pKa has many impacts in drug discovery, such as:

• Affects absorption, distribution, metabolism and excretion
• Safety profile (off-targets liabilities, e.g. hERG inhibition)
• Binding with membranes, membrane analogs and proteins.
• Can affect drug-receptor binding (salt-bridge formation, desolvation)
• Useful in formulation, manufacturing and process control pKa is the key parameter for other physchem properties, such as
• Lipophilicity
• Solubility
• Permeability
• Dissolution

By Dr. Michael Reutlinger