Novel inverse agonist of Mas G-protein signaling, dose-dependently inhibiting inositol 1,4,5-trisphosphate accumulation in AdMas-infected cells, and attenuating the sarcomeric organization and cell enlargement observed in Mas overexpressing myocytes

Novel Rho kinase inhibitor

Novel potent androgen receptor (AR) degrader, exhibiting excellent AR binding affinity (85%) and AR degradation efficacy at 30 μM

Novel AR antagonist, targeting the AR AF2, showing excellent AR antagonistic activity (IC 50 = 0.47 μM) and peptide displacement activity (IC 50 = 18.05 μM)

Novel Antiandrogen, Suppressing Castration-Resistant and MDV3100-Resistant Prostate Cancer Growth

Novel SH2-​containing inositol 5-​phosphatase (SHIP 1) modulator

Selective blocker of the Aquaporin-1 ion channel conductance, slowing cancer cell migration

Inactive analog of pyrabactin used as the negative controller

Prodrug of APX-001A, the first-in-class inhibitor of the fungal protein Gwt1

First-in-class inhibitor of APS reductase (APSR), a critical enzyme in the assimilation of sulfate for the biosynthesis of cysteine and other essential sulfur-containing molecules

Novel tumor calibrated inhibitor, showing unique polypharmacology and strongly improved therapeutic index in fly and human MTC xenograft models

Marine-Derived Peptidic Stimulator of VEGF-A and Other Growth Factors with Potential Application in Wound Healing

Aminoglycoside antibiotic used in veterinary medicine

Novel anticancer agent, arresting MCF-7 cell growth at G2/M phase and S phase, dose dependent increasing in the mitochondrial membrane potential (ΔΨm) and ROS levels, decreasing in Gal-1 protein levels

Novel inducer of cell death by activating apoptosis in cancer cells

Inhibitor of HMG-CoA-reductase, promoting apoptosis of myeloma cells in vitro

Potent inhibitor of Bcl-2 and Mcl-1, acting as a BH3 mimetic

Novel apolipoprotein E4 (apoE4) stabilizer, showing activity in an IL-6 and IL-8 cytokine release assay

Novel inducer of endogenous ApoA-I, protecting against atherosclerotic lesion development in ApoE-/- mice, upregulating the apolipoprotein A-I gene expression, enhancing its function of promoting cholesterol efflux, ABCA1 expression and activation of PPAR

Novel extremely potent inhibitor of APN activity in vitro, selective against other zinc-dependent enzymes such as matrix metalloproteases, and possessed limited cytotoxicity against Ad293 cells and favorable physicochemical and metabolic stability propert

Potent aminopeptidase N/CD13 (APN) inhibitor

Histamine H3 receptor antagonist

Novel inhibitor of PCAF bromodomain/Tat-AcK50 association

Selective A2a adenosine receptor agonist

Novel inhibitor of PCAF bromodomain/Tat-AcK50 association

Novel inhibitor of the Ap4A phosphorylase (Rv2613c) of Mycobacterium tuberculosis (Mtb)

Potent and selective antitumor agent, effectively depleting cellular Fe, resulting in transferrin receptor-1 up-regulation, ferritin down-regulation, and increased expression of the potent metastasis suppressor, N-myc downstream regulated gene-1

Novel inhibitor of the gatekeeper mutant of BCR-ABL, suppressing in vitro resistance

Novel highly potent and selective Src_%28gene%29>Src kinase inhibitor

Inhibitor of both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation