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GPCRProfiler™ Service Safety & Disease Panels

Date post: 11-Mar-2015
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The current pace of drug discovery often demands that in-house drug discovery efforts be supplemented. GPCRProfiler can either bolster current screening capacity or jump-starting drug discovery efforts on new targets or therapeutic areas. Beyond lead identification, it is obvious that the successful progression of a lead compound to clinical drug is to have a solid knowledge base surrounding the compound. Our GPCRProfiler is the first complete cell-based functional platform utilizing a common validated readout for over 155 GPCRs, representing all 3 GPCR classes and over 57 ligand families. The foundation of GPCRProfiler is our proprietary ChemiScreen Stable Calcium Optimized GPCR Cell Lines used for real-time calcium mobilization assays to rapidly, reliably and reproducibly screen and profile compounds. Using one platform allows ligands to be screened with identical buffer conditions and incubation times for the entire spectrum of GPCRs, regardless of native G protein coupling, for easy analysis and comparison.
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Data Sheet With GPCRProfiler Service, you receive: The flexibility to choose from 1 to 140 different receptors to screen against Your choice of 15 different service panels, including more than 57 distinct ligand families, 2 safety panels and 11 disease-focused panels A functional readout that includes both agonist and antagonist data The experience and knowledge of the Millipore scientists—the assay experts Whether you need to profile your lead compounds to evaluate potential side-effects or identify the therapeutic target for a biological active molecule, GPCRProfiler Service Safety and Disease Panels can help you choose which GPCR targets will best address your research needs. Millipore’s GPCRProfiler service is the first complete cell-based profiling service, providing functional data using a single readout, which makes analyzing and interpreting data easy and straightforward. Built with flexibility in mind, GPCRProfiler panels enable you to choose from over 140 different receptors to meet your needs. Or choose from our wide selection of disease and liability service panels, which include 55 distinct ligand families, two different safety panels and 11 disease- focused panels. Developed by the Millipore scientists, these service panels help you identify which receptors are most appropriate for your research. In fact, you can call on the Millipore team of GPCR experts at any time, providing excellent support for your in-house research and screening efforts. Our expertise in cell-based assays is just one reason professionals everywhere continue to turn to Millipore for their GPCR profiling needs. When it comes to GPCRs, Millipore has the information know-how to help you take on the drug discovery challenges you face. GPCRProfiler Service Safety & Disease Panels The premier provider of functional cell-based assays for GPCR screening and profiling
Transcript
Page 1: GPCRProfiler™ Service Safety & Disease Panels

Data SheetData Sheet

With GPCRProfiler Service, you receive:• Theflexibilitytochoosefrom1to140different

receptorstoscreenagainst

• Yourchoiceof15differentservicepanels,

includingmorethan57distinctligandfamilies,

2safetypanelsand11disease-focusedpanels

• Afunctionalreadoutthatincludesbothagonist

andantagonistdata

• TheexperienceandknowledgeoftheMillipore

scientists—theassayexperts

Whether you need to profile your lead compounds

to evaluate potential side-effects or identify the

therapeutic target for a biological active molecule,

GPCRProfiler Service Safety and Disease Panels can help

you choose which GPCR targets will best address your

research needs.

Millipore’s GPCRProfiler service is the first complete

cell-based profiling service, providing functional data

using a single readout, which makes analyzing and

interpreting data easy and straightforward. Built with

flexibility in mind, GPCRProfiler panels enable you to

choose from over 140 different receptors to meet your

needs. Or choose from our wide selection of disease and

liability service panels, which include 55 distinct ligand

families, two different safety panels and 11 disease-

focused panels. Developed by the Millipore scientists,

these service panels help you identify which receptors

are most appropriate for your research. In fact, you can

call on the Millipore team of GPCR experts at any time,

providing excellent support for your in-house research

and screening efforts.

Our expertise in cell-based assays is just one reason

professionals everywhere continue to turn to Millipore

for their GPCR profiling needs. When it comes to GPCRs,

Millipore has the information know-how to help you take

on the drug discovery challenges you face.

