Medicinal and Pharmaceutical Chemistry
Chemistry of drug discovery, design, and development.
Medicinal and Pharmaceutical Chemistry — Chemistry of drug discovery, design, and development.
The field organises around several methodological axes: how the underlying objects are modelled, how they are measured, how they are connected to the rest of chemistry, and which empirical phenomena drive open questions. The references below anchor the topic in established treatments and current literature.
Foundations and core methods
A primary reference for this area is An Introduction to Medicinal Chemistry (Patrick, 2017), which lays out the core concepts that govern medicinal and pharmaceutical chemistry. The treatment frames the subject within the broader context of chemistry and motivates the conceptual vocabulary used throughout this page. The discussion here cites this work as a general anchor rather than for a specific claim, since the exact contribution claim is treated cautiously in line with the Charted sourcing policy.
A complementary perspective comes from The Organic Chemistry of Drug Design and Drug Action (Silverman and Holladay, 2014), which provides further background on the methods and results most relevant to medicinal and pharmaceutical chemistry. Together with the previous reference, it establishes the standard expectations for how practitioners approach the topic in current practice.
Open questions
Open methodological questions in medicinal and pharmaceutical chemistry include the transferability of the standard methods to harder regimes, the integration of newer measurement and modelling tools, and the connection to neighbouring subfields of chemistry. Future revisions of this page will deepen the treatment as more primary literature is curated.
Prerequisites
Sources
- textbook · primary · 2017An Introduction to Medicinal Chemistrypatrick-2017
- textbook · primary · 2014The Organic Chemistry of Drug Design and Drug Actionsilverman-2014, holladay-2014
In context
Where this topic sits in the prerequisite graph. Click any node to jump.
Explore
- 01
Drug Design Principles
Hit-to-lead, lead optimization, and the rule-of-five for drug-likeness.
- 02
Structure-Based Drug Design
Crystal and cryo-EM structures, docking, and scaffold growth from binding poses.
- 03
Fragment-Based Drug Discovery
Fragment screening by NMR, SPR, and crystallography; fragment growing and linking.
- 04
Covalent Drug Discovery
Targeted covalent inhibitors, warhead design, and reversible covalent chemistry.
- 05
PROTACs and Targeted Protein Degradation
Bifunctional degraders, molecular glues, and ternary-complex design.
- 06
ADME and Pharmacokinetics
Absorption, distribution, metabolism, excretion, and PK/PD modeling.
- 07
Bioisosterism and Scaffold Hopping
Classical and non-classical bioisosteres for property optimization.
- 08
Peptide and Macrocycle Therapeutics
Cyclic peptides, stapled peptides, and beyond-rule-of-five medicinal chemistry.
- 09
Antibody–Drug Conjugates
Linker chemistry, payload design, and conjugation strategies for ADCs.
- 10
Prodrug Chemistry
Designed bioactivation for improved PK, targeting, and tolerability.
- 11
DNA-Encoded Libraries
DEL synthesis, screening, and hit triage for ultra-large compound collections.
- 12
Antimicrobial Chemistry
Antibiotic, antiviral, and antifungal scaffolds and resistance-breaking design.
- 13
Oncology Medicinal Chemistry
Kinase inhibitors, DDR drugs, and chemistry of targeted cancer therapeutics.
- 14
CNS Medicinal Chemistry
Brain-penetrant drugs, blood-brain barrier, and neuropharmacology scaffolds.
- 15
Pharmaceutical Formulation
Solid-state forms, polymorphs, amorphous solid dispersions, and excipient chemistry.
- 16
Process Chemistry
Route scouting, scale-up, and manufacturing-friendly synthesis of APIs.
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