Table of Contents
What is the difference between lead and hit?
In drug discovery, a hit is any compound that is confirmed to have binding activity to the target and appears on High Throughput Screening. In drug discovery, a lead is the chemical compound with therapeutic or pharmacological activity but suboptimal structure that still require modification.
What does the term hit refer to in drug discovery?
A hit is a compound which has the desired activity in a compound screen. This activity should be confirmed upon retesting. The main motive is to identify molecules that interact with the drug target.
What is PCC in drug discovery?
Jubilant offers integrated drug discovery services spanning across Hit Identification/Target Validation (HI/TV) to Lead Optimization (LO)/Pre-clinical Candidate (PCC), for multiple therapeutic areas.
What is the purpose of hit-to-lead optimization?
In general, the purpose of the hit-to-lead process is to improve the potency, selectivity and physicochemical properties (e.g. solubility and stability) of the compounds for further in vitro and in vivo testing and for subsequent lead optimization.
How was lead discovered?
Discovery of Lead Lead has been known since ancient times. We do not know who discovered it. Its ores are widely distributed and it has a low melting point so it is easily smelted. It was used in antiquity to make statues, coins, utensils and writing tablets.
What is a lead drug?
(leed KOM-pownd) In medicine, a chemical compound that shows promise as a treatment for a disease and may lead to the development of a new drug. Thousands of compounds are tested in the laboratory to find a lead (“leading”) compound that may act on specific genes or proteins involved in a disease.
What are hits and leads in the process of developing new drugs?
The drug discovery process generally follows the following path that includes a hit to lead stage: Target validation (TV) → Assay development → High-throughput screening (HTS) → Hit to lead (H2L) → Lead optimization (LO) → Preclinical development → Clinical development.
What is a hit molecule?
A hit compound is a molecule that shows the desired type of activity in a screening assay. It is important to develop pharmacologically relevant screening assays for hit discovery and for the subsequent hit-to-lead selection process.
What is a counter screen?
Counter-screen – A screen performed in parallel with or after the primary screen. The assay used in the counter-screen is developed to identify compounds that have the potential to interfere with the assay used in the primary screen (the primary assay).
What is lead drug?
Who discovered drugs?
The first modern, pharmaceutical medicine was invented in 1804 by Friedrich Sertürner, a German scientist. He extracted the main active chemical from opium in his laboratory and named it morphine, after the Greek god of sleep.
What is the meaning of lead optimization?
Lead optimization is a critical process that culminates in the identification of a preclinical candidate. The most promising hit series, once they are identified through hit-to-lead efforts, advance into the lead optimization stage of drug discovery.
How was lead used in the past?
Lead was also used widely for fashioning decorative objects. The oldest known lead-containing object made by human hands is a small statue found in Turkey, from 6,500 B.C. Egyptian Pharaohs between 3,000 and 4,000 B.C. used lead to glaze pottery. Lead was useful as well in construction.
What is the origin of lead?
Origin of name : from the Anglo-Saxon word “lead; Latin, plumbum” (the origin of the symbol Pb is the Latin word “plumbum” meaning “liquid silver”.
What is the difference between a lead and a drug?
There are two distinct categories of leads: those that lack any therapeutic use (i.e., “pure” leads), and those that are marketed drugs themselves but have been altered to yield novel drugs.
What are lead molecules?
What is hit to lead?
Optimizing the properties of numerous hits is often a multi-dimensional and challenging process. The hit to lead (H2L) aspect of drug discovery was developed to address these challenges and fully explore the chemistry and biological components of hits to ultimately eliminate any weakly active compounds.
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.
What is the hit to lead stage of drug discovery?
Hit to lead. These lead compounds undergo more extensive optimization in a subsequent step of drug discovery called lead optimization (LO). The hit to lead stage starts with confirmation and evaluation of the initial screening hits and is followed by synthesis of analogs (hit expansion). Typically the initial screening hits display binding…
What happens after hits are identified from a high throughput screen?
After hits are identified from a high throughput screen, the hits are confirmed and evaluated using the following methods: Confirmatory testing: compounds that were found active against the selected target are re-tested using the same assay conditions used during the HTS to make sure that the activity is reproducible.