COVID-19 Update: We are currently shipping orders daily. However, due to transit disruptions in some geographies, deliveries may be delayed. To provide all customers with timely access to content, we are offering 50% off Science and Technology Print & eBook bundle options. Terms & conditions.
Pharmacology in Drug Discovery and Development - 2nd Edition - ISBN: 9780128037522, 9780128037539

Pharmacology in Drug Discovery and Development

2nd Edition

Understanding Drug Response

Author: Terry Kenakin
Paperback ISBN: 9780128037522
eBook ISBN: 9780128037539
Imprint: Academic Press
Published Date: 21st October 2016
Page Count: 350
Sales tax will be calculated at check-out Price includes VAT/GST
Price includes VAT/GST

Institutional Subscription

Secure Checkout

Personal information is secured with SSL technology.

Free Shipping

Free global shipping
No minimum order.


Pharmacology in Drug Discovery and Development: Understanding Drug Response, Second Edition, is an introductory resource illustrating how pharmacology can be used to furnish the tools necessary to analyze different drug behavior and trace this behavior to its root cause or molecular mechanism of action. The concepts discussed in this book allow for the application of more predictive pharmacological procedures aimed at increasing therapeutic efficacy that will lead to more successful drug development.

Chapters logically build upon one another to show how to characterize the pharmacology of any given molecule and allow for more informed predictions of drug effects in all biological systems. New chapters are dedicated to the interdisciplinary drug discovery environment in both industry and academia, and special techniques involved in new drug screening and lead optimization.

This edition has been fully revised to address the latest advances and research related to real time kinetic assays, pluridimensional efficacy, signaling bias, irreversible and chemical antagonism, allosterically-induced bias, pharmacokinetics and safety, target and pathway validation, and much more. With numerous valuable chapter summaries, detailed references, practical examples and case studies throughout, Dr. Kenakin successfully navigates a highly complex subject, making it accessible for students, professors, and new researchers working in pharmacology and drug discovery.

Key Features

  • Includes example-based cases that illustrate how the pharmacological concepts discussed in this book lead to practical outcomes for further research
  • Provides vignettes on those researchers and scientists who have contributed significantly to the fields of pharmacology and drug discovery throughout history
  • Offers sample questions throughout the book and an appendix containing answers for self-testing and retention


Graduate students, new researchers and professors in pharmacology, as well as scientists (biologists or chemists) who foresee applying pharmacology to the discovery of new drug molecules from either industry or academic standpoints

Table of Contents

Chapter 1. Pharmacology: The Chemical Control of Physiology

  • Abstract
  • Pharmacology and Cellular Drug Response
  • New Terminology
  • Pharmacological Targets
  • Dose–Response Curves
  • Linking Observed Pharmacology With Molecular Mechanism
  • Descriptive Pharmacology: I
  • Summary
  • Questions
  • References

Chapter 2. Drug Affinity and Efficacy

  • Abstract
  • Introduction
  • New Terminology
  • Agonist Selectivity
  • Affinity
  • Efficacy
  • Drugs With Multiple Efficacies
  • Quantifying Agonist Activity
  • Descriptive Pharmacology: II
  • Summary
  • Questions
  • References

Chapter 3. Predicting Agonist Effect

  • Abstract
  • Agonist Response in Different Tissues
  • New Terminology
  • The Black–Leff Operational Model of Agonism
  • Applying the Black–Leff Model to Predict Agonism
  • Receptor Selectivity
  • Biased Agonist Signaling
  • Descriptive Pharmacology: III
  • Summary
  • Questions
  • References

Chapter 4. Drug Antagonism: Orthosteric Drug Effects

  • Abstract
  • Bimolecular Systems
  • New Terminology
  • What Is Drug Antagonism?
  • Antagonist Potency
  • Mechanism(s) of Receptor Antagonism
  • Orthosteric (Competitive and Noncompetitive) Antagonism
  • Slow Dissociation Kinetics and Noncompetitive Antagonism
  • Partial and Inverse Agonists
  • Antagonist Effects In Vivo
  • Descriptive Pharmacology: IV
  • Summary
  • Questions
  • References

Chapter 5. Allosteric Drug Effects

  • Abstract
  • Introduction
  • New Terminology
  • Protein Allosterism
  • Allosteric Phenotypes
  • Unique Effects of Allosteric Modulators
  • Detecting Allosterism
  • Quantifying Allosteric Effect
  • Descriptive Pharmacology: V
  • Summary
  • Questions
  • References

