BioKin, Ltd. - Technical notes: Determination of inhibition constants (K<sub>i</sub>) and inactivation rate constants (k<sub>inact</sub>)

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TN201502

EGFR inhibition: K_i and k_inact

Determination of inhibition constants (K_i) and inactivation rate constants (k_inact)

Automated determination of k_inact and K_i for covalent inhibition using the Omnia assay

BioKin Technical Note TN-2015-02

Petr Kuzmic
BioKin Ltd.
Draft - Rev. 1.01 - February 4, 2015

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Abstract

This document is an accompaniment to a published report [Schwartz et al. (2014) Proc. Natl. Acad. Sci. USA 111, 173–178] on covalent inhibition the EGFR kinase. It describes in detail the raw experimental data that were used to generate the list of K_i and k_inact values specifically for the double mutant EGFR-L858R/T790M enzyme. The document also provides links to all theoretical model description files utilized within the DynaFit software package to analyze the raw experimental data. The data and the DynaFit "script" (i.e., model description) files are made part of a fully automated demonstration package.

Keywords

enzyme kinetics; mathematics; covalent inhibition; EGFR kinase

How to Cite

Kuzmic, P. (2015) Automated determination of k_inact and K_i for covalent inhibition using the Omnia assay, BioKin Technical Note TN-2015-02, BioKin Ltd., Watertown MA, [Online] www.biokin.com/TN/2015/02

Download Data and Software Package

Download ~21 MB

After downloading the ZIP archive file, extract the entire package into any arbitrary directory.

The raw data files are located in files named sheet.txt located in sub-directories named data.

The auto-execution data analysis sofware package will run under the Microsoft Windows operating system or emulator (e.g. Wine under Linux or equivalent under Mac OS X).

www.biokin.com/publications/technotes/TN201502.html
Sat Apr 20 18:22:31 2019

Automated determination of kinact and Ki for covalent inhibition using the Omnia assay