Off-the-shelf profiling panels

Profile your compounds in our functional-first, natural coupling-oriented GPCR panels for selectivity and off-target effects. You can also contact us with a list of preferred targets so we can build your own custom-panel.

57 GPCR Diversity Panel

Profile the activity of your GPCR modulator over a broad panel representing the main receptor families. Compounds are tested for agonist and antagonist activities in functional assays favoring the natural coupling of each receptor, increasing the chances of picking up allosteric effects.

Target Natural coupling Assay Target Natural coupling Assay
Serotonin 5-HT1A Gi/o cAMP Leukotrien CysLT1 Gq/11 AEQ
Serotonin 5-HT1B Gi/o cAMP Dopamine D1 Golf, Gs cAMP
Serotonin 5-HT2A Gq/11 AEQ Dopamine D2 Gi/o GTPγS
Serotonin 5-HT2B Gq/11 AEQ Dopamine D3 Gi/o GTPγS
Serotonin 5-HT2Cne Gq/11 AEQ Dopamine D4.4 Gi/o GTPγS
Serotonin 5-HT3 Ion channel AEQ Endothelin ETA Gq/11, Gs AEQ
Serotonin 5-HT4e Gs cAMP Endothelin ETB Gq/11, Gi/o AEQ
Serotonin 5-HT5a Gi/o AEQ Ghrelin GHS-R Gq/11 AEQ
Serotonin 5-HT6 Gs cAMP Histamine H1 Gq/11 AEQ
Serotonin 5-HT7 Gs cAMP Histamine H2 Gs cAMP
Adenosine A1 Gi/o cAMP Histamine H3 Gi/o GTPγS
Adenosine A2A Gs cAMP Motilin MTL Gq/11 AEQ
Adenosine A3 Gi/o cAMP Muscarinic M1 Gq/11 AEQ
Adrenergic beta1 Gs cAMP Muscarinic M2 Gi/o GTPγS
Adrenergic beta2 Gs cAMP Muscarinic M3 Gq/11 AEQ
Adrenergic  alpha1A Gq/11 AEQ Muscarinic M4 Gi/o GTPγS
Adrenergic  alpha1B Gq/11 AEQ Muscarinic M5 Gq/11 AEQ
Adrenergic  alpha2A Gi/o GTPγS Nociceptin OFQ (NOP) Gi/o GTPγS
Adrenergic  alpha2B Gi/o GTPγS Neurokinin NK1 Gq/11 AEQ
Adrenergic  alpha2C Gi/o GTPγS Neurokinin NK2 Gq/11 AEQ
Angiotensin AT1 Gq/11 AEQ Neuropeptide NPY1 Gi/o cAMP
Bradykinin B1 Gq/11 AEQ Opioid OP1 Gi/o GTPγS
Cannabinoid CB1 Gi/o cAMP Opioid OP2 Gi/o GTPγS
Cannabinoid CB2 Gi/o cAMP Opioid OP3 Gi/o GTPγS
Cholecystokinin CCK1 Gq/11, Gs AEQ Somatostatin sst4 Gi GTPγS
Cholecystokinin CCK2 Gq AEQ Urotensin-II Gq/11 AEQ
Calcitonin CGRP Gq/11, Gs AEQ Vasopressin V1a Gq/11 AEQ
Chemokine CXCR1 Gi/o GTPγS Vasopressin V1b Gq/11 AEQ
VPAC1 Gs AEQ

CNS panel

Profile your GPCR modulator against a panel of 37 CNS-focused receptors. Compounds are tested for agonist and antagonist activities in functional assays favoring the natural coupling of each receptor, increasing the chances of picking up allosteric effects.

