Therapeutic area profiling panels

Profile your compounds in our functional-first, natural coupling-oriented GPCR panels focused on specific therapeutic areas. You can also contact us with a list of preferred targets so we can build your own custom-panel.

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

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