Prodrug of 4FGalNAz to label a variety of proteins in mammalian cells without perturbing endogenous glycosylation pathways and primarily act as a substrate for O-GlcNAc transferase (OGT)

Novel potent, nontoxic, and highly selective breast cancer resistance protein (BCRP) inhibitor

Novel inhibitor of Mycobacterium tuberculosis (Mtb), selectively killing Mtb at acidic pH and potentiating the bactericidal activity of isoniazid, clofazimine, and diamide

Novel inhibitor of Mycobacterium tuberculosis (Mtb) growth at acidic pH, killing Mtb by selectively depleting free thiols at acidic pH

Orally bioavailable M(1) muscarinic receptor allosteric agonist improving cognitive performance in an animal model

Novel potent, nontoxic, and highly selective breast cancer resistance protein (BCRP/ABCG2) inhibitor

Selective NPFF(1) receptor ligand

Novel blocker of HOX antisense intergenic RNA (HOTAIR) by abrogating the scaffold interaction with EZH2

Novel potent, nontoxic, and highly selective breast cancer resistance protein (BCRP) inhibitor

Novel potent and selective KOR antagonist, potentially stabilizing the bioactive conformation and enhancing its metabolic stability

Novel agonist of STING (stimulator of interferon genes) with enhanced binding to STING and cellular function

Inhibitor of protein synthesis with potent activity against multidrug-resistant Gram-positive bacterial strains

Selective dopamine D3 receptor antagonist

Orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction

Potent nicotinic acetylcholine receptor agonist

Hghly selective antagonist for endothelin ET A receptor

Novel PARP inhibitor

Agonist of neural nicotinic acetylcholine receptors

Potent and selective histamine H3 receptor antagonist

Natural hACE2 inhibitor with strong affinity for the exopeptidase site of hACE2

Natural TMPRSS2 inhibitor

Novel cyanine-5 containing probe for cathepsin K, showing selective visualization in complex proteomes, and live cell imaging of a human osteosarcoma cell line

Inhibitor of ribonucleotide reductase (RNR)

Peptide substrate for Abl Kinase (Abl protein tyrosine kinase), a partner in the gag-Abl fusion protein of the Abelson murine leukemia virus

Novel potent and selective inhibitor of ABHD10 (IC50 value ~ 30 nM)

Novel potent type II ABL/c-KIT dual kinase inhibitor

Novel potent colchicine binding site inhibitor (CBSI) and tubulin inhibitor

ABI-231 analogue, disrupting tubulin polymerization, promoting microtubule fragmentation, inhibiting cancer cell migration, overcoming paclitaxel resistance in a taxane-resistant PC-3/TxR model

Novel fluorescent A3 adenosine receptor (A3‐AR) agonist

Novel fluorescent highly potent agonist at the adenosine A3 receptor in both reporter gene (pEC50 = 8.48 ± 0.09) and internalization assays (pEC50 = 7.47 ± 0.11)