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WuXi Biology GPCR Cell Lines and Assays

Family Receptor

(Human)

G Protein

Coupling Host Cell Line Assay Format

Adenosine

A1/ADORA1A Gi/Gq HEK293/Gα15 Calcium/Binding

A2A/ADORA2A Gs CHO/Gα15 Calcium/Binding

A2B/ADORA2B Gs HEK293/Gα15 Calcium/Binding

A3/ADORA3A Gi CHO/Gα15 Calcium/Binding

Adrenergic

alpha1A/ADRA1A Gq HEK293 Calcium/Binding

alpha2A/ADRA2A Gi HEK293/Gα15 Calcium/Binding

alpha2C/ADRA2C Gi HEK293/Gα15 Calcium

beta1/ADRA1B Gs HEK293/Gα15 Calcium/Binding


beta3/ADRA3B Gs HEK293/Gα15 Calcium

Anaphylotoxin C3aR/C3AR1 Gi HEK293/Gα15 Calcium

Angiotensin

AT1/AGTR1 Gq CHO Calcium

AT2/AGTR2 Gq CHO Calcium

Bombesin BB2/GRPR Gq HEK293 Calcium/Binding

Bradykinin

B1/BDKRB1 Gi/Gq HEK293 Calcium

B2/BDKRB2 Gi/Gq HEK293/Gα15 Calcium

Cannabinoid

CB1/CNR1 Gi HEK293/Gα15 Calcium/Binding

CB2/CNR2 Gi CHO/Gα15 Calcium/Binding

Chemokine

CCR1 Gi HEK293/Gα15 Calcium




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CXCR1 Gi HEK293/Gα15 Calcium



