The one day 'Introduction to Drug Discovery' course: 

                        (A 200+ figure manual plus reference list is  provided and four individual/team exercises are also included).

Step-by-step from project initiation through lead compound/biologic identification to selection of candidate for clinical trials.

  • Selection of a target human protein whose modulation results in the desired therapeutic effect.
  • Obtaining a compound/biologic capable of carrying this out in vitro and in animal disease models.
  • Prediction of the compound/biologic’s safety in humans via in vitro and animal model studies.  
The Science Base of Drug Discovery - the Biology, Medicinal Chemistry, ADMET and Informatics required to reach key discovery milestones.  Focus on small molecule drug discovery.                                                                                

                                                                     Course Schedule                                                Typical drug Discovery Processes: Classical routes for successful drug discovery. 
  • Key Milestones and decision points.
  • Scientific Skills Base Required ( Medicinal Chemistry, Biology, ADMET, Informatics)
  • Small Molecule v. Biologic Drugs
  • Target Product Profile.
  • Scientific activities and their phasing

Project Initiation:

Matching the project to the organisation's needs.

  •  Best Practice in Project Initiation:
  •  Use of a Target Product Profile (TPP).

Target Protein Selection:

Identifying the right protein drug target for the disease.

 How to select the right protein drug target for the disease.

  • Drug action at the cellular level.
  • Target tractability.
  • Translational research.
  • Target proteins for existing small molecule drugs. (GPCR, Ion Channels, Nuclear Receptors, Kinases).

 Lead / Lead Series Identification:

The path to obtaining a lead compound with the quality to become a Clinical Candidate.

  • Scientific activities and their phasing.
  • Key Scientific Tools in Drug Discovery:

                  -   Genomics, Proteomics, Chemogenomics, Stem cell biology.

                  -   Low Throughput screening, High Throughput Screening, High Content Screening, Biostructural Analysis (X-Ray).

  • Potency and selectivity analysis - key Constants and Parameters.
  • In vitro ADMET methodologies and their application:

    - Cellular permeability - adsorption at the gut and blood brain barrier.

    - Cyp 450 / P-glycoprotein / glucuronidation / metabolic stability.

    - Protein binding.

Medicinal Chemistry:
  • Chemical and physical properties of drug-like compounds.
  • Structure activity relationships (SAR).
  • The company compound library and its use.
  • Cheminformatics.
  • Virtual compound screening.
Animal Model Studies:

  • Efficacy in animal models of disease:
  • Animal models in: Inflammation, Cancer, HIV-AIDS.
  • Essential attributes of a Lead Compound.

Clinical Candidate Identification:

Final ‘polishing’ of the lead compound with a view to its further Development.

  • Essential attributes of a clinical candidate.
  • Manufacture.
  • Formulation.
  • Pharmacokinetics (PK) and Pharmacodynamics (PD).
  • Toxicology Assays.
  • hERG.

Course Ends