Article
Dopamine D2 Receptor Agonist Binding Kinetics-Role of a Conserved Serine Residue.
International journal of molecular sciences - 15 Apr 2021
Ågren Richard, Stepniewski Tomasz Maciej, Zeberg Hugo, Selent Jana, Sahlholm Kristoffer
Abstract excerpt
The forward (kon) and reverse (koff) rate constants of drug-target interactions have important implications for therapeutic efficacy. Hence, time-resolved assays capable of measuring these binding rate constants may be informative to drug discovery efforts. Here, we used an ion channel activation assay to estimate the kons and koffs of four dopamine D2 receptor (D2R) agonists; dopamine (DA), p-tyramine, (R)- and...
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