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Competition Binding Assays (IC50/KI)

Competition Binding Assays (IC50/KI)

Cell or tissue homogenate containing the receptor of interest is incubated together with a radioligand for the receptor and a range of concentrations of the test (competing) drug. Typically up to 11 concentrations of the test drug are evaluated over a three log unit range and with triplicate (or quadruplicate) replicates at each concentration.

After equilibrium has been reached, receptor-bound radioligand is separated from non-bound radioligand using either.

Filter-based Separation

Scintillation Proximity Assay (SPA)

Example Competition Binding Graph

The filters or SPA plate are counted for radioactivity to determine the level of receptor-bound radioligand and the results are plotted to obtain the IC50 and Ki values for the drug-receptor interaction.

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Compound Characterization

Compound Characterization

Compound Characterization Study Goal Determine ex vivo receptor occupancy of CMPDx at Orexin-1 (OX1) receptors using radiolabeled Orexin antagonist Created by potrace 1.10, written by Peter Selinger 2

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Compound Characterization 1

Compound Characterization 1

Compound Characterization Study Goal Determine ex vivo receptor occupancy of CMPDx at Orexin-1 (OX1) receptors using radiolabeled Orexin antagonist Created by potrace 1.10, written by Peter Selinger 2

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