Orally available active prodrug of ICRF-154, interferring with topoisomerase II activity prior to the formation of intermediate cleavable DNA-enzyme complexes during the catalytic cycle resulting in tumor cell growth inhibition

Inhibitor of tubulin polymerization, resulting in cell cycle arrest and induction of apoptosis

Novel macrophage modulator, inhibiting inflammation and M1 polarization of macrophages, restoring the balance between M1-polarized and M2-polarized macrophages in high fat diets (HFD)-induced obese mice resulting in the improvement of adipose inflammation

Highly selective inhibitor of CDK8 and its isoform CDK19

Novel agonist of PPAR-gamma, inhibiting lipopolysaccharide (LPS)-induced NO production and pro-inflammatory cytokines, potentiating interleukin-4-induced arginase-1 expression, promoting microglial polarization toward to an M2 anti-inflammatory phenotype

Inducer of apoptosis in neuroblastoma cells through inhibition of AKT signaling pathway

Novel potent serotonin and noradrenaline reuptake inhibitor (SNRI) with moderate 5-HT2A antagonist activity for anti-depression

Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Eraser (SNIPER), acting as a a protein degradation inducer of phosphodiesterase-4 (PDE4)

Novel potent and selective degrader of the ERα protein

Novel potent degrader of the mitochondrial CRABP-II protein

Novel fused proteins degrader of the His-tagged CRABP-II and Smad2 in cells

Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Eraser (SNIPER), acting as a a protein degradation inducer of bromodomain-containing protein 4 (BRD4)

Specific and Nongenetic IAP-dependent Protein Eraser (SNIPER), acting as a protein degradation inducer of oncogenic BCR-ABL protein

Highly selective alpha1A-adrenoceptor antagonist

Potent and selective GAL3 antagonist

Novel Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency In Vivo

Novel specific inhibitor of Aldo-keto reductase 1C3 (AKR1C3, EC 1.1.1.188)

Novel potent DNA-binding topoisomerase II-directed antitumor agent.

Selective ligand of GC-rich sequences in DNA

Novel Smurf1 inhibitor, promoting bone formation in mouse models of distinctive age-related osteoporosis

Novel dual inhibitor of thrombolysis and soluble epoxide hydrolase

Second-generation modulator of utrophin, increasing utrophin expression in skeletal, respiratory and cardiac muscles

Novel specific splicing enhancer, targeting RNA for a specific splicing correction, recognizing the interface between U1 snRNP and the SMN2 E7 5ʹ SS, promoting the U1-C zinc finger RNA duplex binding activity

Novel Stablizer of Survival of Motor Neuron 2 (SMN2) , Post-Translationally Stablizing SMN Protein for the Treatment of Spinal Muscular Atrophy (SMA)

Novel Active Site Inhibitor of Oncogenic K-Ras G12C

Selective, direct-acting covalent inhibitor of the K-Ras G12C mutant relative to wild-type Ras

Novel highly hydrophilic and non-ATP-competitive MEK1/2 inhibitor

Novel TLR2 agonist, promoting cross-presentation by mouse and human antigen presenting cells

Novel enhancer of the cyclin-dependent kinase (CDK) inhibitor p27(Kip)

Novel strathclyde minor groove binder (S-MGB), curing animal African trypanosomiasis (AAT)