GPCRProfiler™ServiceSafety&DiseasePanelsThe premier provider of functional cell-based assays for GPCR screening and profiling

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A non-peptideAcetylcholine (muscarinic)

M1 HTS044C • • • • • • • •

A non-peptideAcetylcholine (muscarinic)

M2 HTS115C • • • • • • • • • • • •

A non-peptideAcetylcholine (muscarinic)

M3 HTS116C • • • • • • • • •

A non-peptideAcetylcholine (muscarinic)

M4 HTS117C • • • • • •

A non-peptideAcetylcholine (muscarinic)

M5 HTS075C • • • • • •A non-peptide Adenosine A1 HTS047C • • • • • • • • • • • •A non-peptide Adenosine A2B HTS051C • • • • • • •A non-peptide Adenosine A3 HTS052C • • • • • • • • • •A non-peptide Adrenergic a1A HTS087C • • • • • •A non-peptide Adrenergic a1B HTS158C • • • • • •A non-peptide Adrenergic a1D HTS216C • • • • •A non-peptide Adrenergic a2A HTS096C • • • • • • • •A non-peptide Adrenergic a2B HTS157C • •A non-peptide Adrenergic b1 HTS104C • • • •

GPCRPROFILeR COMPReHeNSIVe SeRVICe PANeLS

Panels Subcategories, target tissues and/or description

FULL Complete listing of receptors available on the GPCRProfiler service panel.

DIVeRSITY Diverse collection of receptors, including one representative member of each ligand family.

SAFeTY PANeLS BroadSafety-A comprehensive panel of receptors with known or anticipated side-effects or liabilities.

FocusedSafety-A focused panel of receptors known to be linked to common side-effects or liabilities.

DISeASe PANeLS Cancer

Cardiovascular-Heart, Thrombosis, Angiogenesis, Atherosclerosis, Hypertension, Flushing

Digestive&Renal-GI, Renal, Liver, Urinary, Prostate

Inflammation-Inflammation / Arthritis, Allergy, Itching, Dermatitis, Sepsis, Fever, Immunosuppression, Viral infection, HIV, MS, WHIM

Metabolic-Appetite, Diabetes, Metabolic, Obesity, Dry mouth, Growth, Hyperthyroidism, Body Temperature Regulation, Osteoporosis, Calcium Homeostasis

NeurologicalDisorders-Parkinson’s, Epilepsy, Cognition, Neuroprotection, Alzheimer’s, Nausea, MS

PsychiatricDisorders-Psychosis, Depression, Mood / Anxiety, Addiction, Tourette’s, ADHD

Reproduction-Reproduction, Fetal Development, Pre-term Labor, New Born Health

Respiratory-Respiratory, Asthma

Sensory-Pain, Migraine, Vision, Macular Degeneration, Pupil Size, Glaucoma, Auditory, Smell

Sleep-Sedation, Narcolepsy

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A non-peptide Adrenergic b2 HTS073C • • • • • • • •A non-peptide Adrenergic b3 HTS159C • • •A peptide Anaphylotoxin C3aR HTS016C • • • •A peptide Anaphylotoxin C5aR HTS017C • • • • • •A peptide Angiotensin AT1 HTS064C • • • • • • • •A peptide Bombesin BB1 HTS123C • • •A peptide Bombesin BB2 HTS084C • • • • • • • • • • • •A peptide Bombesin BB3 HTS160C • • • • •A peptide Bradykinin B2 HTS041C • • • • • • • • • • • •B peptide Calcitonin CGPR1 HTS172C • • • • • • • • • •C non-peptide Calcium sensor CaS HTS137C • • • • •A non-peptide Cannabinoid CB1 HTS019C • • • • • • •A non-peptide Cannabinoid CB2 HTS020C • • • • • • • • •A peptide Chemoattractant ChemR23 HTS071C • • •A peptide Chemokine CCR1 HTS005C • • • • • •A peptide Chemokine CCR10 HTS014C • • • • •A peptide Chemokine CCR2B HTS007C • • • • • • • • • • • •A peptide Chemokine CCR3 HTS008C • • • • • •A peptide Chemokine CCR4 HTS009C • • • • •A peptide Chemokine CCR6 HTS011C • • • • •A peptide Chemokine CCR7 HTS012C • • • • •A peptide Chemokine CCR8 HTS013C • • •A peptide Chemokine CCR9 HTS036C • • • •A peptide Chemokine CX3CR1 HTS015C • • • • • •A peptide Chemokine CXCR1 HTS001C • • • • •A peptide Chemokine CXCR2 HTS002C • • • • • •A peptide Chemokine CXCR3 HTS003C • • • • • •A peptide Chemokine CXCR4 HTS004C • • • • •A peptide Chemokine

XCR1 / GPR5

HTS053C • •A peptide Cholecystokinin CCK1 HTS184C • • • •A peptide Cholecystokinin CCK2 HTS083C • • • • • • • • •B peptide CRF Receptor CRF1 HTS023C • • • • • • •B peptide CRF Receptor CRF2 HTS024C • • •C non-peptide