Target Natural coupling Assay Target Natural coupling Assay
Serotonin 5-HT1A Gi/o GTPγS Muscarinic M1 Gq/11 AEQ
Serotonin 5-HT2A Gq/11 AEQ Muscarinic M2 Gi/o GTPγS
Serotonin 5-HT2Ce Gq/11 AEQ Muscarinic M3 Gq/11 AEQ
Adenosine A1 Gi/o cAMP Muscarinic M4 Gi/o GTPγS
Adrenergic  alpha1B Gq/11 AEQ Muscarinic M5 Gq/11 AEQ
Adrenergic  alpha2A Gi/o cAMP Nociceptin OFQ (NOP) Gi/o GTPγS
Bombesin B2 Gq/11 AEQ Neurokinin NK1 Gq/11 AEQ
Cannabinoid CB1 Gi/o cAMP Neurokinin NK2 Gq/11 AEQ
Cholecystokinin CCK2 Gq AEQ Neurokinin NK3 Gq/11 AEQ
Corticotropin CRF1 Gs cAMP Neuropeptide NPY2 Gq/11, Gi/o AEQ
Corticotropin CRF2b Gs cAMP Neurotensin NT1 Gq/11 AEQ
Dopamine D1 Golf, Gs cAMP Opioid OP1 Gi/o GTPγS
Dopamine D2L Gi/o cAMP Opioid OP2 Gi/o GTPγS
Galanin GAL2 Gq/11, Gi/o AEQ Opioid OP3 Gi/o GTPγS
Histamine H1 Gq/11 AEQ Orexin OX1 Gq/11 AEQ
Histamine H3 Gi/o GTPγS Orexin OX2 Gq/11 AEQ
MCH1 Gq/11, Gi/o AEQ Somatostatin sst2 Gi GTPγS
mGluR2 Gi/o cAMP Vasopressin V1b Gq/11 AEQ
PAC1 Gs AEQ

Metabolic panel

Profile your compounds against a panel of 54 GPCR implicated in metabolic regulation and diseases. Compounds are tested for agonist and antagonist activities in functional assays favoring the natural coupling of each receptor, increasing the chances of picking up allosteric effects.

Target Natural coupling Assay Target Natural coupling Assay
Serotonin 5-HT2Ce Gq/11 AEQ Histamine H1 Gq/11 AEQ
Adenosine A1 Gi/o cAMP Histamine H3 Gi/o GTPγS
Adenosine A2B Gs cAMP MCH1 Gq/11, Gi/o AEQ
Adrenergic beta3 Gs cAMP MC4 Gs cAMP
Adrenergic  alpha1B Gq/11 AEQ MC5 Gs cAMP
Adrenergic  alpha2A Gi/o cAMP Muscarinic M1 Gq/11 AEQ
Angiotensin AT1 Gq/11 AEQ Muscarinic M2 Gi/o GTPγS
Bombesin BB1 Gq/11 AEQ Muscarinic M3 Gq/11 AEQ
Bombesin BB2 Gq/11 AEQ NMUR1 Gq/11 AEQ
Bombesin BB3 Gq/11 AEQ Neuropeptide NPY2 Gq/11, Gi/o AEQ
Bradykinin B2 Gq/11 AEQ Neurotensin NT1 Gq/11 AEQ
Calcitonin CGRP Gq/11, Gs AEQ Niacin receptor Gi/o cAMP
Calcium CaS Gq/11, Gi/o AEQ Nociceptin OFQ (NOP) Gi/o GTPγS
Cannabinoid CB1 Gi/o GTPγS Opioid OP2 Gi/o GTPγS
Cannabinoid CB2 Gi/o GTPγS Opioid OP3 Gi/o GTPγS
Chemokine CCR2b Gi/o GTPγS Orexin OX1 Gq/11 AEQ
Chemokine CCR4 Gi/o GTPγS Orexin OX2 Gq/11 AEQ
Chemokine CXCR3 Gi/o GTPγS Oxytocin OT1 Gq/11 AEQ
Cholecystokinin CCK1 Gq/11, Gs AEQ Prokineticin PKR2 Gq/11 AEQ
Corticotropin CRF2b Gs cAMP Prostanoid EP2 Gs cAMP
FFA1 /GPR40 Gq/11 AEQ PTH1 Gs cAMP
FFA2 / GPR43 Gi/o, Gq/11 cAMP Secretin Gs cAMP
Galanin GAL2 Gq/11, Gi/o AEQ Somatostatin sst2 Gi GTPγS
GIP Gs cAMP Urotensin-II Gq/11 AEQ
GLP-1 Gs cAMP Vasopressin V1a Gq/11 AEQ
Glucagon Gs cAMP PAC1 Gs AEQ
GPR7 Gi/o GTPγS VPAC2 Gs AEQ

 

Inflammation panel

Profile your compounds against a panel of 56 GPCR playing a role in immune response and inflammation. Compounds are tested for agonist and antagonist activities in functional assays favoring the natural coupling of each receptor, increasing the chances of picking up allosteric effects.

