Potent vanilloid receptor (VR1) agonist

Potent TRPV1 agonist

High-affinity partial agonist of the vanilloid receptor

Novel BH3 α-helix mimetic, inducing apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak

Novel potent stimulator of glucagon-like peptide-1 (GLP-1) secretion in vitro, also potently stimulating Ca(2+) influx through TRPA1 cation channels, being one of the most potent non-electrophilic TRPA-1 channel agonists

Potent cannabinoid (CB) receptor agonist

Novel BET selective inhibitor, targeting BRD4

Novel neuroprotective agent, improving cognitive performances in a transgenic mouse model of AD

Novel live-cell peobe of voltage-dependent structural changes of voltage-gated Kv2.1 channels

Specific inhibitor of factor Xa

Novel K(ATP) channel opener

Novel inhibitor of urate transporter 1 (URAT1)

Novel orally active and selective transient receptor potential vanilloid 1 (TRPV1) antagonist

Novel nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase

Cytokine release inhibitor, inhibiting production of IL-1ß, IL-8, IL-6, IL-10 and TNFalpha

Novel RORγ

Novel ERK inhibitor, alleviating IMQ-induced mice skin lesions through ERK/IL-17 signaling pathway

Novel potent antitubercular agent, inhibiting InhA and FAS-II pathway

Novel antitubercular agent, inhibiting InhA and FAS-II pathway

Novel specific inhibitor of Fusarium myosin I; Fungicide

Novel inhibitor of CD4-gp120 binding, blocking the binding of the HIV-1 envelope glycoprotein gp120 to the CD4 receptor

Novel selective inhibitor of nuclear translocation of IKKα as the most potent synthetic gibberellin against cancer-derived cell lines, displaying no cytotoxicity in cells derived from noncancerous sources (HEK 293T, HS 578BST, HS 888Lu, HS 895Sk, HUVEC)

Non-toxic anti-relapse agent, acamprosate

Non-toxic radioprotector GS-nitroxide, improving hematopoiesis in long-term bone marrow cultures (LTBMCs)

Novel SMAC mimetic, sensitizing non-small cell lung cancers to multiple chemotherapy agents in an IAP-dependent but TNF-α-independent manner

Novel cysteine-reactive covalent ligand, selectively targeting C377 of PPP2R1A to impair breast cancer signaling, proliferation, and in vivo tumor growth

Selective DGAT2 inhibitor

Selective DGAT1 inhibitor

Novel TARP γ-8 Selective AMPAR Negative Modulator

Negative control for JNJ-54119936