Glutamate (metabotropic)

mGlu2 HTS146C • • • • •

GPCRPROFILeR COMPReHeNSIVe SeRVICe PANeLS

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A non-peptide Dopamine D1 HTS102C • • • • • •A non-peptide Dopamine D2L HTS039C • • • • • •A non-peptide Dopamine D5 HTS129C • • • • • •A peptide Endothelin ETA HTS070C • • • • • • •A peptide Endothelin ETB HTS046C • • • • • • •A non-peptide Free Fatty Acid

FFA1 / GPR40

HTS038C • •

A non-peptide Free Fatty AcidFFA2 / GPR41

HTS135C • •

A non-peptide Free Fatty AcidFFA3 / GPR43

HTS063C • • •C non-peptide GABAB GABAB1b HTS119C • • • • •A peptide Galanin GAL1 HTS094C • • • • • •A peptide Galanin GAL2 HTS186C • • • • •B peptide Glucagon GIP HTS134C • •B peptide Glucagon GLP-1 HTS163C • • • • • •B peptide Glucagon glucagon HTS112C • •B pept ide Glucagon

secretin receptor

HTS174C • • • •

C non-peptideGlutamate

(metabotropic)mGlu2 HTS146C • • • • •

A peptideGlycoprotein

hormoneTSH HTS133C • • • • • • • • •

A non-peptide Histamine H1 HTS050C • • • • • • • • • • •A non-peptide Histamine H2 HTS086C • • • • • •A non-peptide Histamine H3 HTS029C • • • • • • • •

A non-peptide a-KetoglutarateOXGR1, GPR99, GPR80

HTS191C • • •

A peptideKiSS1-derived

peptideKiSS1 / GPR54

HTS032C • • • •A non-peptide Leukotriene BLT1 HTS042C • • • •A non-peptide Leukotriene CysLT1 HTS061C • • • • • •A non-peptide Leukotriene CysLT2 HTS088C • • • •A non-peptide Lysophospholipid LPA1 HTS089C • • • • • • • • •A non-peptide Lysophospholipid LPA3 HTS130C • • • • • •A non-peptide Lysophospholipid S1P1 HTS176C • • • • • • • •A non-peptide Lysophospholipid S1P2 HTS078C • • • • •A non-peptide Lysophospholipid S1P3 HTS097C • • • • • • •A non-peptide Lysophospholipid S1P4 HTS192C • • • • •

GPCRPROFILeR COMPReHeNSIVe SeRVICe PANeLS

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A non-peptide Lysophospholipid S1P5 HTS193C • • • • • • •A non-peptide Mas-related gene MrgD HTS206C • •A peptide Mas-related gene MRGX2 HTS058C • • •

A peptideMelanin-

concentrating hormone

MCHR1 HTS025C • • • • •

A peptideMelanin-

concentrating hormone

MCHR2 HTS026C •

A peptide Melanocortin MC2 HTS021C • • • • •A peptide Melanocortin MC4 HTS105C • • •A peptide Melanocortin MC5 HTS155C • • • • •

A peptide MotilinMotilin

Receptor / MTLR

HTS121C • • • • •

A peptide Neuromedin U NMU1 HTS062C • • • • • •A peptide Neuromedin U NMU2 HTS098C • • •A peptide Neuropeptide B / W

NPBW1 / GPR7

HTS180C • • • • • •A peptide Neuropeptide Y Y2 HTS066C • • • • • • • • • •A peptide Neuropeptide Y Y4 HTS204C • • • • • •A peptide Neurotensin NTR1 HTS034C • • • • • • • • • • •A peptide

Prolactin-releasing peptide

PRP HTS057C • • • • • • • • • • •A peptide N-formylpeptide FPR1 HTS018C • • • • • •A peptide N-formylpeptide FPRL1 HTS056C • • • • •A non-peptide Nicotinic Acid GPR109A HTS201C • • • • • • • • • •A peptide Opioid d HTS100C • • • • • • • • • •A peptide Opioid k HTS095C • • • • • • • • • • •A peptide Opioid m HTS101C • • • • • • • • • • •A peptide Opioid

NOP /ORL1

HTS040C • • • • • • • •A peptide Orexin OX1 HTS175C • • • • • • • • • • •A peptide Orexin OX2 HTS045C • • • • •A peptide Oxytocin OT HTS090C • • • • • • • •A peptide Peptide P518

