For instance in a set of kinase inhibitors being tested, Inhibitor A shows excellent % inhibition - >85% at 5nM concentration, 45% at 10nM, 30% at 100nM and so on) and gives an IC50 value of ~10nM.
Another inhibitor B however shows poorer % inhibition - ~50-60% at 5nM concentration, ~45% at 10nM, 25-30% at 100nM and so on, and gives a lower IC50 value of ~5nM
So based on IC50 purely, one would say B is the more potent inhibitor, but % inhibition suggests otherwise. So is there supposed to be a correlation between these 2 values? Based on this data, which inhibitor would be considered better/more effective?
It would be great if someone could help a novice like me understand this concept.
I do not understand how your inhibition decreases with higher concentration of the kinase inhibitor.
I would expect a dose-related effect. Your question shows exactly the opposite : lower inhibition at higher dose. This is highly unusual.
Hi,
Is it possible that you got confused with inhibition% and activity% values? I am agree with Tomas.
Hi .. I think that if the laboratory conditions are stable for both cases, the A&B inhibitors have same effective. Anomalous readings can be deleted. LC5 can be calculated using statistical programs that measure the slop of the raw figures.
The reason that you are confused is that you're expecting the the Hill Slopes would be these same for both of these dose response curves, but they are obviously not. when you plot them out you will see how one is steeper than the other. I agree with Dr. Qari, that, under these conditions, the two compounds are essentially equipotent.
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