About this Author
DBL%20Hendrix%20small.png College chemistry, 1983

Derek Lowe The 2002 Model

Dbl%20new%20portrait%20B%26W.png After 10 years of blogging. . .

Derek Lowe, an Arkansan by birth, got his BA from Hendrix College and his PhD in organic chemistry from Duke before spending time in Germany on a Humboldt Fellowship on his post-doc. He's worked for several major pharmaceutical companies since 1989 on drug discovery projects against schizophrenia, Alzheimer's, diabetes, osteoporosis and other diseases. To contact Derek email him directly: Twitter: Dereklowe

Chemistry and Drug Data: Drugbank
Chempedia Lab
Synthetic Pages
Organic Chemistry Portal
Not Voodoo

Chemistry and Pharma Blogs:
Org Prep Daily
The Haystack
A New Merck, Reviewed
Liberal Arts Chemistry
Electron Pusher
All Things Metathesis
C&E News Blogs
Chemiotics II
Chemical Space
Noel O'Blog
In Vivo Blog
Terra Sigilatta
BBSRC/Douglas Kell
Realizations in Biostatistics
ChemSpider Blog
Organic Chem - Education & Industry
Pharma Strategy Blog
No Name No Slogan
Practical Fragments
The Curious Wavefunction
Natural Product Man
Fragment Literature
Chemistry World Blog
Synthetic Nature
Chemistry Blog
Synthesizing Ideas
Eye on FDA
Chemical Forums
Symyx Blog
Sceptical Chymist
Lamentations on Chemistry
Computational Organic Chemistry
Mining Drugs
Henry Rzepa

Science Blogs and News:
Bad Science
The Loom
Uncertain Principles
Fierce Biotech
Blogs for Industry
Omics! Omics!
Young Female Scientist
Notional Slurry
Nobel Intent
SciTech Daily
Science Blog
Gene Expression (I)
Gene Expression (II)
Adventures in Ethics and Science
Transterrestrial Musings
Slashdot Science
Cosmic Variance
Biology News Net

Medical Blogs
DB's Medical Rants
Science-Based Medicine
Respectful Insolence
Diabetes Mine

Economics and Business
Marginal Revolution
The Volokh Conspiracy
Knowledge Problem

Politics / Current Events
Virginia Postrel
Belmont Club
Mickey Kaus

Belles Lettres
Uncouth Reflections
Arts and Letters Daily
In the Pipeline: Don't miss Derek Lowe's excellent commentary on drug discovery and the pharma industry in general at In the Pipeline

In the Pipeline

« Plavix vs. Effient | Main | Merck, Shopping in the UK? »

November 19, 2009

What Are the Best Med-Chem Books?

Email This Entry

Posted by Derek

I get regular requests to recommend books on various aspects of medicinal chemistry and drug development. And while I have a few things on my list, I'm sure that I'm missing many more. So I wanted to throw this out to the readership: what do you think are the best places to turn? This way I can be more sure of pointing people in the right directions.

I'm interested in hearing about things in several categories - best introductions and overviews of the field (for people just starting out), as well as the best one-stop references for specific aspects of drug discovery (PK, toxicology, formulations, prodrugs, animal models, patent issues, etc.)

Feel free to add your suggestions in the comments, or e-mail them to me. I'll assemble the highest-recommended volumes into a master list and post that. Just in time for the holidays, y'know. . .

Comments (35) + TrackBacks (0) | Category: Life in the Drug Labs | Pharma 101


1. molecular architect on November 19, 2009 12:21 PM writes...

"Real World Drug Discovery - A Chemist's Guide to Biotech and Pharmaceutical Research" by Bob Rydzewski

An excellent guide for the newly graduated chemist written by a talented former co-worker of mine.

Permalink to Comment

2. Seehecht on November 19, 2009 12:38 PM writes...

A general textbook for synthesis:

"Organic Chemistry" by Jonathan Clayden

Molecular Modeling

"Molecular Modelling: Principles and Applications" by Andrew R. Leach

"Molecular Modeling and Simulation" by Schlick

Simulating the Physical World" by Berendsen
"Understanding Molecular Simulations" by Frenkel

Something more general in the light of protein structure:

"Introduction to Protein Structure" by Branden and Tooze

Permalink to Comment

3. TA on November 19, 2009 12:48 PM writes...

"The Practice of MEDICINAL CHEMISTRY" by C. G. Wermuth is a kind of bible.

