Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.

Highly selective inhibitor of the ​FK506-binding protein 51 (FKBP51)

Galicaftor (ABBV-2222/GLPG-2222) is an orally bioavailable small molecule that functions as a CFTR corrector, demonstrating potential for therapeutic development in cystic fibrosis research.

TH 287 is a first-in-class MTH1 inhibitor (IC50 value 5.0 nM) that selectively and effectively kills U2OS and other cancer cell lines, with considerably less toxicity towards several primary or immortalized cells.

PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. MM2 is the binding site of RMI complex on Fanconi anemia complementation group M protein (FANCM). PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.

RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.

PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.

Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.

BMS-195614 is a potent, orally bioavailable RARα antagonist (Ki = 2.5 nM) that modulates multiple signaling pathways. It upregulates Bcl2 expression while suppressing NF-κB, AP-1, and PPAR transactivation. Additionally, it reduces IL-6 and VEGF production, mitigates phototoxic damage from blue light, and exhibits anti-migratory, anti-inflammatory, and anti-angiogenic properties.

AZ3976 is a selective PAI-1 inhibitor that exhibits potent profibrinolytic effects, with IC50 values of 26 μM (chromogenic assay) and 16 μM (plasma clot lysis assay). Unlike conventional inhibitors, it does not target active PAI-1 but instead binds reversibly to the latent form, accelerating the transition of active PAI-1 to its inactive state.

WQ-2101 (WQ2101, PKUMDL-WQ-2101) is a specific, allosteric inhibitor of PHGDH with IC50 of 34.8 uM (WT PHGDH), shows dramatically reduced potenecy for mutants R134A (IC50 =141 uM) and K57AT59A (IC50=128 uM).

ZLD1039 is a novel, orally active EZH2 inhibitor demonstrating high selectivity and potency. It effectively suppresses PRC2 enzymatic activity across wild-type EZH2 (IC50 = 5.6 nM) and mutant forms (Y641F: 15 nM; A677G: 4.0 nM), while exhibiting significant anti-tumor and anti-metastatic effects in breast cancer models.

Novel Inhibitor of Monoubiquitinated Proliferating Cell Nuclear Antigen (PCNA), inhibiting Repair of Interstrand DNA Crosslink, enhancing DNA Double-strand Break, and sensitizing Cancer Cells to Cisplatin.

LY305 is a potent non-steroidal SARM exhibiting high androgen receptor binding affinity (Ki = 2.03 nM) and strong agonist activity in C2C12 cells (EC50 = 0.499 nM), demonstrating its selective modulation capabilities.

corticotropin releasing factor (CRF) antagonist.

SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).

EX229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM

Sufugolix(TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively).

NNK is a procarcinogen, a major tobacco-specific toxicant that inhibits the expression of lysyl oxidase, a tumor suppressor.

CYM 50769 is a small-molecule, selective NPBWR1 antagonist that effectively inhibits NPW-23-stimulated proliferation in ATDC5 cells, making it a valuable tool for studying endochondral ossification processes.

SSAA09E2 is a novel inhibitor of SARS-CoV replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2)

Novel inhibitor of TRPM6, promoting mesoderm and definitive endoderm differentiation of human embryonic stem cells through alteration of magnesium homeostasis

Tradipitant (VLY-686) is a selective neurokinin-1 (NK-1) receptor antagonist with potential therapeutic applications.

KYN-101 (KYN101) is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.

SKI-178 is a potent, specific, non-lipid SphK1 inhibitor with Ki of 1.33 uM, displays no significant activity for SphK2 (IC50>25 uM).

SW-100 (SW100) is a potent, selective, brain penetrable HDAC6 inhibitor with IC50 of 2.3 nM, displays >1,000-fold selectivity over all other class I, II, and IV HDAC isoforms.

Adaphostin is a novel activator of Fas-mediated death pathway in Bcr/Abl-positive leukaemia.

M351-110 is a V-domain immunoglobulin suppressor of T-cell activation (VISTA) agonist that enhances immune responses, making it a promising candidate for cancer immunotherapy research.

ML202 represents a selective allosteric modulator of human pyruvate kinase M2 (hPK-M2) that specifically enhances phosphoenolpyruvate (PEP) binding cooperativity without significantly affecting adenosine diphosphate (ADP) binding kinetics.

Phevamine A is a phytotoxic secondary metabolite produced by Pseudomonas syringae. This small molecule compound facilitates bacterial proliferation through its ability to suppress host plant defense mechanisms.