gpcrPANELS Assay Panel
Listed below are the assays currently available for screening and profiling.
Chemokine Family Selectivity Panel
With the complete family of
20 functional, cell-based chemokine assays available and regularly scheduled test dates, our goal is to help you make more informed decisions about the therapeutic potential and off target liabilities of your compounds.
The complete family of PathHunter Arrestin Chemokine receptors were tested in agonist mode (1uM screening concenration) to screen for highly selective agonist compounds. The Arrestin panel was able to detect both full and partial agonist responses due to its broad dynamic range.
The PathHunter arrestin chemokine panel was were tested with 6 reference antagonists to generate a ligand profile for the chemokine family. Three compounds (right panels) exhibited low specificity and inhibited a wide range of targets. In contrast, BMSCCR2 22, AMD3100 and Miraviroc had significantly lower cross reactivity. Of note, the highly specific AMD3100 and Maraviroc antagonists have previously gained FDA approval.
Data Analysis & Interpretation
Definitions
Percent Activity/Inhibition
The results for single concentration (primary screen) for tested compound(s) are reported in your study report and spreadsheets as '% Activity' or '% Inhibition' and are calculated in the following manner:
% Activity
(Agonist Mode) =
100% x
|
[ |
Mean RLU (test sample)- Mean RLU(vehicle control)
Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
|
] |
test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)
% Inhibition
(Antagonist mode) =
100% x
|
[ |
1- |
Mean RLU (test sample)- Mean RLU(vehicle control)
Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
|
] |
test sample = client supplied compound
vehicle control = DMSO (0% activity)
EC80 control = control compound (80% activity)
Dose Response Curve (EC50/IC50)
The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as EC50/IC50, which are values derived using the Hill equation:
