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CHY8421 : Advanced Methods in Drug Discovery

  • Offered for Year: 2022/23
  • Module Leader(s): Dr Ian Hardcastle
  • Lecturer: Dr Matt Hopkinson
  • Other Staff: Dr James Knight
  • Owning School: Natural and Environmental Sciences
  • Teaching Location: Newcastle City Campus
Semester 1 Credit Value: 10
ECTS Credits: 5.0


To provide an overview of the methods and approaches used in modern drug discovery. To introduce the key stages of a project i.e. target identification and validation, hit discovery, hit validation, hit-to-lead optimisation and lead optimisation. To familiarise students with the most commonly used synthetic methods in medicinal chemistry. To provide students with an understanding of the role of medical imaging in drug discovery, synthetic methods for the incorporation of radioisotopes into biologically active molecules and the quality control requirements for clinical production.

Outline Of Syllabus

The discovery of new drugs to treat unmet needs of patients is a global undertaking. This module covers modern topics in drug discovery, e.g. target validation, hit identification and the pre-clinical optimisation of drugs, along with the preparation and application of radiopharmaceuticals for imaging and therapy. It is illustrated with case studies from recent discovery projects.

Methods in Drug Discovery
Dr IR Hardcastle
List of topics covered:
1 Overview of drug discovery and drug targets
2 Peptide synthesis and peptide libraries
3 Hit identification technologies
4 Small-molecule library synthesis
5 Hit-to-lead strategies and methods
6 Fragment-based drug discovery
7 Lead optimisation - challenges
8 Lead optimisation - in vitro and in vivo DMPK
10 Lead optimisation – synthesis
11 Case studies

Isotopes and Imaging in Drug Discovery
Dr J Knight
List of topics covered:
1 Introduction to radioactivity       , modes of Decay (?, ?, ?), radioactive decay calculations
2 Overview of PET Imaging, dosimetry, common PET radioisotopes
3 Calculating radiochemical yield and molar (radio)activity
4 Radiolabelling with carbon-11
5 Radiolabelling with fluorine-18: electrophilic approach, nucleophilic approach, example
6 Radiolabelling with iodine-124
7 Influence of radiotracer design upon biodistribution and pharmacokinetics
8 PET radiometals: chelation requirements, examples of radiometal-based PET radiotracers
9 PET imaging of hypoxia
10 PET radiotracers as companion diagnostics
11 Radiopharmaceutical Production

Teaching Methods

Teaching Activities
Category Activity Number Length Student Hours Comment
Guided Independent StudyAssessment preparation and completion21:002:00Formative coursework exercises
Guided Independent StudyAssessment preparation and completion21:002:00Summative coursework exercises
Guided Independent StudyAssessment preparation and completion61:006:00Preparation for coursework tasks
Scheduled Learning And Teaching ActivitiesLecture101:0010:00PiP Seminars or online if no PiP due to social distancing
Scheduled Learning And Teaching ActivitiesSmall group teaching101:0010:00PiP seminars covering course materials
Guided Independent StudyIndependent study500:3025:00Accessing prerecorded lecture material and background reading
Guided Independent StudyIndependent study145:0045:00Background reading and practice questions
Jointly Taught With
Code Title
CHY8821Modern Methods in Drug Discovery
Teaching Rationale And Relationship

Key concepts and supporting examples are delivered by online teaching materials. Seminars are used to reinforce key concepts, provide additional examples and to provide practice questions. Formative coursework and case studies will be discussed during seminars.

Assessment Methods

The format of resits will be determined by the Board of Examiners

Other Assessment
Description Semester When Set Percentage Comment
Written exercise1M50Summative assessment of lecture materials
Written exercise1M50Summative assessment of lecture materials
Formative Assessments
Description Semester When Set Comment
Written exercise1MCoursework exercises
Assessment Rationale And Relationship

Two coursework exercises will assess the students’ ability to understand and apply their learning to relevant case studies in drug discovery and imaging, respectively.
Online quizzes revise and reinforce conceptual understanding.

Study Abroad students may request to take their exam before the semester 1 exam period, in which case the format of the paper may differ from that shown in the MOF. Study Abroad students should contact the school to discuss this.

Reading Lists