Selcia Fragment Library generates hits for GPCR target using TR-FRET

Selcia Fragment Library generates hits for GPCR target using TR-FRET

Professor Steven Charlton discusses the use of the Selcia Fragment Library in his oral presentation at the British Pharmacological Society Conference in London on Monday 11th December 2017. In his presentation, entitled ‘Kinetic profiling of fragments at receptors using TR-FRET’, he demonstrates that a TR-FRET assay for the dopamine D2 receptor group is a sensitive method for detecting low affinity fragment hits at a GPCR, allowing simultaneous determination of kon , koff and Kd. The fragment screen successfully identified fragments of known potent dopamine D2 receptor partial agonists and antagonists.

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