GPR103 / QRFP

HTS189C • • •

A non-peptideP2Y / Purinergic (metabotropic)

P2Y1 HTS049C • • • • • • •

A non-peptidePlatelet Activating

FactorPAF HTS076C • • • • • • • • •

A peptide Prokineticin PK1 HTS074C • • • • • •A peptide Prokineticin PK2 HTS182C • • • • • • •

GPCRPROFILeR COMPReHeNSIVe SeRVICe PANeLS

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A peptideProlactin-releasing

peptidePRP HTS057C • • • • • • • • • • •

A non-peptide Prostanoid DP HTS091C • • • • • • • •A non-peptide Prostanoid EP1 HTS099C • • • • • • • • • •A non-peptide Prostanoid EP2 HTS185C • • • • • • • • • •A non-peptide Prostanoid EP3 HTS092C • • • • • • • • •A non-peptide Prostanoid EP4 HTS142C • • • • • • • •A non-peptide Prostanoid FP HTS093C • • • • • •A non-peptide Prostanoid IP1 HTS131C • • • • • • • •A non-peptide Prostanoid TP HTS081C • • • • • • •A peptide Protease-activated PAR2 HTS037C • • • • • •A peptide Protease-activated PAR4 HTS162C • • • • • • • •B peptide PTH receptor PTH1 HTS030C • • • • • • •B peptide PTH receptor PTH2 HTS173C • • • •A non-peptide Serotonin 5-HT1A HTS107C • • • • • • •A non-peptide Serotonin 5-HT2A HTS082C • • • • • •A non-peptide Serotonin 5-HT2B HTS109C • • • • • •A non-peptide Serotonin 5-HT2C HTS132C • • • • • • • •A peptide Somatostatin sst2 HTS028C • • • • • • • •A peptide Somatostatin sst3 HTS171C • • •A peptide Somatostatin sst4 HTS125C • • • • •A peptide Somatostatin sst5 HTS139C • • •A non-peptide

SPC / LPC / proton-sensor

GPR68 / OGR1

HTS153C • • •

A peptideTackykinin /neurokinin

NK1 HTS080C • • • • • • • • • •

A peptideTackykinin /neurokinin

NK2 HTS144C • • • • • •

A peptideTackykinin /neurokinin

NK3 HTS190C • • • • • • •A peptide TRH TRH HTS126C • • • • •A peptide Urotensin II

UT / GPR14

HTS033C • • • • • • •A peptide Vasopressin V1A HTS059C • • • • • • • •A peptide Vasopressin V1B HTS136C • •A peptide Vasopressin V2 HTS060C • • • • •B peptide VIP / PACAP

PAC1 long isoform

HTS114C • • • • • • • • • • • • • •B peptide VIP / PACAP VPAC1 HTS043C • • • • • • • • • •B peptide VIP / PACAP VPAC2 HTS079C • • • • • • • • • • •

GPCRPROFILeR COMPReHeNSIVe SeRVICe PANeLS

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Full Panel - 143 Targets (Screening for both Agonist and Antagonist activity)

Family Receptor Family Receptor

Acetylcholine (muscarinic) M1, M2, M3, M4, M5 Mas-related gene MrgD, MRGX2

Adenosine A1, A2B, A3 Melanin-concentrating hormone MCHR1, MCHR2

Adrenergic a1A, a1B a2A, a2B, b1, b2, b3 Melanocortin MC2, MC4, MC5

Anaphylotoxin C3aR, C5aR Motilin Motilin Receptor / MTLR

Angiotensin AT1 Neuromedin U NMU1, NMU2

Bombesin BB1, BB2, BB3 Neuropeptide B / W NPBW1 / GPR7

Bradykinin B2 Neuropeptide Y Y2, Y4

Calcitonin CGPR1 Neurotensin NTR1

Calcium sensor CaS N-formylpeptide FPR1, FPRL1

Cannabinoid CB1, CB2 Nicotinic Acid GPR109A

Chemoattractant ChemR23 Opioid d, k, µ, NOP / ORL1

Chemokine

CCR1, CCR10, CCR2B, CCR3, CCR4, rhesus macaque CCR5,

CCR6, CCR7, CCR8, CCR9, CX3CR1, CXCR1, CXCR2, CXCR3,

CXCR4, XCR1 / GPR5

Orexin OX1, OX2

Cholecystokinin CCK1, CCK2 Oxytocin OT

CRF Receptor CRF1, CRF2 P2Y / Purinergic (metabotropic) P2Y1

Dopamine D1, D2L, D5 Platelet Activating Factor PAF

Endothelin ETA, ETB Prokineticin PK1, PK2

Free Fatty AcidFFA1 / GPR40, FFA2 / GPR41,

FFA3 / GPR43Prolactin-releasing peptide PRP

GABAB GABAB1b ProstanoidDP, EP1, EP2, EP3, EP4, FP, IP1,

TP

Galanin GAL1, GAL2 Protease-activated PAR2, PAR4

GlucagonGIP, GLP-1, glucagon, secretin

receptorPTH receptor PTH1, PTH2

Glutamate (metabotropic) mGluR2 Serotonin5-HT1A, 5-HT2A, 5-HT2B,

5-HT2C

Glycoprotein hormone TSH Somatostatin sst2, sst3, sst4, sst5

GnRH GnRH / LHRH SPC / LPC / proton-sensor GPR68 / OGR1

Histamine H1, H2, H3 Tackykinin / neurokinin NK1, NK2, NK3

a-Ketoglutarate OXGR1 / GPR99 / GPR80 TRH TRH

KiSS1-derived peptide KiSS1 / GPR54 Urotensin II UT / GPR14

Leukotriene BLT1, CysLT1, CysLT2 Vasopressin V1A, V1B, V2

LysophospholipidLPA1, LPA3, S1P1, S1P2, S1P3,

S1P4, S1P5VIP / PACAP

PAC1 long isoform, VPAC1, VPAC2

FULL PANeL Millipore’s Full Panel includes every receptor available on the GPCRProfiler service panel. Use it to identify targets

or drug mechanism of actions (MOAs) of biologically active compounds or extracts, or to provide other information

about your compounds, such as potential side effects.

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Diversity Panel - 57 Targets (Screening for both Agonist and Antagonist activity)

M2 ChemR23 mGlu2 MC2 OT sst4

A3 CCR2B TSHMotilin Receptor /

MTLRGPR103 / QRFP GPR68 / OGR1

b2 CCK2 GnRH / LHRH NMU1 P2Y1 NK1

C5aR CRF1 H1 NPBW1 / GPR7 PAF TRH

AT1 D5OXGR1 / GPR99 /

GPR80Y2 PK1 UT / GPR14

BB2 ETB KiSS1 / GPR54 NTR1 PRP V1A

B2 FFA3 / GPR43 CysLT1 FPR1 IP1 PAC1 long isoform

CGPR1 GABAB1b S1P3 GPR109A PAR4

CaS GAL1 MRGX2 k PTH1

CB2 GLP-1 MCHR1 OX1 5-HT2B

Broad Safety Panel - 117 Targets (Screening for both Agonist and Antagonist activity)

M1 B2 CCK2 S1P2 NOP / ORL1 5-HT1A

M2 CGPR1 CRF1 S1P3 OX1 5-HT2A

M3 CaS D1 S1P4 OX2 5-HT2B

M4 CB1 D2L S1P5 OT 5-HT2C

M5 CB2 D5 MCHR1 P2Y1 sst2

A1 CCR1 ETA MC2 PAF sst3

A2B CCR10 ETB MC4 PK1 sst4

A3 CCR2B GAL1 MC5 PK2 sst5

a1A CCR3 GAL2Motilin Receptor /

MTLRPRP NK1

a1B CCR4 TSH NMU1 DP NK2

a1DCCR5, rhesus

macaqueGnRH / LHRH NPBW1 / GPR7 EP1 NK3

a2A CCR6 H1 Y2 EP2 UT / GPR14

b1 CCR7 H2 Y4 EP3 V1A

b2 CCR8 H3 NTR1 EP4 V2

b3 CCR9 BLT1 FPR1 FP PAC1 long isoform

C3aR CX3CR1 CysLT1 FPRL1 IP1 VPAC1

C5aR CXCR1 CysLT2 GPR109A TP VPAC2

AT1 CXCR2 LPA1 d PAR2

BB2 CXCR3 LPA3 k PAR4

BB3 CXCR4 S1P1 µ PTH1

DIVeRSITY PANeL Our Diversity Panel includes one representative receptor from each ligand family. Like the Full Panel, the Diversity

Panel can also help to identify targets or MOAs of your active compounds.

BROAD SAFeTY & FOCUSeD SAFeTY PANeLS Choose from two different Safety Panels to provide information about whether a new lead series or chemical entity

may have any potential side effects. The Broad Safety Panel is a comprehensive panel of receptors with known or

anticipated side effects or liabilities, while the Focused Safety Panel includes a more narrow set of receptors known

to be linked to common side effects or liabilities.

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Broad Safety Panel - 117 Targets (Screening for both Agonist and Antagonist activity)

M1 B2 CCK2 S1P2 NOP / ORL1 5-HT1A

M2 CGPR1 CRF1 S1P3 OX1 5-HT2A

M3 CaS D1 S1P4 OX2 5-HT2B

M4 CB1 D2L S1P5 OT 5-HT2C

M5 CB2 D5 MCHR1 P2Y1 sst2

A1 CCR1 ETA MC2 PAF sst3

A2B CCR10 ETB MC4 PK1 sst4

A3 CCR2B GAL1 MC5 PK2 sst5

a1A CCR3 GAL2Motilin Receptor /

MTLRPRP NK1

a1B CCR4 TSH NMU1 DP NK2

a1DCCR5, rhesus

macaqueGnRH / LHRH NPBW1 / GPR7 EP1 NK3

a2A CCR6 H1 Y2 EP2 UT / GPR14

b1 CCR7 H2 Y4 EP3 V1A

b2 CCR8 H3 NTR1 EP4 V2

b3 CCR9 BLT1 FPR1 FP PAC1 long isoform

C3aR CX3CR1 CysLT1 FPRL1 IP1 VPAC1

C5aR CXCR1 CysLT2 GPR109A TP VPAC2

AT1 CXCR2 LPA1 d PAR2

BB2 CXCR3 LPA3 k PAR4

BB3 CXCR4 S1P1 µ PTH1

Cancer Panel - 27 Targets (Screening for both Agonist and Antagonist activity)

A3CCR5, rhesus

macaqueCCK2 S1P1 NTR1 sst2

BB2 CCR6 ETA S1P3 EP1 sst3

CB2 CCR7 KiSS1 / GPR54 S1P4 EP2

CCR10 CXCR2 LPA1 S1P5 PAR2

CCR2B CXCR4 LPA3 MC2 PAR4

Cadiovascular Panel - 65 Targets (Screening for both Agonist and Antagonist activity)

M1 b1 CXCR3 S1P3 PRP 5-HT2A

M2 b2 D1 Y2 DP 5-HT2B

M3 AT1 D5 Y4 EP1 sst2

A1 BB3 ETA FPRL1 EP2 TRH

A2B B2 ETB GPR109A EP3 UT / GPR14

A3 CGPR1 GLP-1 d EP4 V1A

a1A CCR2B TSH NOP / ORL1 FP V2

a1B CCR3 LPA1 OX1 IP1 PAC1 long isoform

a1DCCR5, rhesus

macaqueLPA3 OT TP VPAC1

a2A CX3CR1 S1P1 P2Y1 PAR4 VPAC2

a2B CXCR2 S1P2 PAF PTH1

DISeASe PANeLS Choose one or more of the Disease Panels to meet your needs. They include receptors for Cancer, Cardiovascular,

Inflammation, Metabolic, Respiratory and more. Use these panels in your drug discovery campaigns to reveal whether

a given lead compound hits a single disease-related target or multiple targets that may act synergistically to treat a

disorder.

Focused Safety Panel - 76 Targets (Screening for both Agonist and Antagonist activity)

M1 B2 ETA MC5 PAF 5-HT2B

M2 CGPR1 ETBMotilin Receptor /

MTLRPK1 5-HT2C

M3 CB1 GAL1 NMU1 PRP sst4

A1 CB2 TSH Y2 DP NK1

A3 CCR1 GnRH / LHRH NTR1 EP2 NK3

a1A CCR2B H1 FPR1 EP3 UT / GPR14

a1D CX3CR1 H2 GPR109A FP V1A

a2A CXCR1 H3 d IP1 V2

b1 CCK2 BLT1 k TP PAC1 long isoform

b2 CRF1 CysLT1 µ PAR4 VPAC1

C5aR D1 LPA1 OX1 PTH1 VPAC2

AT1 D2L LPA3 OT 5-HT1A

BB2 D5 S1P3 P2Y1 5-HT2A

BROAD SAFeTY & FOCUSeD SAFeTY PANeLS

Page 10: GPCRProfiler™ Service Safety & Disease Panels

10

Digestive & Renal Panel - 62 Targets (Screening for both Agonist and Antagonist activity)