Target Natural coupling Assay Target Natural coupling Assay
Serotonin 5-HT2A Gq/11 AEQ GPR109a Gi/o AEQ
Adenosine A1 Gi/o cAMP Leukotrien BLT1 Gi/o, Gq/11 AEQ
Adenosine A2A Gs cAMP Leukotrien CysLT1 Gq/11 AEQ
Adenosine A3 Gi/o cAMP Leukotrien CysLT2 Gq/11 AEQ
Complement C3a Gi/o GTPgS Muscarinic M2 Gi/o GTPgS
Complement C5a Gi/o GTPgS Muscarinic M4 Gi/o GTPgS
Bombesin BB1 Gq/11 AEQ Neurokinin NK1 Gq/11 AEQ
Bombesin BB2 Gq/11 AEQ Neuromedin U NMU-1R Gq/11 AEQ
Bradykinin B2 Gq/11 AEQ Neurotensin NTS1 Gq/11 AEQ
Calcitonin CGRP Gq/11, Gs AEQ Opioid OP1 Gi/o GTPgS
Cannabinoid CB2 Gi/o cAMP Opioid OP2 Gi/o GTPgS
Chemokine CCR1 Gi/o GTPgS Opioid OP3 Gi/o GTPgS
Chemokine CCR2b Gi/o AEQ Platelet Activating Factor PAF Gq/11, Gs cAMP
Chemokine CCR3 Gi/o AEQ Prokineticin PKR1 Gq/11 AEQ
Chemokine CCR4 Gi/o AEQ Prostanoid DP Gs cAMP
Chemokine CCR5 Gi/o AEQ Prostanoid EP1 Gq/11 AEQ
Chemokine CCR6 Gi/o AEQ Prostanoid EP3 Gi/o AEQ
Chemokine CCR7 Gi/o AEQ Prostanoid EP4 Gs cAMP
Chemokine CCR8 Gi/o AEQ Prostanoid IP1 Gs cAMP
Chemokine CCR9a Gi/o AEQ Protease-activated PAR2 Gi/o, Gq/11 AEQ
Chemokine CCR10 Gi/o AEQ Protease-activated PAR4 Gi/o, Gq/11 AEQ
Chemokine CXCR2 Gi/o AEQ Sphingosine S1P1 Gi/o AEQ
Chemokine CXCR3a Gi/o AEQ Sphingosine S1P2 Gq AEQ
Chemokine CXCR4 Gi/o AEQ Sphingosine S1P4 Gq/11, Gs AEQ
Chemokine XCR1 Gi/o AEQ Sphingosine S1P5 Gi/o AEQ
Free Fatty Acid GPR43 Gi/o, Gq/11 cAMP PAC1 Gs AEQ
Histamine H1 Gq/11 AEQ VPAC1 Gs AEQ
Histamine H2 Gs cAMP VPAC2 Gs AEQ

 

Sensory Pain panel

Profile your compounds against a panel of 42 GPCR and ion channels implicated in sensory pain. Compounds are tested for agonist and antagonist activities in functional assays favoring the natural coupling of each receptor, increasing the chances of picking up allosteric effects.

