Article
A Scale of Agonism and Allosteric Modulation for Assessment of Selectivity, Bias, and Receptor Mutation.
Molecular pharmacology - 1 Oct 2017
Kenakin Terry
Abstract excerpt
An index of agonism is described that can be used to quantify agonist receptor selectivity, bias, cell-based agonism, and the effects of receptor mutation on signaling. The parameter is derived from agonist concentration-response curves and comprises the maximal response to the agonist (max) and the EC50 in the form of Δlog(max/EC50). This parameter is derived from equations describing agonists as positive...
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