M2 B2 CRF1 Y4 EP1 NK3

M3 CGPR1 ETA NTR1 EP2 TRH

M4 CaS ETB GPR109A EP3 V1A

M5 CB2 GLP-1 d EP4 V2

A1 CCR1 secretin receptor k PAR2 PAC1 long isoform

A2B CCR2B TSH m PAR4 VPAC1

a1A CCR3 H2 NOP / ORL1 PTH2 VPAC2

a1D CCR6 MC5 OX1 5-HT2B

b2 CCR9Motilin Receptor /

MTLRPK1 sst2

AT1 CCK1 NMU1 PK2 NK1

BB2 CCK2 Y2 PRP NK2

Inflammation Panel - 62 Targets (Screening for both Agonist and Antagonist activity)

M2 CB2 CCR9 CysLT1 d PAR2

M4 ChemR23 CX3CR1 CysLT2 k PAR4

A1 CCR1 CXCR1 S1P1 m 5-HT2A

A2B CCR10 CXCR2 S1P2 PAF NK1

A3 CCR2B CXCR3 S1P4 PK1 PAC1 long isoform

C3aR CCR3 CXCR4 S1P5 DP VPAC1

C5aR CCR4 XCR1 / GPR5 NMU1 EP1 VPAC2

BB1CCR5, rhesus

macaqueFFA3 / GPR43 NTR1 EP3

BB2 CCR6 H1 FPR1 EP4

B2 CCR7 H2 FPRL1 IP1

CGPR1 CCR8 BLT1 GPR109A TP

Metabolic Panel - 67 Targets (Screening for both Agonist and Antagonist activity)

M1 B2 GAL2 MC4 OX2 sst2

M2 CGPR1 GIP MC5 OT sst5

M3 CaS GLP-1 NMU2 GPR103 / QRFP GPR68 / OGR1

A1 CB1 glucagon NPBW1 / GPR7 P2Y1 UT / GPR14

A2B CB2 secretin receptor Y2 PK2 V1A

a1B CCR2B TSH Y4 PRP PAC1 long isoform

a2A CCR4 H1 NTR1 EP2 VPAC2

b3 CXCR3 H3 GPR109A EP4

AT1 CCK1OXGR1 / GPR99 /

GPR80k TP

BB1 CRF2 LPA1 m PTH1

BB2 FFA1 / GPR40 MCHR1 NOP / ORL1 PTH2

BB3 FFA2 / GPR41 MC2 OX1 5-HT2C

DISeASe PANeLS

Page 11: GPCRProfiler™ Service Safety & Disease Panels

11

Reproduction Panel - 39 Targets (Screening for both Agonist and Antagonist activity)

A1 CCR10 GnRH / LHRH NPBW1 / GPR7 PRP TRH

A3 CCR7 KiSS1 / GPR54 Y4 DP PAC1 long isoform

a1A CXCR4 LPA1 GPR109A EP2 VPAC1

AT1 CRF1 LPA3 k EP3 VPAC2

BB3 D2L S1P1 m EP4

B2 ETA S1P2 OT FP

CCR1 ETB S1P5 PK2 PTH1

Digestive & Renal Panel - 62 Targets (Screening for both Agonist and Antagonist activity)

M2 B2 CRF1 Y4 EP1 NK3

M3 CGPR1 ETA NTR1 EP2 TRH

M4 CaS ETB GPR109A EP3 V1A

M5 CB2 GLP-1 d EP4 V2

A1 CCR1 secretin receptor k PAR2 PAC1 long isoform

A2B CCR2B TSH m PAR4 VPAC1

a1A CCR3 H2 NOP / ORL1 PTH2 VPAC2

a1D CCR6 MC5 OX1 5-HT2B

b2 CCR9Motilin Receptor /

MTLRPK1 sst2

AT1 CCK1 NMU1 PK2 NK1

BB2 CCK2 Y2 PRP NK2

Neurological Disorders Panel - 50 Targets (Screening for both Agonist and Antagonist activity)

M1 CCR2B GAL2 S1P5 OX1 sst4

M2 CXCR3 GLP-1 Y2 P2Y1 NK1

M4 CCK1 secretin receptor NTR1 PAF PAC1 long isoform

M5 CCK2 mGlu2 FPR1 PRP VPAC1

A1 D1 TSH FPRL1 EP1 VPAC2

a1B D2L H1 GPR109A EP2

BB2 D5 H2 d 5-HT1A

B2 GABAB1b H3 m 5-HT2C

CB1 GAL1 S1P1 NOP / ORL1 sst2

Psychiatric Disorders Panel - 37 Targets (Screening for both Agonist and Antagonist activity)

