orphanMAX^℠ GPCR Assay Panel

LeadHunter Discovery Services provides the largest collection of functional cell-based assays for liganded and non-liganded Orphan GPCR (oGPCR) receptors. The panel includes a collection of 73 human oGPCRs that utilize the proven PathHunter^® Arrestin recruitment technology. With a single, G-protein independent readout the panel provides a robust, high quality screening platform that is capable of uncovering novel ligand and receptor pairings and is the ideal solution for any ligand fishing or deorphanization campaign.

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orphanMAX Assay Panel

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

Family ▲	Target Gene	Common Name	Arrestin
Chemokine	CCRL2	CCRL2	X
Chemokine	DARC	FY	X
Class A Orphan	GHSR1b	GHSR1b	X
Class A Orphan	GPR101	GPR101	X
Class A Orphan	GPR12	GPR12	X
Class A Orphan	GPR132	GPR132	X
Class A Orphan	GPR135	GPR135	X
Class A Orphan	GPR139	GPR139	X
Class A Orphan	GPR141	GPR141	X
Class A Orphan	GPR142	GPR142	X
Class A Orphan	GPR146	GPR146	X
Class A Orphan	GPR148	GPR148	X
Class A Orphan	GPR149	GPR149	X
Class A Orphan	GPR15	GPR15	X
Class A Orphan	GPR150	GPR150	X
Class A Orphan	GPR151	GPR151	X
Class A Orphan	GPR152	GPR152	X
Class A Orphan	GPR161	GPR161	X
Class A Orphan	GPR162	GPR162	X
Class A Orphan	GPR17	GPR17	X
Class A Orphan	GPR171	GPR171	X
Class A Orphan	GPR173	GPR173	X
Class A Orphan	GPR176	GPR176	X
Class A Orphan	GPR18	GPR18	X
Class A Orphan	GPR182	GPR182	X
Class A Orphan	GPR20	GPR20	X
Class A Orphan	GPR23	LPA4	X
Class A Orphan	GPR25	GPR25	X
Class A Orphan	GPR26	GPR26	X
Class A Orphan	GPR27	GPR27	X
Class A Orphan	GPR3	GPR3	X
Class A Orphan	GPR31	GPR31	X
Class A Orphan	GPR32	GPR32	X
Class A Orphan	GPR37	EDNRBL	X
Class A Orphan	GPR37L1	GPR37L1	X
Class A Orphan	GPR39	GPR39	X
Class A Orphan	GPR4	GPR4	X
Class A Orphan	GPR45	GPR45	X
Class A Orphan	GPR50	GPR50	X
Class A Orphan	GPR52	GPR52	X
Class A Orphan	GPR55	GPR55	X
Class A Orphan	GPR6	GPR6	X
Class A Orphan	GPR61	GPR61	X
Class A Orphan	GPR65	GPR65	X
Class A Orphan	GPR75	GPR75	X
Class A Orphan	GPR78	GPR78	X
Class A Orphan	GPR79	GPR79	X
Class A Orphan	GPR83	GPR83	X
Class A Orphan	GPR84	GPR84	X
Class A Orphan	GPR85	GPR85	X
Class A Orphan	GPR88	GPR88	X
Class A Orphan	LGR4	LGR4	X
Class A Orphan	LGR5	LGR5	X
Class A Orphan	LGR6	LGR6	X
Class A Orphan	MRGPRD	MRGPRD	X
Class A Orphan	MRGPRE	MRGPRE	X
Class A Orphan	MRGPRF	MRGPRF	X
Class A Orphan	MRGPRX4	MRGPRX4	X
Class A Orphan	OPN5	OPN5	X
Class A Orphan	OXGR1	OXGR1	X
Class A Orphan	P2RY8	P2RY8	X
Class A Orphan	TAAR5	TAAR5	X
Class A Orphan	GPR22	GPR22	X
Class B Orphan	BAI1	BAI1	X
Class B Orphan	BAI2	BAI2	X
Class B Orphan	BAI3	BAI3	X
Class B Orphan	GPR123	GPR123	X
Class B Orphan	GPR157	GPR157	X
Class B Orphan	GPR97	GPR97	X
Estrogen (G protein coupled) receptor	GPR30	GPER	X
Other 7TM proteins	GPR107	GPR107	X
Other 7TM proteins	GPR137	TM7SF1	X
Other 7TM proteins	GPR143	GPR143	X

Performance

Arrestin orphan panel successfully used to de-orphanize many GPCRs
12 targets uniquely identified or verified using the arrestin platform
Customer validated - 11 novel target interactions identified using orphan GPCR panel
27% of targets have produced hits

Robust Platform for Novel Ligand Discovery

Expression and glycosylation status of the PathHunter Arrestin GPR32 cell lines was confirmed by Eastern blot (Left Panel, lane 3). Basal ‘constitutive’ receptor activity following receptor expression compared with host cell line (Middle Panel). Analysis of receptor expression by flow cytometry was confirmed using Pro-Link MAb (Right panel).

Dose response curve for Zaprinast, a surrogate ligand for GPR35 shows a robust response to agonist (Left panel). Overlap of ranked average CV per assay vs mean RLU for 83 primary Orphan GPCR screens. <12.5% CV was obtained for 78 of 83 completed (Right panel).

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 and Benefits

Comprehensive menu of 73 functional cell-based assays for orphan GPCRs
Arrestin recruitment readout for novel ligand identification & receptor de-orphanization
Single assay readout facilitates reliable data comparison across all targets regardless of coupling status
Regularly scheduled panel dates
Run in agonist mode

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

orphanMAX℠ GPCR Assay Panel