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10 Cards in this Set

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Hit

Molecule that has potential to become a lead compound

Types of Scaffolds

Can be linear, cyclic, or peptide framework

Privileged Scaffolds

A molecular framework that can serve as a scaffold for a diverse number of targets

Types of Privileged Scaffolds

These can be spider-like or have tadpole design

Disadvantages of Privileged Scaffolds

1. Limits innovation


2. Inherently promiscuous

Advantages of Peptide Scaffold

1. Easy to synthesize


2. Rapid diversity


May not be orally available if larger than 500Da due to fast metabolism

Spider-like (cyclic) scaffold

This type of scaffold is used to target pharmacodynamic properties

Click Chemistry

This type of chemistry approaches the perfect synthesis.


Cheap


Very high yielding


Specific


Low toxicity


Easily purified

Chemical space

Describes structural diversity and the possible number of structures that could be synthesized

Epitopes

Small molecules involved in fragment-based lead discovery that interact with a target binding site