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GPCR
Our G protein-coupled receptor (GPCR) libraries have been designed using both BioFocus' proprietary Thematic Analysis, and commercially available computational tools. We have developed three types of libraries: SoftFocus GPCR, ThemePair GPCR and FieldFocus GPCR.
GPCRs are cell membrane proteins widely found in many organ systems. They form an important part of drug development as one of the most heavily investigated targets for action.
Please contact us for more information, or visit eMolecules to see a list of current stock.
SoftFocus GPCR
The SoftFocus libraries are based around central cores selected to target specific sub-sets of GPCRs. Each core contains two or more points of diversity where specific monomer combinations, chosen using Thematic Analysis, are included.
Each individual library has been selected to target specific sub-sets of GPCRs including family A and family B. SoftFocus GPCR libraries provide selective hits across a range of these receptors and have a track record of delivering:
- Antagonist hit series against a range of aminergic, peptidic, purinergic and lipid targets
- Agonist hit series against several peptidic targets
- Agonist and antagonist hit series against orphan and recently de-orphanized receptors
ThemePair GPCR
The libraries consist of low molecular weight, low cLogP compounds. In a similar way to the SoftFocus GPCR libraries, ThemePair libraries are built around a set of central cores with a range of different substituents. The libraries cover the majority of GPCR targets and are likely to provide agonists, antagonists, and allosteric modulators.
FieldFocus GPCR
Our FieldFocus GPCR (FFG) libraries are the first SoftFocus GPCR libraries directed at the allosteric site of mGluR receptors, a subtype of Family C G-protein coupled receptors. These scaffold ideas were generated from overlays of known mGluR4, mGluR2 and mGluR5 Positive Allosteric Modulators (PAMs). Computational tools such as MOE and Cresset enabled pharmacophore models for the three subtypes to be generated and consistent shape features and H-bonding patterns to be identified. These pharmacophore models have been utilised as templates to generate novel scaffolds for the FFG libraries.
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