Course Description

Course description

Lipophilicity and biomimetic properties to support drug discovery

Introductory free short description of the drug discovery process. 

How do medicinal chemists design the required properties into a candidate molecule?

How to measure octanol/water partition coefficients?


What will you learn?
  • You learn what will be the topics of the more detailed follow up courses.

Useful Resources

Look for more detailed courses on

Lipophilicity

Biomimetic properties

How to measure protein binding?

How to measure phospholipid binding?

How lipophilicity and biomimetic binding depends on the charge?

How to apply the measured lipophilicity and protein binding data to estimate in vivo drug distribution?

Links to other courses:

Lipophilicity course

Biomimetic properties course

Abraham solvation equation course

pH dependence of lipophilicity course

Solubility in early drug discovery course

Permeability in early drug discovery course

In vivo models course


Need Help? Contact the tutor

[email protected]




Director, Honorary Professor at UCL School of Pharmacy

Klara Valko

Leaving GSK after 22 years of service, she is now founder director of Bio-Mimetic Chromatography Ltd providing data analysis, biomimetic HPLC method development and measurements, in vivo drug distribution modelling and various courses for pharmaceutical companies. She is an Honorary Professor to the UCL School of Pharmacy since 2004; leading the Physchem/ADME module for the Drug Discovery MSc course. She has developed biomimetic HPLC methods for high throughput measurements of serum albumin, glycoprotein and phospholipid binding. She invented the Chromatographic Hydrophobicity Index (CHI) for the fast determination of a compound’s lipophilicity using generic gradient reversed phase chromatography. She has built mathematical statistical models based on measured properties to predict human in vivo drug distribution, such as, volume of distribution, DRUGeff max and tissue/plasma partition. She has contributed to the Drug Efficiency Index (DEI) concept and dose estimation based on DEI. She has published over 100 papers that have achieved over 3000 citations. She has written a book on “Physicochemical and Biomimetic Properties in Drug Discovery; Chromatographic Techniques for lead optimization” published by Wiley in 2014. Currently, she is working on the second edition of the “Handbook of Analytical Separations” Volume 1 “Separation Methods in Drug Synthesis and Purification” published by Elsevier.  

Reviews

5 star rating

Excellent course.

Vesna Gabelica Markovic

This course is excelent. The subject is described in a simple and clear way. I suggest it to all medicinal chemists.

This course is excelent. The subject is described in a simple and clear way. I suggest it to all medicinal chemists.

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