gpcrMAX^℠ GPCR Assay Panel

The largest commercial panel of functional cell-based assays available, gpcrMAX contains a set of 168 GPCRs covering over 60 distinct receptor families including Adrenergic, Dopamine, P2Y, Serotonin and many others. Powered by the PathHunter^® technology, this panel utilizes Arrestin recruitment to rapidly, reliably and reproducibly profile compounds using a common G-protein independent readout.

With the largest menu of functional GPCR assays and regularly scheduled test dates, gpcrMAX is an ideal choice for all stages of drug discovery and development, from lead discovery & hit identification to lead optimization, preclinical and compound safety.

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gpcrMAX Assay Panel

Listed below are the assays currently available for screening and profiling.

Family ▲	Target Gene	Common Name	Arrestin
5-Hydroxytryptamine	HTR1A	5HT1A	X
5-Hydroxytryptamine	HTR1B	5HT1B	X
5-Hydroxytryptamine	HTR1F	5HT1F	X
5-Hydroxytryptamine	HTR2A	5HT2A	X
5-Hydroxytryptamine	HTR2C	5HT2C	X
5-Hydroxytryptamine	HTR5A	5HT5A	X
5-Hydroxytryptamine	HTR1E	5HT1E	X
Acetylcholine	CHRM1	M1	X
Acetylcholine	CHRM5	M5	X
Acetylcholine	CHRM2	M2	X
Acetylcholine	CHRM3	M3	X
Acetylcholine	CHRM4	M4	X
Adenosine	ADORA3	A3	X
Adrenoceptors	ADRA2A	α2A-adrenoceptor	X
Adrenoceptors	ADRA2C	α2C-adrenoceptor	X
Adrenoceptors	ADRB1	β1-adrenoreceptor	X
Adrenoceptors	ADRB2	β2-adrenoreceptor	X
Adrenoceptors	ADRA1B	α1B-adrenoceptor	X
Adrenoceptors	ADRA2B	α2B-adrenoceptor	X
Angiotensin	AGTR1	AT1	X
Apelin	AGTRL1	APJ	X
Bombesin	BRS3	BB3	X
Bombesin	GRPR	BB2	X
Bombesin	NMBR	BB1	X
Bradykinin	BDKRB1	B1	X
Bradykinin	BDKRB2	B2	X
Calcitonin	CALCR	CT	X
Calcitonin	CALCRL-RAMP1	Calcitonin receptor-like receptor	X
Calcitonin	CALCRL-RAMP2	Calcitonin receptor-like receptor	X
Calcitonin	CALCRL-RAMP3	Calcitonin receptor-like receptor	X
Calcitonin	CALCR-RAMP2	CT	X
Calcitonin	CALCR-RAMP3	CT	X
Cannabinoid	CNR1	CB1	X
Cannabinoid	CNR2	CB2	X
Chemerin	CMKLR1	CMKLR1	X
Chemokine	CCR1	CCR1	X
Chemokine	CCR10	CCR10	X
Chemokine	CCR2	CCR2	X
Chemokine	CCR3	CCR3	X
Chemokine	CCR7	CCR7	X
Chemokine	CCR8	CCR8	X
Chemokine	CCR9	CCR9	X
Chemokine	CCR4	CCR4	X
Chemokine	CCR5	CCR5	X
Chemokine	CCR6	CCR6	X
Chemokine	CX3CR1	CX3CR1	X
Chemokine	CXCR1	CXCR1	X
Chemokine	CXCR5	CXCR5	X
Chemokine	CXCR2	CXCR2	X
Chemokine	CXCR3	CXCR3	X
Chemokine	CXCR4	CXCR4	X
Chemokine	CXCR7	CXCR7	X
Cholecystokinin	CCKAR	CCK1	X
Cholecystokinin	CCKBR	CCK2	X
Class A Orphan	EBI2	GPR183	X
Class A Orphan	GPR1	GPR1	X
Class A Orphan	GPR119	GPR119	X
Class A Orphan	GPR35	GPR35	X
Class A Orphan	MRGPRX1	MRGPRX1	X
Class A Orphan	MRGPRX2	MRGX2	X
Complement peptide	C5L2	C5L2	X
Complement peptide	C5AR1	C5A	X
Corticotropin-releasing factor	CRHR1	CRF1	X
Corticotropin-releasing factor	CRHR2	CRF2	X
Dopamine	DRD3	D3	X