M4 CCK2 TSH d 5-HT1A V1B

M5 CRF1 H1 k 5-HT2A PAC1 long isoform

A1 CRF2 H3 m 5-HT2C

a1B D1 LPA1 NOP / ORL1 sst2

a2A D2L MCHR1 OX1 NK1

BB2 GAL2 Y2 OX2 NK2

CB1 mGlu2 NTR1 EP1 NK3

Respiratory Panel - 38 Targets (Screening for both Agonist and Antagonist activity)

M1 C5aR CXCR1 S1P3 EP2 PAC1 long isoform

M2 BB2 CXCR2 S1P4 EP3 VPAC1

M3 B2 GABAB1b S1P5 IP1 VPAC2

A2B CGPR1 H1 d TP

A3 CCR2B CysLT1 m NK1

b2 CCR3 CysLT2 PAF NK2

C3aR CCR4 S1P1 DP NK3

Inflammation Panel - 62 Targets (Screening for both Agonist and Antagonist activity)

M2 CB2 CCR9 CysLT1 d PAR2

M4 ChemR23 CX3CR1 CysLT2 k PAR4

A1 CCR1 CXCR1 S1P1 m 5-HT2A

A2B CCR10 CXCR2 S1P2 PAF NK1

A3 CCR2B CXCR3 S1P4 PK1 PAC1 long isoform

C3aR CCR3 CXCR4 S1P5 DP VPAC1

C5aR CCR4 XCR1 / GPR5 NMU1 EP1 VPAC2

BB1CCR5, rhesus

macaqueFFA3 / GPR43 NTR1 EP3

BB2 CCR6 H1 FPR1 EP4

B2 CCR7 H2 FPRL1 IP1

CGPR1 CCR8 BLT1 GPR109A TP

Metabolic Panel - 67 Targets (Screening for both Agonist and Antagonist activity)

M1 B2 GAL2 MC4 OX2 sst2

M2 CGPR1 GIP MC5 OT sst5

M3 CaS GLP-1 NMU2 GPR103 / QRFP GPR68 / OGR1

A1 CB1 glucagon NPBW1 / GPR7 P2Y1 UT / GPR14

A2B CB2 secretin receptor Y2 PK2 V1A

a1B CCR2B TSH Y4 PRP PAC1 long isoform

a2A CCR4 H1 NTR1 EP2 VPAC2

b3 CXCR3 H3 GPR109A EP4

AT1 CCK1OXGR1 / GPR99 /

GPR80k TP

BB1 CRF2 LPA1 m PTH1

BB2 FFA1 / GPR40 MCHR1 NOP / ORL1 PTH2

BB3 FFA2 / GPR41 MC2 OX1 5-HT2C

DISeASe PANeLS

Page 12: GPCRProfiler™ Service Safety & Disease Panels

www.millipore.com/offices

Millipore is a registered trademark of Millipore Corporation.GPCRProfiler, ChemiScreen, the M mark, and Advancing Life Science Together are trademarks of Millipore Corporation.Lit. No. DS1798EN00 08DD019 06/08 Printed in U.S.A. DD SBU-08-00453© 2008 Millipore Corporation, Billerica, MA 01821 U.S.A. All rights reserved.

Sensory Panel - 46 Targets (Screening for both Agonist and Antagonist activity)

M1 B2 GAL1 NPBW1 / GPR7 PK2 5-HT1A

M2 CGPR1 mGlu2 NTR1 PRP 5-HT2C

M3 CB1 H1 d EP1 NK1

M5 CB2 H3 k EP3 NK2

A1 CCR2B LPA1 m FP NK3

A3 CX3CR1 MrgD NOP / ORL1 IP1 PAC1 long isoform

a2A CCK2 MRGX2 OX1 PAR2

b2 GABAB1b NMU2 PAF PTH2

Sleep Panel - 24 Targets (Screening for both Agonist and Antagonist activity)

M2 BB2 k PK2 EP4 V1A

M3 H1 OX1 PRP 5-HT1A PAC1 long isoform

A1 H3 OX2 DP 5-HT2C VPAC1

a2A Y2 OT EP1 UT / GPR14 VPAC2

FOR ADDITIONAL INFORMATION OR TO PLACe AN ORDeRMillipore continually strives to develop innovative

products for your GPCR research. GPCRProfiler service

is part of our popular array of offerings that enable you

to accelerate the drug discovery process by providing a

better, more efficient way to profile your compounds. To

place an order, visit us online or call 1-800-MILLIPORE. To learn more, visit www.millipore.com/gpcrprofiler or

[email protected] for service inquires.

DISeASe PANeLS


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