GPCR Drug Discovery | NCE Discovery


Heptares technology for the first time allows powerful, precision SBDD drug discovery methods to be applied to discovering novel small molecules that modulate historically undruggable or challenging GPCRs. These techniques, which are routinely used for soluble enzyme targets, can now be applied to StaR® protein from early screening of chemical libraries, through hit selection and lead optimisation.

Heptares' approach is expected to radically improve the chances of discovering safer and more selective drugs targeting GPCRs that may overcome issues such as low selectivity, poor pharmacokinetic profiles or toxicity, often present in existing chemotypes identified by other means. This approach has been validated by the generation of highly differentiated candidates to multiple challenging/intractable targets.

Leveraging its deep GPCR expertise and fully-integrated drug discovery platform, Heptares is generating a broad pipeline of first-in-class and best-in-class GPCR-targeted candidates, for serious CNS and metabolic indications, including Alzheimer's disease, Parkinson's disease, schizophrenia, depression, chronic insomnia, addiction, migraine and diabetes. See Pipeline.

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Structure of a StaR® protein in complex with a selective inverse agonist (green). View into the orthosteric binding cavity from extracellular perspective. StaR® protein atoms represented as spheres / spacefill with adjusted depth cue.

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