Novel inhibitor of the second bromodomain (BD2) of the BET family protein BRD2

Apoptosis inducer; Antitumor agent

Selective non-lipid agonist of LPA2/3

Selective inhibitor of shp2 protein tyrosine phosphatase (PTP)

Novel selective inhibitor of JAK3

Novel potent inhibitor of Huntington's disease (HD) pathogenesis via targeting CAG repeats RNA and Poly Q protein

Inhibitor of human tyrosyl-DNA phosphodiesterase 1 (TDP1)

Novel substrate of ABCG2

Ligand of the Grb7 SH2 domain, inhibiting the growth of MDA-MB-468 cancer cells

Novel inhibitor of ABCG2 transporter function

Ras converting enzyme 1 (Rce1) inhibitor

Novel antagonist of the Grb7 SH2 domain; Antitumor Agent

Novel Inhibitor of the Ras Converting Enzyme 1 (Rce1) Protease, Disrupting Ras Membrane Localization in Human Cells

Novel potent growth inhibitor for gammaherpesvirus-associated B-lymphomas through activation of both the NF-κB and c-Myc-mediated signaling pathways

Novel α7 nAChR agonist at human and rat receptors

Novel potent α7 nAChR partial agonist

Novel molulator of SK-IK channels [small- and intermediate-conductance Ca2(+) -activated K(+) channels]

Novel allosteric inhibitor of HCV NS3 protein function

Novel Inhibitor with Activity against NS3/4A proteases from Multiple Hepatitis C Virus Genotypes

Potent, non-selective partial agonist at GABAA receptors with little efficacy at the alpha1 subtype and more at alpha2 and alpha3

Novel inhibitor of CDK5 translocation, increasing CDK5 accumulation in the nucleus, suppressing both cancer cell proliferation and xenograft tumorigenesis.

Novel activator of the Nrf2/HO-1 pathway, upregulating heme oxygenase-1 (HO-1) via promoting nuclear translocation of nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) to regulate LPS‐induced oxidative stress in macrophages

Novel NMDA/NR2B Antagonist

Novel substrate for NAD(P)H: quinone oxidoreductase 1 (NQO1), acting as an effective intracellular ROS generator for the treatment of drug-resistant non-small-cell lung cancer

Calcilytic negative allosteric modulator of calcium-sensing receptor (CaR)

Novel potent activator of the natriuretic peptide receptor C (NPR-C) with EC 50 ~1 μM

Novel inhibitor of TGF-β1 signaling pathway, inhibiting the upregulation of MAT2A mechanistically, dose-dependently activating PP2Cα and efficiently alleviating liver fibrosis

Novel heterotrimeric G-protein Gi modulator, inhibiting GDP/GTP exchange on a Gαi subunit induced by a G-protein-coupled receptor agonist, but not on another G-protein from the Gαs family, regulating Gβγ-dependent cellular processes, most likely by causin

Novel tubulin inhibitor

Novel competitive MTH1 inhibitor