Selective Dopamine D3 Receptor Antagonist

Novel inhibitor of BAG-1-mediated protein interactions, targeting the RAF-MEK-ERK signaling pathway, transformed cells

Allosteric Inhibitor of the NS2B-NS3 Protease from Dengue Virus

Novel potent nonbrain-penetrant BACE1 inhibitor

Novel activator of Pyrin inflammasome

Novel HBV core protein allosteric modulator (CpAM), bing to the HAP pocket and modulating HBV capsid assembly in a distinct manner

Novel CCR5 antagonist-based HIV-1 entry inhibitor

Novel chimeric inhibitor of dimeric RAF, inhibiting B-Raf V600E mutan

Natural potent HDAC inhibitor

Potent and selective PFKFB3 inhibitor

Novel photoswitchable agonist for peroxisome proliferator-activated receptor γ (PPARγ)

Novel photoswitchable ligand for the cannabinoid receptor 2 (CB2)

Novel photoswitchable agonist for peroxisome proliferator-activated receptor γ (PPARγ)

Excellent photoswitchable agonist for neuronal α7 nAChRs

Macrolide antibiotic, binding to the 50S subunit of the bacterial ribosome and thus inhibiting translation of mRNA

Mitochondria-luciferin releasing agent, reacting with mitochondria-activatable luciferin (MAL-Probe), such as TPP-CL2, to release luciferin

Novel CNS penetrant potent inverse agonist of GHS-R1a (IC 50 (affinity) = 0.77 nM)

Potent, second-generation, selective histamine-H1-receptor antagonist and mast cell stabilizer

Potent and selective ATP-competitive Dyrk1B kinase inhibitor

Antimicrobials, active against methicillin resistant S. aureus (MRSA)

Novel potent smoothened inhibitor, demonstrating in vivo activity in abrogating the Hh paracrine pathway as well as anti- tumor effects

Novel, potent and selective inhibitor of p38α MAP kinase

Novel selective inhibitor of 5-Lipoxygenase Activating Protein (FLAP) for the treatment of inflammatory diseases

Novel Fibrinolysis Inhibitor, Acting via Interference of a Protein-Protein Interaction

Glucokinase activator, decreasing fasting and postprandial glucose in type 2 diabetes mellitus patients

First-in-class selective, partial CDK2 degrader against hearing loss and cancer, protecting against cisplatin ototoxicity and kainic acid excitotoxicity

Novel potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis

Novel peroxisome proliferator-activated receptor alpha (PPARalpha) agonist, inducing alanine aminotransferase-1 gene and protein expression in human, but not in rat hepatocytes

Novel transient receptor potential vanilloid 1 (TRPV1) antagonist

Selective alpha7 nicotinic receptor activator