I saw there are more people use a K inact in a video seminar ("Recent Highlights in Covalent Drug Discovery"). could you explain what it is? why does it matters?
Irreversible inhibitors operate on a target differently, so traditional potency measures for reversible binders (Ki and IC50) may not be satisfactory. kinact is a rate constant. It is often used with Ki to give kinact/Ki as a way to measure the effectiveness of drug-target binding (covalent binding). My expertise in this area is very limited, but here is a freely accessible reference - journals.sagepub.com/doi/pdf/10.1177/1087057116671509.
really like your video! Now I have a clear mind about Ki and IC 50. thanks
I saw there are more people use a K inact in a video seminar ("Recent Highlights in Covalent Drug Discovery"). could you explain what it is? why does it matters?
Irreversible inhibitors operate on a target differently, so traditional potency measures for reversible binders (Ki and IC50) may not be satisfactory. kinact is a rate constant. It is often used with Ki to give kinact/Ki as a way to measure the effectiveness of drug-target binding (covalent binding). My expertise in this area is very limited, but here is a freely accessible reference - journals.sagepub.com/doi/pdf/10.1177/1087057116671509.
Thank you for the reference. I will dig into it. @@ChemHelpASAP