Orthosteric Drugs And Allosteric Drugs - Medicinal Chemistry 1.15

There are two types of drugs on the market: orthosteric drugs and allosteric drugs. Orthosteric drugs bind at the active site of the target and directly compete with the endogeneous substrate. One example is the ATP competitive inhibitors that directly compete with the binding of ATP. Allosteric drugs bind elsewhere other than the active site or the orthosteric site, and they don’t directly compete with the endogeneous substrate. One of the earliest allosteric modulators discovered were the GABA positive allosteric modulators.

-About me-

I am a computational chemist in the pharmaceutical industry. I created the Mole Man Chem channel to explain some basic medicinal and biochemistry concepts because I believe the best way to relearn a concept is through teaching.

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0:00 Overview
2:22 Mechanism of action
4:06 ATP-competitive inhibitor
5:31 GABA allosteric regulator