Dopamine	DRD4	D4	X
Dopamine	DRD5	D5	X
Dopamine	DRD1	D1	X
Dopamine	DRD2L	D2L	X
Dopamine	DRD2S	D2S	X
Endothelin	EDNRA	ETA	X
Endothelin	EDNRB	ETB	X
Formylpeptide	FPR1	FPR1	X
Formylpeptide	FPRL1	FPR2/ALX	X
Free Fatty Acid	FFAR1	FFA1	X
Free fatty acid	GPR120	FFA4	X
Galanin	GALR1	GALR1	X
Galanin	GALR2	GALR2	X
Ghrelin	GHSR	ghrelin	X
Glucagon	GCGR	glucagon	X
Glucagon	GIPR	GIP	X
Glucagon	GLP1R	GLP-1	X
Glucagon	GLP2R	GLP-2	X
Glucagon	SCTR	secretin	X
Glycoprotein hormone receptor	FSHR	FSHR	X
Glycoprotein hormone receptor	LHCGR	LH	X
Glycoprotein hormone receptor	TSHR(L)	TSH	X
Histamine	HRH1	H1	X
Histamine	HRH2	H2	X
Histamine	HRH3	H3	X
Histamine	HRH4	H4	X
Hydroxycarboxylic acid	GPR109A	HCA2	X
Hydroxycarboxylic acid	GPR109B	HCA3	X
Kisspeptin receptor	KISS1R	kisspeptin	X
Leukotriene	LTB4R	BLT1	X
Leukotriene	OXER1	OXE	X
Lysophospholipid (LPA)	EDG7	LPA3	X
Lysophospholipid (LPA)	EDG4	LPA2	X
Lysophospholipid (LPA)	GPR92	GPR92	X
Lysophospholipid (S1P)	EDG1	S1P1	X
Lysophospholipid (S1P)	EDG3	S1P3	X
Lysophospholipid (S1P)	EDG6	S1P4	X
Lysophospholipid (S1P)	EDG5	S1P2	X
Melanin-concentrating hormone	MCHR1	MCH1	X
Melanin-concentrating hormone	MCHR2	MCH2	X
Melanocortin	MC1R	MC1	X
Melanocortin	MC3R	MC3	X
Melanocortin	MC4R	MC4	X
Melanocortin	MC5R	MC5	X
Melatonin	MTNR1A	MT1	X
Motilin	MLNR	motilin	X
Neuromedin U	NMU1R	NMU1	X
Neuropeptide B & W	NPBWR1	NPBW1	X
Neuropeptide B & W	NPBWR2	NPBW2	X
Neuropeptide FF & AF	NPFFR1	NPFF1	X
Neuropeptide S	NPSR1b	NPS receptor	X
Neuropeptide Y	NPY1R	Y1	X
Neuropeptide Y	NPY2R	Y2	X
Neuropeptide Y	PPYR1	Y4	X
Neurotensin	NTSR1	NTS1	X
Opioid	OPRM1	μ	X
Opioid	OPRD1	δ	X
Opioid	OPRK1	κ	X
Opioid	OPRL1	NOP	X
Orexin	HCRTR2	OX2	X
Orexin	HCRTR1	OX1	X
P2Y	P2RY1	P2RY1	X
P2Y	P2RY11	P2Y11	X
P2Y	P2RY12	P2Y12	X
P2Y	P2RY2	P2Y2	X
P2Y	P2RY4	P2Y4	X
P2Y	P2RY6	P2Y6	X
Parathyroid hormone	PTHR1	PTH1	X
Parathyroid hormone	PTHR2	PTH2	X
Peptide P518	GPR103	QRFPR	X
Platelet-activating factor	PTAFR	PAF	X
Prokineticin	PROKR1	PKR1	X
Prokineticin	PROKR2	PKR2	X
Prolactin releasing peptide receptor	PRLHR	PRRP	X
Prostanoid	CRTH2	PTGDR2	X
Prostanoid	PTGER2	EP2	X
Prostanoid	PTGER3	EP3	X
Prostanoid	PTGER4	EP4	X
Prostanoid	PTGFR	FP	X
Prostanoid	PTGIR	IP1	X
Prostanoid	TBXA2R	TP	X
Protease activated	F2R	PAR1	X
Protease activated	F2RL1	PAR2	X
Protease activated	F2RL3	PAR4	X
Relaxin	RXFP3	RXFP3	X
Somatostatin	SSTR3	SST3	X
Somatostatin	SSTR5	SST5	X
Somatostatin	SSTR1	SST1	X
Somatostatin	SSTR2	SST2	X
Tachykinin	TACR1	NK1	X
Tachykinin	TACR2	NK2	X
Tachykinin	TACR3	NK3	X
Thyrotropin releasing hormone	TRHR	TRH1	X
Urotensin	UTR2	UT	X
Vasopressin and Oxytocin	AVPR2	V2	X
Vasopressin and Oxytocin	AVPR1A	V1A	X
Vasopressin and Oxytocin	AVPR1B	V1B	X
Vasopressin and Oxytocin	OXTR	OT	X
VIP and PACAP	ADCYAP1R1	PAC1	X
VIP and PACAP	VIPR1	VPAC1	X
VIP and PACAP	VIPR2	VPAC2	X

