In layman terms IC50 or EC50 values are
quantitative measures of a drug needed for a particular biological function. IC50 or EC50 values should be as
small as possible; i.e. the smaller the value, the better is the drug (compound). This goes
by the definition of these terms – IC is the inhibitory concentration and EC is
the effective concentration. If the amount (relates to
concentration) of drug (compound) needed is less for the necessary biological
response, then that drug (compound) should be good.
Conceptually IC50 and EC50
are not different.
In general, EC50 is used when dealing with cell-receptors.
IC50 is used when dealing with enzymes.
In general, EC50 is used when dealing with cell-receptors.
IC50 is used when dealing with enzymes.
IC50 [half maximal
inhibitor concentration]
IC50 is the drug concentration causing 50% inhibition of the desired activity.
IC50 is the drug concentration causing 50% inhibition of the desired activity.
EC50 [half maximal
effective concentration]
EC50 is the drug concentration which induces a response halfway between baseline and maximum.
EC50 is the drug concentration which induces a response halfway between baseline and maximum.
If you are dealing with compounds
which are agonists for a particular cell-receptor, then binding of the agonist
to the cell-receptor will activate a biological process which can be
measured.
In a competitive binding assay, say
antagonist is bound to the cell-receptor deactivating a biological process
(100% deactivation); now adding different amounts of agonist this
antagonist can be displaced causing activation and biological response of
different degree (0% to 100%) based on the amount of compound added.
Concentration required for observing 50% biological response is EC50.
Remember
In
vitro biological activity data: IC50 for inhibitors and EC50 for
agonists/antagonists. Depending on the design of assay protocol for
antagonists IC50 will also be used sometimes. Smaller the IC50/EC50
number - better is the compound. The activity data is expressed in 'nM'
(nanomolar) or 'mM'
(micromolar) units.
You obtain IC50 or
EC50 data only for vitro studies (both in enzymatic assays and
cell-based assays). Enzyme/receptor data vs cell-based
assay results are differentiated by providing the data in this way - IC50
/ EC50 (enzymatic assay) and IC50 / EC50 (cell
assay).
[IC50 or EC50 values are no way related to in vivo data]
IC50 or EC50
are just numbers. The information these numbers give is that the
compound is providing some kind of biological response by binding to the enzyme. However, one should
keep in mind that IC50 or EC50 values will not give you
information about where and how the drugs (compounds) are interacting with
enzyme/receptor (mode of interaction).[IC50 or EC50 values are no way related to in vivo data]
No comments:
Post a Comment
Note: Only a member of this blog may post a comment.