A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.

LBL1 is a first-in-class pyrroloquinazoline small molecule that selectively targets the coiled-coil domain of lamin A (binding affinity Kd = 5.11 μM), demonstrating potent anticancer effects through nuclear lamina disruption.

SD-36 (STAT3 degrader SD-36) is a potent, selective STAT3 degrader (PROTAC), potently induces the degradation of STAT3 protein in vitro and in vivo.SD-36 is designed using an analogue of CRBN ligand lenalidomide and the STAT3 inhibitor SI-109, binds to recombinant STAT3 protein with Ki of 11 nM.SD-36 (250 nM) depleted >90% of STAT3 protein in MOLM-16 cells after 4 hr treatment and >50% of STAT3 protein in DEL, KI-JK and SU-DHL-1 cells after 7 hr treatment, also efficiently degraded STAT3 protein in murine cells.SD-36 displays extremely high cellular selectivity for degradation of STAT3 over other STATs.SD-36 effectively degrades both wild-type and mutated STAT3 proteins in cells, effectively degrades mutated STAT3 (D661Y, K658R mutant), also effectively degrades CRISPR-mutated homozygous Y705F mutant STAT3 protein in DLD-1/STAT3Y705F/Y705F cells.SD-36 displayed strong growth-inhibitory activities in a subset of leukemia and lymphoma cell lines (MOLM-16 cell line IC50, 35 nM), 100-fold more potent than SI-109.SD-36 (i.v. 25 mg/kg) effectively and selectively depletes STAT3 protein, achieves complete and long-lasting tumor regression in in mouse xenograft tumors.

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.

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)

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.

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).

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.

VL285 is a potent VHL ligand, degrading HaloTag7 fusion proteins.

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.

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.

VU-29 (DPAP) is a potent, selective and allosteric potentiator of rat mGlu5 receptor with EC50 of 9 nM, displays >50-fold selectivity over mGlu1 and mGlu2 receptor (EC50=557 nM and 1.51 uM).

Hydrophobic inducer of the degradation of stabilized proteins, degrading HaloTag2 fusion proteins

ARN-21934 is a novel potent and highly selective inhibitor for human topoisomerase II α over β.

AGI-001 is an orally bioavailable, competitive antagonist of 5-HT1A/1B receptors with reversible binding properties. This compound also functions as a partial agonist at β-adrenergic receptors, making it a valuable pharmacological tool for investigating neurological disorders.

ElteN378 is a selective FKBP12e inhibitor with potential therapeutic applications in neurodegenerative disorders and oncology. This compound shows particular relevance for research involving Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), as well as various proliferative disorders and malignancies.