Preset GPCR panels to profile your compounds - EuroscreenFast

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-HT_1A	G_i/o	cAMP	Leukotrien CysLT1	G_q/11	AEQ
Serotonin 5-HT_1B	G_i/o	cAMP	Dopamine D₁	G_olf,G_s	cAMP
Serotonin 5-HT_2A	G_q/11	AEQ	Dopamine D₂	G_i/o	GTPγS
Serotonin 5-HT_2B	G_q/11	AEQ	Dopamine D₃	G_i/o	GTPγS
Serotonin 5-HT_2Cne	G_q/11	AEQ	Dopamine D_4.4	G_i/o	GTPγS
Serotonin 5-HT₃	Ion channel	AEQ	Endothelin ET_A	G_q/11,G_s	AEQ
Serotonin 5-HT_4e	G_s	cAMP	Endothelin ET_B	G_q/11,G_i/o	AEQ
Serotonin 5-HT_5a	G_i/o	AEQ	Ghrelin GHS-R	G_q/11	AEQ
Serotonin 5-HT₆	G_s	cAMP	Histamine H₁	G_q/11	AEQ
Serotonin 5-HT₇	G_s	cAMP	Histamine H₂	G_s	cAMP
Adenosine A₁	G_i/o	cAMP	Histamine H₃	G_i/o	GTPγS
Adenosine A_2A	G_s	cAMP	Motilin MTL	G_q/11	AEQ
Adenosine A₃	G_i/o	cAMP	Muscarinic M₁	G_q/11	AEQ
Adrenergic beta₁	G_s	cAMP	Muscarinic M₂	G_i/o	GTPγS
Adrenergic beta₂	G_s	cAMP	Muscarinic M₃	G_q/11	AEQ
Adrenergic alpha_1A	G_q/11	AEQ	Muscarinic M₄	G_i/o	GTPγS
Adrenergic alpha_1B	G_q/11	AEQ	Muscarinic M₅	G_q/11	AEQ
Adrenergic alpha_2A	G_i/o	GTPγS	Nociceptin OFQ (NOP)	G_i/o	GTPγS
Adrenergic alpha_2B	G_i/o	GTPγS	Neurokinin NK₁	G_q/11	AEQ
Adrenergic alpha_2C	G_i/o	GTPγS	Neurokinin NK₂	G_q/11	AEQ
Angiotensin AT₁	G_q/11	AEQ	Neuropeptide NPY₁	G_i/o	cAMP
Bradykinin B1	G_q/11	AEQ	Opioid OP1	G_i/o	GTPγS
Cannabinoid CB₁	G_i/o	cAMP	Opioid OP2	G_i/o	GTPγS
Cannabinoid CB₂	G_i/o	cAMP	Opioid OP3	G_i/o	GTPγS
Cholecystokinin CCK₁	G_q/11,G_s	AEQ	Somatostatin sst₄	G_i	GTPγS
Cholecystokinin CCK₂	G_q	AEQ	Urotensin-II	G_q/11	AEQ
Calcitonin CGRP	G_q/11,G_s	AEQ	Vasopressin V_1a	G_q/11	AEQ
Chemokine CXCR1	G_i/o	GTPγS	Vasopressin V_1b	G_q/11	AEQ
			VPAC1	G_s	AEQ

