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)

Novel ligand of the dimerization interface of survivin monomers

Novel GHS-R1a biased ligand, acting as a Gαq/11 inverse agonist

Potent fluorescent agonist of the human A1 or A3 adenosine receptors, (dissociation constants: A1 and A3 receptors were approximately 50 and 10 nM, respectively)

Novel Trojan Horse Prodrug for the Inhibition of P-Glycoprotein with Anti-HIV-1 Activity

Novel Trojan Horse Prodrug for the Inhibition of P-Glycoprotein with Anti-HIV-1 Activity

Atypical antipsychotic, potently binging to D2 receptors and 5-HT2 receptors

Novel inhibitor of the in vivo aggregation of Aβ1-42

Photoswitchable Kv channel blocker

Novel selective dual inhibitor of Aurora/PLK, significantly inhibiting the development of the colon cancer growth and prolonging the median survival time

Novel inhibitor of adaptor associated kinase 1 (AAK1), demonstrating improved activity against dengue virus both in vitro and in human primary dendritic cells and the unrelated Ebola virus

Novel selective Inhibitor for AAA (ATPase associated with diverse cellular activities) Proteins

Ultrapotent in vivo-active serine hydrolase inhibitor

Novel potent agonist and positive allosteric modulator (Ago-PAM) of δ-GABAARs

Novel potent MDM2 degrader

Selective TRPV1 antagonist

Potent and selective histamine H4 receptor antagonist

Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist

Potent and selective histamine H4 receptor antagonist

Selective TRPV1 antagonist

Inactive enantiomer of A-908292 with approximately 50-fold less activity against ACC2, also causing a similar reduction in glucose and triglycerides

Selective dopamine receptor D1 agonist