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

Potent and selective α4β2 nACh receptor agonist

Highly selective agonist of α4β2 subtype of neural nicotinic acetylcholine receptors

Selective α7 nicotinic acetylcholine receptor (nAChR) agonist

High affinity α2-adrenoceptor antagonist and selective 5-HT uptake inhibitor

Potent and selective cannabinoid CB2 receptor agonist

Negative control for A-745

Potent CCK1 agonist

Potent and selective α7 nAChR partial agonist