Table of Contents
What are leads in drug discovery?
A lead compound (/ˈliːd/, i.e. a “leading” compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but may nevertheless have suboptimal structure that requires …
Is there a difference between leads and drugs?
The difference between leads and drugs can be, therefore, expressed as follows: Lead structures exhibit, on average, less molecular complexity (less molecular weight, less number of rings and rotatable bonds), are less hydrophobic (lower CLogP and LogD74) and have lower polarizability (less CMR), and are, not …
What is hit identification?
What is hit identification (hit ID)? The goal of hit identification, also known as hit-finding or hit discovery, is to deliver a compound with confirmed activity against a biological target. This target compound is called a “hit” and is often the starting point for chemistry activities.
What does lead Optimisation mean?
Definition. Lead optimization is the process by which a drug candidate is designed after an initial lead compound is identified.
What is a lead drug?
Lead compound is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but may nevertheless have suboptimal structure that requires modification to fit better to the target. Lead drugs offer the prospect of being followed by back-up compounds called analogs.
What are the three major phases of drug discovery?
Phases Stages
- Step 1: Discovery and Development.
- Step 2: Preclinical Research.
- Step 3: Clinical Development.
- Step 4: FDA Review.
- Step 5: FDA Post-market Safety Monitoring.
What is hit to lead (H2L) in drug discovery?
Hit to lead ( H2L) also known as lead generation is a stage in early drug discovery where small molecule hits from a high throughput screen (HTS) are evaluated and undergo limited optimization to identify promising lead compounds.
What is the difference between a a hit and a lead?
A hit is a positive result in some type of an activity assay. It may be spurious. A lead is a compound that forms the structural basis of a drug analog project. Considerable data is collected on activity, tox, pk, etc. based on the different structures. If successful, a compound( s) are chosen for development as…
What is hit discovery and why is it important?
This plays a significant role in its biological activity with the target. The main approach to hit discovery is high throughput screening (HTS); assays that are used to screen an entire compound library against a new drug’s target. Knowledge-based screening (also known as focused-based screening), is another crucial aspect of hit discovery.
What is a hit compound in drug development?
Once a promising drug target has been identified, researchers aim to identify molecules that can interact with the target to produce desired biological effects. A hit compound is a molecule that shows the desired type of activity in a screening assay.