hydrolase family, with potent inhibitory activity (IC₅₀ ≈5 nM).

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.

RX-3117 is an orally available and potent DNA synthesis inhibitor with potential antineoplastic activity.

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.

Leukadherin-1 is a specific agonist of CR3 and the leukocyte surface integrin CD11b/CD18.

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.

ML303 is an antagonist of pyrazolopyridine influenza virus nonstructural protein 1 (NS1) (IC90 : 155 nM).

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.

AT-56 is a selective, competitive, and highly bioavailable inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) with a Ki value of 75 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.