Chapter 6. Enzymes as Drug Targets

  • Abstract
  • Introduction
  • New Terminology
  • Enzyme Kinetics
  • Enzymes as Drug Targets
  • Reversible Enzyme Inhibition
  • Irreversible Enzyme Inhibition
  • Allosteric Enzyme Modulation
  • Enzyme Activation
  • Intracellular Effects of Enzyme-Active Drugs
  • Summary
  • Questions
  • References

Chapter 7. Pharmacokinetics I: Permeation and Metabolism

  • Abstract
  • The Importance of Drug Concentration
  • New Terminology
  • “Drug-Like” Properties of Molecules
  • Drug Absorption
  • Drug Metabolism
  • Oral Bioavailability
  • Summary
  • Questions
  • References

Chapter 8. Pharmacokinetics II: Distribution and Multiple Dosing

  • Abstract
  • Drugs in Motion: In Vivo Pharmacokinetics
  • New Terminology
  • The Central Compartment and In vivo Clearance
  • Renal Excretion
  • Drug Distribution
  • In Vivo PK
  • Oral Bioavailability
  • Drug–Drug Interactions
  • Nonlinear Pharmacokinetics
  • Scaling Data to Predict Human Pharmacokinetic Behavior
  • Summary
  • Questions
  • References

Chapter 9. In Vivo Pharmacology

  • Abstract
  • Whole Body Drug Response
  • New Terminology
  • The “Dose” in Dose–Response
  • What Constitutes Drug Response?
  • The Importance of Kinetics In Vivo
  • Summary
  • Questions
  • References

Chapter 10. Safety Pharmacology

  • Abstract
  • Introduction
  • New Terminology
  • Safety Versus Toxicity
  • Safety Pharmacology
  • Early Safety Tests
  • Hepatic Toxicity
  • Summary
  • Questions
  • References

Chapter 11. Pharmacology in Drug Discovery

  • Abstract
  • Introduction
  • Unique Aspects of Pharmacology in the Discovery Process
  • Target-Versus System-Based Discovery Strategies
  • Progression Scheme for Drug Discovery
  • Libraries and Molecules as Drug Sources
  • Pharmacological Assay Design
  • High-Throughput Screening
  • Lead Optimization
  • Drug Development
  • Summary
  • Questions
  • References

Appendix A. Answers to Chapter Questions

  • Chapter 1
  • Chapter 2
  • Chapter 3
  • Chapter 4
  • Chapter 5
  • Chapter 6
  • Chapter 7
  • Chapter 8
  • Chapter 9
  • Chapter 10
  • Chapter 11

Appendix B. Derivations and Proofs

  • Successive Saturable Functions Leads to Amplification of Signals
  • The Potency of a Full Agonist Depends on Both Affinity and Efficacy
  • Derivation of the Black–Leff Operational Model
  • Derivation of Variable Slope Black–Leff Operational Model
  • Derivation of the Gaddum Equation for Competitive Antagonism
  • Correction of IC50 to pKB for Competitive Antagonists
  • Derivation of the Equation for Noncompetitive Antagonism
  • Derivation of the Equation for Allosteric Modulation
  • Derivation of the Equation for Allosteric Modulation with Direct Agonism
  • Derivation of the Michaelis–Menten Equation for Enzymes


No. of pages:
© Academic Press 2017
21st October 2016
Academic Press
Paperback ISBN:
eBook ISBN:

About the Author

Terry Kenakin

Terry Kenakin

Terry P. Kenakin is the recipient of the 2008 Poulsson Medal for Pharmacology awarded by the Norwegian Society of Pharmacology for achievements in basic and clinical pharmacology and toxicology. He has also been awarded the 2011 Ariens Award from the Dutch Pharmacological Society and the 2014 Gaddum Memorial Award from the British Pharmacological Society. Having been involved in drug discovery for over 30 years, his interests include the optimal design of drug activity assays systems and quantitative drug receptor theory. He is a member of numerous editorial boards as well as Editor-in-Chief of the Journal of Receptors and Signal Transduction and Current Opinion in Pharmacology. In addition, Dr. Kenakin has authored numerous articles and has also written a number of books on pharmacology.

Affiliations and Expertise

Professor of Pharmacology, The University of North Carolina School Of Medicine, Chapel Hill, NC, USA

Ratings and Reviews