Peakdale launches latest GPCR library

By Wai Lang Chu

- Last updated on GMT

Related tags: Signal transduction

Peakdale Molecular launches its latest G-Protein Coupled Receptor
(GPCR) library, specifically designed to synthesise and
characterise for screening against aminergic GPCR targets.

The 5th Class A GPCR library is the latest expansion of the company's peakexplorer library collection - created to include chemotypes derived from novel Peakdale compounds and were designed using De Novo Pharmaceuticals' in silico pharmacophore modelling and virtual screening algorithms.

A spokesman for Peakdale Molecular told DrugResearcher.com​: "The peakexplorer G5 library extends the chemical space significantly for researchers in the drug discovery area."

"This is a continuation of our GPCR development work and the library is based on eight novel chemotypes, covering over 1200 compounds. This brings the total offering of the peakexplorer libraries to over 27 major chemotypes and more than 6000 purified and characterised drug-like compounds,"​ he added.

"50 per cent of all marketed drugs act on GPCRs, covering almost every therapeutic application,"​ said Ray Fisher, Peakdale Molecular's commercial director.

"Building on the success of these we are pleased to announce that we now plan to develop libraries focusing on other classes of GPCRs."

Peakdale plan to extend its peakexplorer range to include kinase libraries, starting with c-Abl Tyrosine Kinase. Peakdale said that this will further increase Peakdale's offering of drug-like screening compounds to produce high quality, patentable leads in the drive for new drugs.

This latest expansion of the Company's peakexplorer libraries is specifically designed, synthesised and characterised for screening against aminergic GPCR targets. There are estimated to be 2000 GPCR sequences in the human genome, 350 of which are likely to be druggable.

"We have sold libraries G1-G4 to pharmaceutical and biotech companies all over the world, with particular success in the USA and Japan. Researchers in drug discovery aiming to develop new drugs for various diseases are the main customers,"​ the spokesman added.

On commenting on the GPCR market, the spokesman said that the high volume screening market was in decline. However, GPCRs remain an area of very active interest.

"The market is continuing to look for focussed well-designed libraries so, as well as other classes of GPCRs, we are now developing a range of kinase libraries using a fragment-based approach targeted against the c-Abl Tyrosine Kinase,"​ he added.

All the compounds are now available from Peakdale Molecular's website.

Related topics: Clinical Development

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