Enzymlogic
Mechanism matters!
The identification of compounds capable to modulate the activity of therapeutic targets relies on using interaction potency as a predictor of in vivo efficacy. Despite that this approach facilitates high-throughput screening of large compound libraries, potency alone fails to reveal the actual pharmacological diversity of compounds.
There are several biochemical features related to the drug-target interaction that drive its mechanism of action and all of them contribute to the ultimate pharmacological response. Although more than 80% of the marketed drugs compete with endogenous effectors, approximately 75% of these inhibitors use an additional mechanism to produce an efficacious response (uncompetitive or non-competitive inhibition, slow dissociation, conformational changes, etc).
We believe that early identification of the driving mechanism of action and assessment of the different biochemical parameters involved in the binding modulation are pivotal in the design of therapeutic agents with improved clinical efficacy and security profiles. Feel free to use this image, just link to www.enzymlogic.com.
Mechanism matters!
The identification of compounds capable to modulate the activity of therapeutic targets relies on using interaction potency as a predictor of in vivo efficacy. Despite that this approach facilitates high-throughput screening of large compound libraries, potency alone fails to reveal the actual pharmacological diversity of compounds.
There are several biochemical features related to the drug-target interaction that drive its mechanism of action and all of them contribute to the ultimate pharmacological response. Although more than 80% of the marketed drugs compete with endogenous effectors, approximately 75% of these inhibitors use an additional mechanism to produce an efficacious response (uncompetitive or non-competitive inhibition, slow dissociation, conformational changes, etc).
We believe that early identification of the driving mechanism of action and assessment of the different biochemical parameters involved in the binding modulation are pivotal in the design of therapeutic agents with improved clinical efficacy and security profiles. Feel free to use this image, just link to www.enzymlogic.com.