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-HT_1A	G_i/o	GTPγS	Muscarinic M₁	G_q/11	AEQ
Serotonin 5-HT_2A	G_q/11	AEQ	Muscarinic M₂	G_i/o	GTPγS
Serotonin 5-HT_2Ce	G_q/11	AEQ	Muscarinic M₃	G_q/11	AEQ
Adenosine A₁	G_i/o	cAMP	Muscarinic M₄	G_i/o	GTPγS
Adrenergic alpha_1B	G_q/11	AEQ	Muscarinic M₅	G_q/11	AEQ
Adrenergic alpha_2A	G_i/o	cAMP	Nociceptin OFQ (NOP)	G_i/o	GTPγS
Bombesin B₂	G_q/11	AEQ	Neurokinin NK₁	G_q/11	AEQ
Cannabinoid CB₁	G_i/o	cAMP	Neurokinin NK₂	G_q/11	AEQ
Cholecystokinin CCK₂	G_q	AEQ	Neuropeptide NPY₂	G_q/11,G_i/o	AEQ
Corticotropin CRF1	G_s	cAMP	Neurotensin NT₁	G_q/11	AEQ
Corticotropin CRF2b	G_s	cAMP	Opioid OP1	G_i/o	GTPγS
Dopamine D₁	G_olf,G_s	cAMP	Opioid OP2	G_i/o	GTPγS
Dopamine D_2L	G_i/o	cAMP	Opioid OP3	G_i/o	GTPγS
Galanin GAL₂	G_q/11,G_i/o	AEQ	Orexin OX₁	G_q/11	AEQ
Histamine H₁	G_q/11	AEQ	Orexin OX₂	G_q/11	AEQ
Histamine H₃	G_i/o	GTPγS	Somatostatin sst2	G_i	GTPγS
MCH₁	G_q/11,G_i/o	AEQ	Vasopressin V_1b	G_q/11	AEQ
mGluR₂	G_i/o	cAMP	PAC1	G_s	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-HT_2Ce	G_q/11	AEQ	Histamine H₁	G_q/11	AEQ
Adenosine A₁	G_i/o	cAMP	Histamine H₃	G_i/o	GTPγS
Adenosine A_2B	G_s	cAMP	MCH1	G_q/11,G_i/o	AEQ
Adrenergic beta₃	G_s	cAMP	MC4	G_s	cAMP
Adrenergic alpha_1B	G_q/11	AEQ	MC5	G_s	cAMP
Adrenergic alpha_2A	G_i/o	cAMP	Muscarinic M₁	G_q/11	AEQ
Angiotensin AT₁	G_q/11	AEQ	Muscarinic M₂	G_i/o	GTPγS
Bombesin BB1	G_q/11	AEQ	Muscarinic M₃	G_q/11	AEQ
Bombesin BB2	G_q/11	AEQ	NMUR1	G_q/11	AEQ
Bombesin BB3	G_q/11	AEQ	Neuropeptide NPY₂	G_q/11,G_i/o	AEQ
Bradykinin B2	G_q/11	AEQ	Neurotensin NT1	G_q/11	AEQ
Calcitonin CGRP	G_q/11,G_s	AEQ	Niacin receptor	G_i/o	cAMP
Calcium CaS	G_q/11,G_i/o	AEQ	Nociceptin OFQ (NOP)	G_i/o	GTPγS
Cannabinoid CB₁	G_i/o	GTPγS	Opioid OP2	G_i/o	GTPγS
Cannabinoid CB₂	G_i/o	GTPγS	Opioid OP3	G_i/o	GTPγS
Chemokine CCR2b	G_i/o	GTPγS	Orexin OX1	G_q/11	AEQ
Chemokine CCR4	G_i/o	GTPγS	Orexin OX2	G_q/11	AEQ
Chemokine CXCR3	G_i/o	GTPγS	Oxytocin OT1	G_q/11	AEQ
Cholecystokinin CCK₁	G_q/11,G_s	AEQ	Prokineticin PKR2	G_q/11	AEQ
Corticotropin CRF2b	G_s	cAMP	Prostanoid EP2	G_s	cAMP
FFA1 /GPR40	G_q/11	AEQ	PTH₁	G_s	cAMP
FFA2 / GPR43	G_i/o, G_q/11	cAMP	Secretin	G_s	cAMP
Galanin GAL2	G_q/11,G_i/o	AEQ	Somatostatin sst₂	G_i	GTPγS
GIP	G_s	cAMP	Urotensin-II	G_q/11	AEQ
GLP-1	G_s	cAMP	Vasopressin V_1a	G_q/11	AEQ
Glucagon	G_s	cAMP	PAC1	G_s	AEQ
GPR7	G_i/o	GTPγS	VPAC2	G_s	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-HT_2A	G_q/11	AEQ	GPR109a	G_i/o	AEQ
Adenosine A₁	G_i/o	cAMP	Leukotrien BLT₁	G_i/o,G_q/11	AEQ
Adenosine A_2A	G_s	cAMP	Leukotrien CysLT₁	G_q/11	AEQ
Adenosine A₃	G_i/o	cAMP	Leukotrien CysLT₂	G_q/11	AEQ
Complement C3a	G_i/o	GTPgS	Muscarinic M₂	G_i/o	GTPgS
Complement C5a	G_i/o	GTPgS	Muscarinic M₄	G_i/o	GTPgS
Bombesin BB₁	G_q/11	AEQ	Neurokinin NK₁	G_q/11	AEQ
Bombesin BB₂	G_q/11	AEQ	Neuromedin U NMU-1R	G_q/11	AEQ
Bradykinin B₂	G_q/11	AEQ	Neurotensin NTS₁	G_q/11	AEQ
Calcitonin CGRP	G_q/11,G_s	AEQ	Opioid OP₁	G_i/o	GTPgS
Cannabinoid CB₂	G_i/o	cAMP	Opioid OP₂	G_i/o	GTPgS
Chemokine CCR₁	G_i/o	GTPgS	Opioid OP₃	G_i/o	GTPgS
Chemokine CCR_2b	G_i/o	AEQ	Platelet Activating Factor PAF	G_q/11,G_s	cAMP
Chemokine CCR₃	G_i/o	AEQ	Prokineticin PKR₁	G_q/11	AEQ
Chemokine CCR₄	G_i/o	AEQ	Prostanoid DP	G_s	cAMP
Chemokine CCR₅	G_i/o	AEQ	Prostanoid EP₁	G_q/11	AEQ
Chemokine CCR₆	G_i/o	AEQ	Prostanoid EP₃	G_i/o	AEQ
Chemokine CCR₇	G_i/o	AEQ	Prostanoid EP₄	G_s	cAMP
Chemokine CCR₈	G_i/o	AEQ	Prostanoid IP₁	G_s	cAMP
Chemokine CCR_9a	G_i/o	AEQ	Protease-activated PAR₂	G_i/o,G_q/11	AEQ
Chemokine CCR₁₀	G_i/o	AEQ	Protease-activated PAR₄	G_i/o,G_q/11	AEQ
Chemokine CXCR₂	G_i/o	AEQ	Sphingosine S₁P₁	G_i/o	AEQ
Chemokine CXCR_3a	G_i/o	AEQ	Sphingosine S₁P₂	G_q	AEQ
Chemokine CXCR₄	G_i/o	AEQ	Sphingosine S₁P₄	G_q/11,G_s	AEQ
Chemokine XCR₁	G_i/o	AEQ	Sphingosine S₁P₅	G_i/o	AEQ
Free Fatty Acid GPR43	G_i/o,G_q/11	cAMP	PAC₁	G_s	AEQ
Histamine H₁	G_q/11	AEQ	VPAC₁	G_s	AEQ
Histamine H₂	G_s	cAMP	VPAC₂	G_s	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-HT_1A	G_i/o	GTPγS	Muscarinic M₁	G_q/11	AEQ
Serotonin 5-HT_2Ce	G_q/11	AEQ	Muscarinic M₂	G_i/o	GTPγS
Adenosine A₁	G_i/o	cAMP	Muscarinic M₃	G_q/11	AEQ
Adenosine A₃	G_i/o	cAMP	Muscarinic M₅	G_q/11	AEQ
Adrenergic beta₂	G_s	cAMP	Nociceptin OFQ (NOP)	G_i/o	GTPγS
Adrenergic alpha_2A	G_i/o	cAMP	Neurokinin NK₁	G_q/11	AEQ
Bradykinin B2	G_q/11	AEQ	Neurokinin NK₂	G_q/11	AEQ
Cannabinoid CB₁	G_i/o	cAMP	NeuromedinNMU2	G_q/11	AEQ
Cannabinoid CB₂	G_i/o	cAMP	Neuropeptide GPR7	G_i/o	GTPγS
Chemokine CCR2b	G_i/o	GTPγS	Neurotensin NTS1	G_q/11	AEQ
Chemokine CX3CR1	G_i/o	GTPγS	Opioid OP1	G_i/o	GTPγS
Cholecystokinin CCK₂	G_q/11	AEQ	Opioid OP2	G_i/o	GTPγS
Calcitonin CGRP	G_q/11,G_s	AEQ	Opioid OP3	G_i/o	GTPγS
Galanin GAL1	G_i/o	GTPγS	Orexin OX1	G_q/11	AEQ
GABAB1a/B2	G_i/o	cAMP	Parathyroid Hormone PTH1	G_q/11,G_s	cAMP
Glutamate mGlu2	G_i/o	cAMP	Platelet-Activating PAF	G_q/11,G_s	cAMP
Histamine H₁	G_q/11	AEQ	Prokineticin PKR1	G_q/11	AEQ
Histamine H₃	G_i/o	GTPγS	Protease Activated PAR2	G_q/11,G_i	GTPγS
MAS related MrgX2	G_q/11	AEQ	TRPA1	Calcium channel	AEQ
5-HT3	Calcium channel	AEQ	TRPV1	Calcium channel	IPOne
NMDA GRIN-1	none	RLB