Permalink to Comment

4. JK on November 19, 2009 1:41 PM writes...

This was a fantastic textbook about properties, ADMET and exp. technologies:
Drug-like Properties: Concepts, Structure Design and Methods: From ADME to Toxicity Optimization von Edward Kerns and Li Di

Permalink to Comment

5. Kutti on November 19, 2009 1:42 PM writes...

I really like: "An Introduction to Medicinal Chemistry" by Graham L. Patrick

Permalink to Comment

6. weirdo on November 19, 2009 1:44 PM writes...

For reading straight through: "Chronicles of Drug Discovery" by Lednicer. Vol. 3 is findable, Vol. 1 & 2 very hard to find, unfortunately.

For looking stuff up: "Burger's Medicinal Chemistry and Drug Discovery" Vol. 1.

Permalink to Comment

7. HelicalZz on November 19, 2009 2:03 PM writes...

Several good ones mentioned. For an industry overview with enough detail to appreciate what others in the company are responsible for I'd recommend "Drugs: From Discovery to Approval" by Rick Ng (2004).

After an introduction it has a few chapters on drug discovery, then preclinical considerations, comments on regulatory responsibilites, GLP - GMP overview, and the clinical process. It ends with a modest history of the industry and some future perspective.


Permalink to Comment

8. Madrid on November 19, 2009 2:49 PM writes...

I agree with TA. Camille Wermuth's "The Practice of Medicinal Chemistry" is the most useful Medicinal Chemistry book. It has all sorts of useful reference tables and great real-world examples of drug development projects. I think it is especially useful to those coming from total synthesis labs, who need to transition into medicinal chemistry.

Permalink to Comment

9. David on November 19, 2009 3:34 PM writes...

Casarett & Doull's Toxicology: The Basic Science of Poisons by Curtis Klaassen is what everyone where I work has on their desks. I understand the new editions are filled with more obscure toxicology info, but the first few chapters had all of the essential info. Editions 4 and 5 were what every I work with learned from.

I also know the same author has a more watered down version : Casarett & Doull's Essentials of Toxicology, but I can't comment as I haven't read it.

Permalink to Comment

10. Wavefunction on November 19, 2009 4:03 PM writes...

1. Real World Drug Discovery by Rydzewski
2. The organic chemistry of drug design and drug action by Silverman
3. Introduction to med chem by Patrick
4. Pharmacology for Chemists by Cannon
5. Molecular Modeling by Leach
6. Drug-like Properties: Concepts, Structure Design and Methods by Kerns and Di
7. Biochemistry by Stryer
8. Goodman and Gilman

Permalink to Comment

11. Jim T on November 19, 2009 4:18 PM writes...

I second the Kerns and Di suggestion. That book is really quite top notch (and for comparison, a much improved text relative to Silverman's).

Permalink to Comment

12. Anonymous on November 19, 2009 4:44 PM writes...

Could I put a call out for process chemistry books, as well as medicinal?

Thank you!

Permalink to Comment

13. Jim T on November 19, 2009 4:52 PM writes...

I'd also be interested in a list of best Biology books for non-biologists (eg for Med Chemists).

I'd put forth The Cell as a good starting point, but I'd love to hear further suggestions.

Permalink to Comment

14. David P on November 19, 2009 5:21 PM writes...

I liked "Pharmacokinetics Made Easy" by Donald J. Birkett. Helped me get going with all things PK.

I also liked the Silverman book (mentioned above), so am interested now in the Kerns and Di book.

Permalink to Comment

15. cliffintokyo on November 19, 2009 7:38 PM writes...

Not a textbook, but for experienced researchers this is a must read:
Ann Reports in Med Chem (ACS)
Great references

Permalink to Comment

16. MattW on November 19, 2009 8:47 PM writes...

I would highly recommend both the text and ACS short course by Kerns and Di.

Permalink to Comment

17. anon on November 19, 2009 8:54 PM writes...

"What color is my Parachute?"

But, seriously, I second the motion for Burkett--great book.

Permalink to Comment

18. drug_hunter on November 19, 2009 9:51 PM writes...

