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INTRODUCING-EUROFINS-BEACON-DISCOVERY-The-GPCR-Experts.Pdf INTRODUCING EUROFINS BEACON DISCOVERY The GPCR Experts Eurofins Discovery welcomes a new company to its organization, Beacon Discovery. Eurofins Beacon Discovery is an industry leader in GPCR drug discovery offering an integrated approach for challenging GPCR targets. The Team has identified in excess of 30 pre-clinical candidates of which more than 20 programs have moved successfully into clinical development. Key to Eurofins Beacon Discovery’s success is the ability to critically evaluate new targets with knowledge acquired from over 20 years of working on this crucial target class. • Industry leading know-how on all aspects of GPCR biology • Complete GPCR drug discovery solution utilizing advanced discovery platforms and technologies • Renowned expertise in prosecuting orphan GPCR targets across therapeutic areas PARTNERING FOR SUCCESS Eurofins Beacon Discovery’s reputation in the field of GPCR discovery is built on the success of its partnerships with biotech and pharma companies worldwide. Beacon scientists take a flexible approach in all of their collaborations with the purpose of designing high quality compounds by employing seasoned medicinal chemistry supported by state-of-the-art computational tools. This chemistry approach combined with a powerful expertise in assay development, mode of action, and biomarker establishment capabilities for over 20 years makes Eurofins Beacon Discovery the partner of choice for your GPCR programs. Join our community of partners who have trusted Eurofins Beacon Discovery to get the biology right in their relentless endeavor to discover and develop life changing drugs. Learn more about GPCR Integrated Drug Discovery and ways to collaborate with Eurofins Beacon Discovery at beacondiscovery.com WORKING WITH EUROFINS BEACON DISCOVERY Support from Concept to Clinic INTEGRATED WORKFLOW DESIGNED WITH YOUR UNIQUE PROGRAM IN MIND Eurofins Beacon Discovery employs an integrated workflow which supports GPCR discovery programs from target validation to providing pre-clinical candidates, with a proven success rate of reaching the clinic. The combination of Eurofins Beacon Discovery’s 600,000 compound screening library and expert biology with proficient medicinal chemistry support is a valid approach to addressing GPCR targets and has been particularly effective for orphan GPCR. Disease Signaling HTS GPR109B GPR109A P2RY11 MRGPRX3 F2RL3 FFAR2 FFAR3 MRGPRX1 FFAR1 F2RL2 MRGPRX4 GPR81 MRGPRX2 OXER1 GPR31 MRGPRD MRGPRG UTR2 MRGPRE Agonist MRGPRF P2RY8 F2R F2RL1 GPR55 GPR18 GPR20 GPR92 GPR35 OXGR1 GPR91 MAS1L P2RY1 TBXA2R P2RY6 P2RY2 PTGER1 P2RY4 MAS1 GPR132 GPR65 PTGER3PTGFR GPR4 GPR68 PTGER2 PTAFR GPR34 600 K PTGDR GPR171 GPR87 PTGER4PTGIR P2RY14 P2RY12 P2RY13 EBI2 LGR6 CYSLTR1 LGR5 CYSLTR2 LGR4 GPR17 LHCGRTSHR GPR174 P2RY10 FSHR GPR23 RXFP2 LPAR6 4R RXFP1 GPR152 LTB OP Antagonist LTB4R2 GPR85OPN3N5 C5AR1 GPR173 C5L2 GPR1 GPBAR1GPR27 C3AR1 CMKLR1 GPR88 Compounds GPR135 GPR33 CRTH2 GPR62 GPR32R1 GPR61 FP G FPR2 PR78 GPR26 FPR3 GPR75 KISS1R GPR150 GALR1 GALR2 ADR GALR3 ADRA2AA MCHR1 PAN/NAM 2 ADRA2 C MCHR2 OPRL1K1 Lead ADRA1BB ADRA1A OPR ADRA1D OPRD1 OPRM1 HTR4 NPBWR1 Expansion HRH2 NPBWR2 HITS DRD3 SSTR1 SSTR4 β DRD2 -Arrestin DRD4 SSTR2 ADRB2 SSTR3 ADRB1 SSTR5 GPCR ADRB3 GPER RXFP3 HTR6 RXFP4 HTR1F Series AGTRL1 HTR1E GPR25 HTR1D GPR15 HTR1B AGTR1 HTR1A Class A AGTR2 DRD5 BDKRB1 DRD1 BDKRB2 HTR7 CXCR7 HTR5A GPR182 TAAR8 CCBP2 TAAR6 XCR1 TAAR9 CCRL2 CX3CR1 Virtual Screening TAAR5 TAAR3 CCR8 TAAR2 CCR4 CCR1 TAAR1 CCR3 HRH1 CCR2 HTR2C CCR5 HTR2A CXCR1 α HTR2B CXCR2 CHRM5 CXCR5 CHRM1 CCR10 CHRM3 CXCR3 β CHRM4 CXCR4 CHRM2 CXCR6 (Billions of Compounds) HRH4 CCRL1 γ HRH3 CCR9 EDG3 CCR6 EDG1 CCR7 EDG5 GPR161 EDG8 GPR101 EDG6 GPR84 Class B Class C GPR50 EDG4 MTNR1A EDG2 MTNR1B EDG7 GPR151 MC5R GPR82 MC4R GPR141 MC3R GPR160 MC2R GPR148 MC1R GPR149 GPR6 GPR153 GPR3 GPR162 GABBR2 GPR12 CNR2 CASR GPRC6A CNR1 GRM1 GRM5 GPR119 GRM2 GRM3 Functional & Binding ADORA2B GRM6 GPCR Assays Available ADORA2A GRM7 ADORA3 GRM4 ADORA1GPR52 GRM8 GPR21 GABBR1 Binding NTSR2 CALCR β-Arrestin NTSR1 CALCRL MLNR CRHR1 GHSR CRHR2 Calcium GLP2R GLP1R NMU2R GCGR cAMP NMU1R GIPR GPR39TRHR PTHR1 PTHR2 Internalization GHRHR ADCYAP1R1 γ GPR142 VIPR2 GTP S SCTR GPR139PPYR1 VIPR1 GPR146 NPY1R DARC NPY5R GPR176 GPR22 GPR37 PRLHR GPR37L1 GPR83 EDNRA EDNRB BRS3 NPY2R GRPR NMBR GPR103 GPR19 GPR45 GPR120 G-Proteins NPFFR2 NPFFR1 HCRTR2 TACR3 TACR1 HCRTR1 TACR2 OXTR CCKBR CCKAR AVPR2 NPSR1 GPR63 AVPR1B GNRHR AVPR1A PROKR2 PROKR1 Mechanistic Studies & β-Arrestin Literature Vetting GPCR Targets Alternatives Lead Clinical Optimization Candidate Tool Compounds HO Synthesis & Testing N Profile Optimization Expression In vitro Pharmacology Medicinal Chemistry Primary Cell Biology Computational Approaches In vivo Model Development ADME/PK TOX/Safety Figure 1. Take advantage of Eurofins Beacon Discovery’s sophisticated and integrated workflow to fast-track your GPCR drug discovery programs. For more information on Eurofins Beacon Discovery and how we can support your GPCR discovery programs, please visit beacondiscovery.com © 2021 Eurofins Discovery. All Rights Reserved. 21243 061521.
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