Peptide lead optimization is to improve upon a lead molecule that demonstrates activity at a target of interest by optimizing its potency or selectivity at the target and its absorption, distribution, metabolism and elimination (ADME) properties. For a successful peptide lead optimization, access to a reliable in vitro assay system is of utmost importance. This allows for precise SAR evaluations based on the binding affinity of peptide analogs to the target protein.

In order to make a compound a drug sample, at least five basic attributes need to be considered including potency, bioavailability, duration, safety, and pharmaceutical acceptability.

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