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 |
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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