Target Natural coupling Assay Target Natural coupling Assay
Serotonin 5-HT1A Gi/o GTPγS Muscarinic M1 Gq/11 AEQ
Serotonin 5-HT2Ce Gq/11 AEQ Muscarinic M2 Gi/o GTPγS
Adenosine A1 Gi/o cAMP Muscarinic M3 Gq/11 AEQ
Adenosine A3 Gi/o cAMP Muscarinic M5 Gq/11 AEQ
Adrenergic beta2 Gs cAMP Nociceptin OFQ (NOP) Gi/o GTPγS
Adrenergic  alpha2A Gi/o cAMP Neurokinin NK1 Gq/11 AEQ
Bradykinin B2 Gq/11 AEQ Neurokinin NK2 Gq/11 AEQ
Cannabinoid CB1 Gi/o cAMP Neurokinin NK3 Gq/11 AEQ
Cannabinoid CB2 Gi/o cAMP NeuromedinNMU2 Gq/11 AEQ
Chemokine CCR2b Gi/o GTPγS Neuropeptide GPR7 Gi/o GTPγS
Chemokine CX3CR1 Gi/o GTPγS Neurotensin NTS1 Gq/11 AEQ
Cholecystokinin CCK2 Gq/11 AEQ Opioid OP1 Gi/o GTPγS
Calcitonin CGRP Gq/11, Gs AEQ Opioid OP2 Gi/o GTPγS
Galanin GAL1 Gi/o GTPγS Opioid OP3 Gi/o GTPγS
GABAB1a/B2 Gi/o cAMP Orexin OX1 Gq/11 AEQ
Glutamate mGlu2 Gi/o cAMP Parathyroid Hormone PTH1 Gq/11, Gs cAMP
Histamine H1 Gq/11 AEQ Platelet-Activating PAF Gq/11, Gs cAMP
Histamine H3 Gi/o GTPγS Prokineticin PKR1 Gq/11 AEQ
MAS related MrgX2 Gq/11 AEQ Protease Activated PAR2 Gq/11, Gi GTPγS
5-HT3 Calcium channel AEQ TRPA1 Calcium channel AEQ
NMDA GRIN-1 none RLB TRPV1 Calcium channel IPOne

Safety panel

Profile your compounds against a panel of 44 GPCR, ion channel, transporters and enzymes for potential safety issues.

GPCR

Family Target Readout Family Target Readout
Adenosine A2A Binding Histamine H2 Binding
Adrenergic α1a Binding Melatonin MT1 Binding
α2a Binding MT2 Binding
β2 Binding Muscarinic Non selective Binding
Cannabinoid CB1 Binding Serotonin 5-HT1A Binding
Dopamine D1 Binding 5-HT1B Binding
D2S Binding 5-HT2A Binding
Opioid σ Binding 5-HT2B Binding
δ Binding Cholecystokinin CCK1 Binding
κ Binding Endothelin ETA Binding
μ Binding ETB Binding
Histamine H1 Binding Vasopressin V1a Binding

Transporters

Family Target Readout
Amine transporter DAT Binding
NET Binding
SERT Binding

Ion channels

Family Target Readout
Ca2+ channel L-type, DHP site Binding
L-type, Verapamil site Binding
K+ channel hERG Binding
Serotonin 5-HT3 Binding
GABA BZD (Central) Binding
NMDA GRIN1 Binding
Nicotinic α4β2 Binding

Enzymes

Family Target Readout
Acetylcholinesterase AChE Fluorescence
Cyclooxygenase COX-2 Colorimetric
Monoamine Oxidase MAO-A Luminescence
Phosphodiesterase PDE-3 HTRF
Phosphodiesterase PDE-4 HTRF
Cytochrome P450 CYP1A2 Luminescence
CYP2C9 Luminescence
CYP2D6 Luminescence
CYP2E1 Luminescence
CYP3A4 Luminescence

Orphan receptors panel

Profile your compounds against a panel of 76 orphan receptors. Receptors will be tested using the most appropriate readout when signaling has been confirmed through constitutive activity (GPR3, GPR6, GPR12, GPR21…) or the use of exogenous/surrogate ligands (GPR17, GPR52…). When no better alternative exists, receptors are tested in the highly sensitive Aequorin (calcium) readout with forced-coupling via a promiscuous Gα16 or a chimeric Gqi5.