A bit out of left field, perhaps, but:

(1) Why Things Bite Back: Technology and the Revenge of Unintended Consequences. Edward Tenner

(2) Happy Accidents: Serendipity in Major Medical Breakthroughs in the Twentieth Century. Morton Meyers

(3) Up the Infinite Corridor: MIT and the Technical Imagination. Fred Hapgood

(4) Decision Traps: The Ten Barriers to Decision-Making and How to Overcome Them. Edward Russo

PS I am none of these authors!

Permalink to Comment

19. CMCguy on November 19, 2009 11:26 PM writes...

I have a few books in various areas in my personal library but none I can recommend highly. For Medchem, Process, Formulations and general Drug Development areas I have never really encountered any books that were better than working with skilled experts willing to share knowledge. Many books will provide basic overviews for beginners but lack any true depth for application and likewise many can suffer from being written by Academics as course texts but have limited real practical value. In same way generally found reading Literature as effective educational resource, although often hard at first to separate good from bad, that was better than most books (particularly OPRD for Process).

Although dated one general Pharma Industry book/story is The Billion Dollar Battle: Merck Versus Glaxo that covers Science vs Marketing Approaches to Drugs that are now more blurred than ever.

Permalink to Comment

20. processchemist on November 20, 2009 5:07 AM writes...

@ #12

Process chemistry classics:

1) Anderson "Practical process research and development"
2) Repic "Process research and chemical development in the pharmaceutical industry"
3) "Design and optimization in organic synthesis" by Carlson (about DOE at work)

An excellent quick introduction is
Lee and Robinson "Process development"

I strongly suggest these readings to the freshly graduated newcomers in my group.
As far as I know Anderson's book is the only general, systematic approach to process development in pharma.
A note: all these books deal mostly with the chemistry of the drugs approved in the eighties.
This is not so bad, suzuki and buchwald case studies are missing, but there's a huge lot of solid chemistry anyway.

Permalink to Comment

21. Caleb on November 20, 2009 8:21 AM writes...

I'm a little surprised that Richard Silverman's book isn't being mentioned more. So far as I know it is the standard (for better or worse) introductory medchem textbook in most grad programs today. Is this difference in preference due to the difference between academic and industrial medchem?

Permalink to Comment

22. Bombauer on November 20, 2009 8:27 AM writes...

Re: Process Chemistry books

Someone already mentioned Practical Process Research and Development by Neal G. Anderson,

but not a day goes by when I don't use:

'The Pilot Plant Real Book' by Francis X. McConville. It's jam packed with lots of useful data. I'd even suggest that most medicinal chemists should have this around too.

I also agree that 'Drug-like Properties: Concepts, Structure Design and Methods' by Kerns and Di is a great book.

Permalink to Comment

23. processchemist on November 20, 2009 8:44 AM writes...

@ Bombauer
"I'd even suggest that most medicinal chemists should have this around too."

Maybe also a medicinal chemist should have a look at the first chapter, but they don't need for sure a centrifugation or an heat exchange primer :)

Permalink to Comment

24. rob on November 20, 2009 10:32 AM writes...

If you want a book that intuitively explains the the basics of enzyme-inhibitor interactions and gives you a feel for drug discovery at the industrial level, I highly recommend

"Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists" by Copeland

Permalink to Comment

25. RTW on November 20, 2009 1:40 PM writes...

Well - Rather than text books, I esentially learned much from J.Med. Chem. Started reading it as an undergraduate in chemistry in 1978. Been a subscriber ever since.

Also there is Burger's Medicinal Chemistry. One I haven't seen mentioned yet. An old but a good one.

Permalink to Comment

26. CM on November 20, 2009 3:26 PM writes...

I find myself repeatedly coming back to this book (mentioned above a couple of times) as a very useful reference....

Drug-like Properties: Concepts, Structure Design and Methods: From ADME to Toxicity Optimization von Edward Kerns and Li Di

Permalink to Comment

27. Pats on November 20, 2009 9:14 PM writes...

more books of inetrest to medicinal chemists!

