Monday, January 8, 2018

All about IC50 and EC50


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.

IC50  [half maximal inhibitor concentration]      
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.

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 enzymeHowever, 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).

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