Assay Performance

Our gpcrMAX panel can identify a specific ligand interaction with a receptor. Once identified, each hit can be confirmed using one of our alternate functional readouts.

Identification and Confirmation of Novel Hits

Full GPCR panel profiling was performed at a single ligand concentration (Left panel), resulting in the identification of a potent interaction. Follow-up IC50s were determined using PathHunter Arrestin and HitHunter cAMP assays to confirm ligand potency for the target, which revealed a novel ligand (Right panels).

Data Analysis & Interpretation

Definitions

Percent Activity/Inhibition

The results for single concentration (primary screen) for tested compound(s) are reported in your study report and spreadsheets as '% Activity' or '% Inhibition' and are calculated in the following manner:

% Activity
(Agonist Mode) =
100% x

[

Mean RLU _{(test sample)}- Mean RLU_{(vehicle control)}

Mean MAX RLU _{(control ligand)}- Mean RLU _{(vehicle control)}

]

test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)

% Inhibition
(Antagonist mode) =
100% x

[

Mean RLU _{(test sample)}- Mean RLU_{(vehicle control)}

Mean MAX RLU _{(control ligand)}- Mean RLU _{(vehicle control)}

]

test sample = client supplied compound
vehicle control = DMSO (0% activity)
EC₈₀ control = control compound (80% activity)

Dose Response Curve (EC₅₀/IC₅₀)

The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as EC₅₀/IC₅₀, which are values derived using the Hill equation:

Panel Features & Benefits

Comprehensive panel of functional cell-based assays for 168 known GPCRs
Single, G-protein independent readout for reliable data comparison across all receptors
Run in agonist and antagonist modes
Regularly scheduled panel dates
Broad applications including target identification, specificity and selectivity
Additional confirmation services available – Arrestin, cAMP, Calcium or Internalization readouts

How it Works

To ensure your compounds are included in the Test Date of your choosing, submit your compounds and PO by the date indicated in the "Compounds & PO Due" column below.

2020 gpcrMAX and orphanMAX Panel Run Schedule

Panel	Test Dates	Compounds & PO Due	Report & Invoicing
gpcrMAX, orphanMAX	January 28	January 24	February 25
	March 10	March 6	April 7
	April 21	April 17	May 19
	June 2	May 29	June 30
	July 14	July 10	August 11
	August 25	August 21	September 22
	October 6	October 2	November 3
	November 17	November 13	December 22

2020 nhrMAX Panel Run Schedule

Panel	Test Dates	Compounds & PO Due	Report & Invoicing
nhrMAX	February 11	February 7	March 10
	March 24	March 20	April 21
	May 5	May 1	June 2
	June 16	June 12	July 14
	July 28	July 24	August 25
	September 8	September 4	October 6
	October 20	October 16	November 17

gpcrMAX℠ GPCR Assay Panel