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	G_q	AEQ
mGluR2	G_i/o	cAMP
mGluR3	G_i/o	AEQ
mGluR4	G_i/o	GTPγS
mGluR5	G_q	AEQ
mGluR6	G_i/o	GTPγS
mGluR7	G_i/o	cAMP
mGluR8	G_i/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	G_q/11	AEQ
M2	G_i/o	GTPγS
M3	G_q/11	AEQ
M4	G_i/o	GTPγS
M5	G_q/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-HT_1A	G_i/o	GTPγS	Serotonin 5-HT_2Ce	G_q/11	AEQ
Serotonin 5-HT_1B	G_i/o	GTPγS	Serotonin 5-HT_2Cne	G_q/11	AEQ
Serotonin 5-HT_1D	G_i/o	GTPγS	Serotonin 5-HT₃	Ion channel	AEQ
Serotonin 5-HT_1E	G_i/o	GTPγS	Serotonin 5-HT_4e	G_s	cAMP
Serotonin 5-HT_1F	G_i/o	GTPγS	Serotonin 5-HT₅	G_i/o	AEQ
Serotonin 5-HT_2A	G_q/11	AEQ	Serotonin 5-HT₆	G_s	cAMP
Serotonin 5-HT_2B	G_q/11	AEQ	Serotonin 5-HT₇	G_s	cAMP

Chemokine receptors panel

Profile your compounds against the 21 human chemokine receptors.

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

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Off-the-shelf profiling panels