Target Assay Target Assay Target Assay
GPR3 cAMP GPR61 cAMP GPR161 (RE2) cAMP
GPR4 cAMP GPR62 cAMP GPR162 (A-2) AEQ
GPR6 cAMP GPR63 AEQ GPR171 (H963) AEQ
GPR12 cAMP GPR65 cAMP GPR173 (SREB3) AEQ
GPR17 cAMP GPR68 (OGR1) IPOne GPR174 (DA6) AEQ
GPR18 AEQ GPR75 AEQ GPR176 (HB954) AEQ
GPR19 (GPR-NGA) AEQ GPR78 cAMP GPR182 (HSGPCP) AEQ
GPR20 AEQ GPR82 AEQ GPRC5A (RAIG1) AEQ
GPR21 cAMP GPR83 (GPR72) AEQ GPRC5B (RAIG2) AEQ
GPR22 AEQ GPR84 cAMP GPRC5C (RAIG3) AEQ
GPR23 (LPAR4) AEQ GPR87 (HG03) IPOne GPRC5D (RAIG4) AEQ
GPR25 AEQ GPR88 cAMP LPA5 (GPR92) IPOne
GPR26 cAMP GPR91 AEQ MAS AEQ
GPR27 (SREB1) AEQ GPR99 AEQ MRG AEQ
GPR30 (GPER) AEQ GPR101 cAMP MRGD AEQ
GPR31 AEQ GPR139 AEQ MRGE AEQ
GPR32 AEQ GPR141 AEQ MRGF (RTA) AEQ
GPR34 cAMP GPR142 IPOne P2Y5 AEQ
GPR35 cAMP GPR146 AEQ P2Y8 AEQ
GPR37 AEQ GPR148 AEQ P2Y10 AEQ
GPR37L1 AEQ GPR149 AEQ TAAR2 (GPR58) cAMP
GPR39 AEQ GPR150 AEQ TAAR5 (PNR) cAMP
GPR45 AEQ GPR151 AEQ TAAR6 (TA4) cAMP
GPR50 AEQ GPR152 AEQ TAAR8 (TA5) cAMP
GPR52 cAMP GPR153 AEQ TAAR9 (TA3) cAMP
GPR55 AEQ

Metabotropic Glutamate receptors panel

Profile your compounds against the 8 mGlu receptors, for agonist, antagonist and allosteric modulator activities.

Target Natural coupling Readout
mGluR1 Gq AEQ
mGluR2 Gi/o cAMP
mGluR3 Gi/o AEQ
mGluR4 Gi/o GTPγS
mGluR5 Gq AEQ
mGluR6 Gi/o GTPγS
mGluR7 Gi/o cAMP
mGluR8 Gi/o GTPγS

Muscarinic receptors panel

Profile your compounds against the 5 Muscarinic receptors, for agonist, antagonist and/or allosteric modulator activities.

Target Natural coupling Assay
M1 Gq/11 AEQ
M2 Gi/o GTPγS
M3 Gq/11 AEQ
M4 Gi/o GTPγS
M5 Gq/11 AEQ

Serotonin receptors panel

Profile your compounds against the 14 Serotonin receptor subtypes, for agonist and antagonist activities.

Target Natural coupling Assay Target Natural coupling Assay
Serotonin 5-HT1A Gi/o GTPγS Serotonin 5-HT2Ce Gq/11 AEQ
Serotonin 5-HT1B Gi/o GTPγS Serotonin 5-HT2Cne Gq/11 AEQ
Serotonin 5-HT1D Gi/o GTPγS Serotonin 5-HT3 Ion channel AEQ
Serotonin 5-HT1E Gi/o GTPγS Serotonin 5-HT4e Gs cAMP
Serotonin 5-HT1F Gi/o GTPγS Serotonin 5-HT5 Gi/o AEQ
Serotonin 5-HT2A Gq/11 AEQ Serotonin 5-HT6 Gs cAMP
Serotonin 5-HT2B Gq/11 AEQ Serotonin 5-HT7 Gs cAMP

Chemokine receptors panel

Profile your compounds against the 21 human chemokine receptors.

Target Natural coupling Assay Target Natural coupling Assay
CCR1 Gi/o GTPγS CXCR1 Gi/o AEQ
CCR2 Gi/o AEQ CXCR2 Gi/o AEQ
CCR3 Gi/o AEQ CXCR3a Gi/o AEQ
CCR4 Gi/o AEQ CXCR3b Gi/o AEQ
CCR5 Gi/o AEQ CXCR4 Gi/o AEQ
CCR6 Gi/o AEQ CXCR5 Gi/o AEQ
CCR7 Gi/o AEQ CXCR6 Gi/o AEQ
CCR8 Gi/o AEQ CXCR7 Gi/o RLB
CCR9a Gi/o AEQ CX3CR1 Gi/o AEQ
CCR10 Gi/o AEQ XCR1 Gi/o AEQ
ChemR23 Gi/o AEQ

Custom profile

If you don’t find a profiling that suits your needs, don’t hesitate to contact us and let us know what you are looking for. We’ll be happy to help you out and design a tailor-made panel!

Contact us