RO5203648 is a high-affinity, selective partial agonist of TAAR1 (trace amine-associated receptor 1) that represents an innovative pharmacological approach for investigating neuropsychiatric disorders.

ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.

MSBN is a highly selective fluorogenic probe for thiols, selectively imaging thiols in live cells and specifically label protein thiols with a turn-on signal to determine diverse reversible protein thiol modifications.

BRD6688 is a selective HDAC2 inhibitor. It acts by enhancing the learning and memory processes.

Creatine riboside is the strongest classifier of lung cancer status in all and stage I-II cases, important for early detection, and also associated with worse prognosis in stage I-II lung cancer.

WAY-169916 functions as a selective estrogen receptor modulator that uniquely suppresses NF-κB-mediated transcription, resulting in significant anti-inflammatory activity.

SGA360 modulates inflammatory SAA1 signaling via an aryl hydrocarbon receptor (AHR)-dependent pathway, functioning as a partial antagonist through a non-canonical mechanism independent of AHR-DNA binding.

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.

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.

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.