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 36 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 | Neuropeptide NPY2 | Gq/11, Gi/o | AEQ |
| Corticotropin CRF1 | Gs | cAMP | Neurotensin NT1 | Gq/11 | AEQ |
| Corticotropin CRF2b | Gs | cAMP | Opioid OP1 | Gi/o | GTPγS |
| Dopamine D1 | Golf, Gs | cAMP | Opioid OP2 | Gi/o | GTPγS |
| Dopamine D2L | Gi/o | cAMP | Opioid OP3 | Gi/o | GTPγS |
| Galanin GAL2 | Gq/11, Gi/o | AEQ | Orexin OX1 | Gq/11 | AEQ |
| Histamine H1 | Gq/11 | AEQ | Orexin OX2 | Gq/11 | AEQ |
| Histamine H3 | Gi/o | GTPγS | Somatostatin sst2 | Gi | GTPγS |
| MCH1 | Gq/11, Gi/o | AEQ | Vasopressin V1b | Gq/11 | AEQ |
| mGluR2 | Gi/o | cAMP | 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 41 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 | NeuromedinNMU2 | Gq/11 | AEQ |
| Cannabinoid CB2 | Gi/o | cAMP | Neuropeptide GPR7 | Gi/o | GTPγS |
| Chemokine CCR2b | Gi/o | GTPγS | Neurotensin NTS1 | Gq/11 | AEQ |
| Chemokine CX3CR1 | Gi/o | GTPγS | Opioid OP1 | Gi/o | GTPγS |
| Cholecystokinin CCK2 | Gq/11 | AEQ | Opioid OP2 | Gi/o | GTPγS |
| Calcitonin CGRP | Gq/11, Gs | AEQ | Opioid OP3 | Gi/o | GTPγS |
| Galanin GAL1 | Gi/o | GTPγS | Orexin OX1 | Gq/11 | AEQ |
| GABAB1a/B2 | Gi/o | cAMP | Parathyroid Hormone PTH1 | Gq/11, Gs | cAMP |
| Glutamate mGlu2 | Gi/o | cAMP | Platelet-Activating PAF | Gq/11, Gs | cAMP |
| Histamine H1 | Gq/11 | AEQ | Prokineticin PKR1 | Gq/11 | AEQ |
| Histamine H3 | Gi/o | GTPγS | Protease Activated PAR2 | Gq/11, Gi | GTPγS |
| MAS related MrgX2 | Gq/11 | AEQ | TRPA1 | Calcium channel | AEQ |
| 5-HT3 | Calcium channel | AEQ | TRPV1 | Calcium channel | IPOne |
| NMDA GRIN-1 | none | RLB |
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!
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