Figure 4
From: Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family
The inhibition pattern by opioid ligands. (a) The percentage of DAMGO responses in SH-SY5Y cells as a function of the binding affinity of opioid ligands to the MOR. (b) The percentage of DAMGO responses in SH-SY5Y cells as a function of the binding affinity of opioid ligands to the DOR. (c) The percentage of DAMGO responses in HEK-MOR cells as a function of the binding affinity of opioid ligands to the MOR. (d) The percentage of DPDPE responses in HEK-DOR cells as a function of the binding affinity of opioid ligands to the DOR. The percentage of agonist responses after pretreatment with ligands in the library were calculated based on the normalization of the agonist response in the presence of a ligand to the positive control (i.e., the agonist response after pretreatment with the vehicle buffer only). The data points in pink were calculated based on the known binding affinity of each ligand against the specific receptor using% agonist response = 1/[1 + 10^log (X – Ki)], wherein X is the concentration of each ligand, and Ki the binding affinity obtained in literature. Included in this analysis are ligands whose binding affinities at specific receptor sites are known.