A Pharmacology Primer: Theory, Application and Methods by Terry Kenakin

Molecular Biology in Medicinal Chemistry (Methods and Principles in Medicinal Chemistry) by Theodor Dingermann

Fundamentals of Antimicrobial Pharmacokinetic​s and Pharmacodynamic​s by Alexander Vinks

Human Drug Metabolism: An Introduction by Michael D. Coleman

Fluorine in Medicinal Chemistry and Chemical Biology by Iwao Ojima

Bioorganic and Medicinal Chemistry of Fluorine by Jean-Pierre Bégué

Antitargets: Prediction and Prevention of Drug Side Effects (Methods and Principles in Medicinal Chemistry) by Roy J. Vaz

Drug Bioavailability​: Estimation of Solubility, Permeability, Absorption and Bioavailability​ (Methods and Principles in Medicinal Chemistry) by Han van de Waterbeemd

Protein-Ligand Interactions: From Molecular Recognition to Drug Design (Methods and Principles in Medicinal Chemistry) by Hans-Joachim Böhm

Analogue-based Drug Discovery by IUPAC

Fragment-based Approaches in Drug Discovery (Methods and Principles in Medicinal Chemistry) by Wolfgang Jahnke

Fragment-Based Drug Discovery: A Practical Approach by Edward Zartler

Organic Synthesis with Enzymes in Non-Aqueous Media by Giacomo Carrea

A Short History of the Drug Receptor Concept (Science, Technology and Medicine in Modern History) by Andreas-Holger Maehle

Managing Scientists: Leadership Strategies in Scientific Research by Alice M. Sapienza

Permalink to Comment

28. GG on November 21, 2009 12:58 PM writes...

As I suspected: no one can name a good book for patent issues

Permalink to Comment

29. Pats on November 21, 2009 5:36 PM writes...

Molecules with Silly or Unusual Names by May Paul

Permalink to Comment

30. HelicalZz on November 23, 2009 9:27 AM writes...

I know this was a shoutout for Medchem books, but let me also plug a good book for general chemistry interest i.e. a good one to get teens interested in chem.

'Napoleon's Buttons: How 17 Molecules Changed History' by Penny LaCouteur


Permalink to Comment

31. Sili on November 24, 2009 11:14 AM writes...

I know this is probably too newbish a request, but I'd like some suggestions on how to 'revise' org chem for lack of a better word.

I've been out of uni for more than three years now, and have been at an intellectual standstill in that time.

I know all those reactions are in there in my brain, somewhere, but I think I'd be hard pushed to shovel around electrons if given the reactants and products. Much less come up with something if just given a name (actually, I wasn't good at recalling named reactions even back in the day).

Of course, I could just reread my books from one end to the other - I'm pretty much doing that with maths - but I'd welcome any and all shortcuts. For that matter some study techniques would probably be a good idea, too. I relied far too much on my being able to pick stuff up almost osmotically in lectures.

(Not that this is likely to ever help me land a job, since I have too little lab experience, but I don't like having 'lost' that many years of my life.)

Permalink to Comment

32. chris on November 25, 2009 1:03 PM writes...

I really like

Drug Prototypes and Their Exploitation by Walter Sneader, John Wiley & Sons Ltd, ISBN-10: 0471948470

Permalink to Comment

33. Hap on November 25, 2009 1:18 PM writes...

Warren et al. is long (I haven't read it all the way through, and my classes didn't use it) but it's really good. I don't know if it has a workbook - most of Warren's do - but that might be a shortcut, and then you could refer to the text if you realize that you're missing something.

There are lots of prep texts for the GREs and that, but I tried to get one to get biochemistry background and was sorely disappointed.

Permalink to Comment

34. anon on November 25, 2009 7:50 PM writes...

#31 Sili,

You will find what you need at

Check it up.

Permalink to Comment

35. Bonnie Largent on November 4, 2011 2:31 PM writes...

RE: #30.
I have a teenager very interested in Chemistry, showing real aptitude. Can you recommend any more books for smart kids with interest, but not too much education yet?

Permalink to Comment


Remember Me?


Email this entry to:

Your email address:

Message (optional):

The Last Post
The GSK Layoffs Continue, By Proxy
The Move is Nigh
Another Alzheimer's IPO
Cutbacks at C&E News
Sanofi Pays to Get Back Into Oncology
An Irresponsible Statement About Curing Cancer
Oliver Sacks on Turning Back to Chemistry