Cholecystokinin

CCKA/CCKAR Gq HEK293 Calcium/Binding

CCKb/CCKBR Gq HEK293 Calcium

Class A Orphans MrgX2 Gi/Gq HEK293/Gα15 Calcium

Corticotropin

Releasing Factor

CRF1/CRHR1 Gs HEK293/Gα15 Calcium

CRF2a/CRHR2 Gs HEK293/Gα15 Calcium

Dopamine

D1/DRD1 Gs HEK293/Gα15 Calcium/Binding

D2/DRD2 Gi HEK293/Gα15 Calcium/Binding

Endothelin

ETA/EDNRA Gq HEK293 Calcium/Binding

ETB/EDNRB Gq/Gs/Gi HEK293/Gα15 Calcium

Formylpeptide FPR1 Gi HEK293/Gα15 Calcium

Galanin GALR1 Gi HEK293/Gα15 Calcium

Gastric GIPR Gs CHO cAMP

Ghrelin GHSR Gq CHO Calcium

Glucagon

GCGR Gs HEK293/Gα15 Calcium/cAMP/Bi

nding

GLP1/GLP1R Gs HEK293/Gα15 Calcium/cAMP/Bi

nding

Gonadotropin-

releasing hormone GNRHR Gq HEK293 Calcium

Histamine

H1/HRH1 Gq HEK293 Calcium/Binding

H2/HRH2 Gs/Gq HEK293 Calcium/Binding

H3/HRH3 Gi HEK293/Gα15 Calcium






5-

Hydroxytryptamine

5-HT1A/HTR1A Gi HEK293/Gα15 Calcium/Binding

5-HT2A/HTR2A Gq HEK293 Calcium/Binding

5-HT1B/HTR1B Gi CHO/Gα15 cAMP/Binding

5-HT2B/HTR2B Gq CHO-K1 Binding

5-HT7/HTR7 Gs HEK293/Gα15 Calcium/Binding

Leukotriene

CYSLTR2 Gq HEK293 Calcium

LTB4R1 Gq CHO Calcium

Lysophospholipid

S1P1 Gi CHO/Gα15 Calcium

S1P2 Gs/Gq CHO/Gα15 Calcium

S1P5 Gi CHO/Gα15 Calcium

Melanocortin

MC3R Gi HEK293/Gα15 Calcium

MC4R Gi HEK293/Gα15 Calcium

Metabotropic

Glutamate

mGluR2 Gi CHO/Gα15 Calcium

mGluR3 Gi HEK293/Gα15 Calcium



Motilin MLNR Gq HEK293 Calcium

Motilin-Canis MLNR Gq HEK293 Calcium

Muscarinic

M1/CHRM1 Gq/Gs/Gi HEK293 Calcium/Binding

M2/CHRM2 Gi HEK293/Gα15 Calcium/Binding

M3/CHRM3 Gq HEK293 Calcium/Binding

M4/CHRM4 Gi HEK293/Gα15 Binding

M5/CHRM5 Gq CHO Calcium/Binding

Neuromedin U NMUR1 Gq HEK293 Calcium

Neuropeptide Y Y1/NPY1R Gi CHO/Gα15 Calcium






Y2/NPY2R Gi HEK293/Gα15 Calcium

Neurotensin

NT1/NTSR1 Gq HEK293 Calcium

NT1/NTSR1 Gq HEK293 Calcium

Opioid

delta/OPRD1 Gi HEK293/Gα15 Calcium/Binding

kappa/OPRK1 Gi HEK293/Gα15 Calcium/Binding

mu/OPRM1 Gi HEK293/Gα15 Calcium/Binding

Orexin

OX1/HCRTR1 Gq/Gs/Gi HEK293/Gα15 Calcium

OX2/HCRTR2 Gs HEK293/Gα15 Calcium

Platelet-activating

factor PAF/PTAFR Gq HEK293 Calcium

Prokineticin

PK1/PROKR1 Gq HEK293 Calcium

PK2/PROKR2 Gi HEK293/Gα15 Calcium

Prostaglandin

EP1/PTGER1 Gq HEK293 Calcium

EP2/PTGER2 Gs CHO/Gα15 Calcium

EP4/PTGER4 Gs HEK293/Gα15 Calcium

Prostanoid

FP/PTGFR Gq HEK293 Calcium

PTGIR/IP1 Gs HEK293/Gα15 Calcium

TP/TBXA2R Gq HEK293 Calcium

Somatostatin SST5 Gi HEK293/Gα15 Calcium

Tachykinin

NK1/TACR1 Gq HEK293 Calcium

NK2/TACR2 Gq/Gs HEK293 Calcium

NK3/TACR3 Gq HEK293 Calcium

Thyrotropin-

releasing hormone TRH1/TRHR Gq HEK293 Calcium

Vasopressin/

Oxytocin

OT/OXTR Gq HEK293 Calcium

V1B/AVPR1B Gq HEK293 Calcium

V1A/AVPR1A Gq CHO Calcium/Binding






V2/AVPR2 Gs HEK293/Gα15 Calcium

VIP and PACAP

VPAC1/VIPR1 Gs HEK293/Gα15 Calcium

VPAC2/VIPR2 Gs HEK293/Gα15 Calcium

PAC1/ADCYAP1

R1 Gs HEK293/Gα15 Calcium

Version: 201802






GPCR Assay Product Sheet (24 targets)

GPCRs listed in the table below are applicable for compound/sample screening as well as for

safety/off-target pharmacological profiling. Assay information sheets are provided. More

information for other targets may be provided upon request.

Family Receptor

(Human)

G Protein

Coupling

Host Cell

Line Assay Format

Adenosine A2A/ADORA2A Gs CHO/Gα15 Calcium/Binding

Adrenergic

alpha1A/ADRA1A Gq HEK293 Calcium/Binding

alpha2A/ADRA2A Gi HEK293/Gα15 Calcium/Binding



Cannabinoid CB1/CNR1 Gi CHO/Gα15 Calcium/Binding

CB2/CNR2 Gi CHO/Gα15 Calcium/Binding

Cholecystokinin CCKA/CCKAR Gq HEK293 Calcium/Binding

Dopamine D1/DRD1 Gs HEK293/Gα15 Calcium/Binding

D2/DRD2 Gi HEK293/Gα15 Calcium/Binding

Endothelin ETA/EDNRA Gq HEK293 Calcium/Binding

Histamine H1/HRH1 Gq HEK293 Calcium/Binding

H2/HRH2 Gs/Gq HEK293 Calcium/Binding

5-

Hydroxytryptamine

5-HT1A/HTR1A Gi HEK293/Gα15 Calcium/Binding

5-HT2A/HTR2A Gq HEK293 Calcium/Binding

5-HT1B/HTR1B Gi CHO/Gα15 cAMP/Binding

5-HT2B/HTR2B Gq HEK293 Binding

Muscarinic

M1/CHRM1 Gq/Gs/Gi HEK293 Calcium/Binding

M2/CHRM2 Gi HEK293/Gα15 Calcium/Binding

M3/CHRM3 Gq HEK293 Calcium/Binding

Opioid

delta/OPRD1 Gi HEK293/Gα15 Calcium/Binding

kappa/OPRK1 Gi HEK293/Gα15 Calcium/Binding

mu/OPRM1 Gi HEK293/Gα15 Calcium/Binding

Vasopressin V1A/AVPR1A Gq CHO Calcium/Binding

Version: 201802






Cell Line Name: HEK293/A2A/Gα15

Species/Source: Human/Recombinant

Gene Synonyms: ADORA2A ; A2aR; ADORA2; RDC8

Accession Number: NM_000675

G coupling Gs

Cellular Background: HEK293


Gene Synonyms: ADORA2A ; A2aR; ADORA2; RDC8


Agonist NECA

Measurement: Intracellular Ca2+

Detection method: FLIPR Fluorimetry

Incubation 25℃

Agonist effect EC50: 5.4 nM

Antagonist CGS-15943



Incubation 25℃

Stimulant NECA: 40 nM

Antagonist effect IC50: 0.22 nM

Ligand [3H] CGS 21680

Ligand concentration 6 nM

Kd (nM) 47.5 nM

Non specific NECA (10 μM)

Incubation 120 min/RT

Detection method Scintillation counting

Reference: NECA (IC50:82.0 nM)

ADORA2A (Adenosine A2A Receptor)

Functional Assay-Calcium Flux Assay

ADORA2A (Adenosine A2A Receptor)

Radio ligand binding Assay

ADORA2A

-2 0 2 4 6-20

0

20

40

60

80

100

120NECA

CPA

Log [Compound] nMA

cti

vit

y (

%)

ADORA2A

-4 -2 0 2 4-20

0

20

40

60

80

100

120CGS-15943

ZM241385

Log [Compound] nM

Inh

ibit

ion

(%

)

ADORA2A

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125NECA

CPA

ZM241385

CGS15943

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: HEK293/Alpha1A


Gene Synonyms: ADRA1A; ADRA1C; ADRA1L1; ALPHA1AAR

Accession Number: NM_000680 (isoform 1)

G coupling Gq

Antagonist 5-Methylurapidil

Agonist (-)Epinephrine



Incubation 25℃




Incubation 25℃

Stimulant (-)Epinephrine : 6.3 nM


Ligand [3H]prazosin

Ligand concentration 0.2 nM

Kd (nM) 0.09 nM

Non specific epinephrine (0.1 mM)



Reference: WB 4101 (IC50:0.28

nM)

Alpha1A (Alpha-1-adrenergic receptor)



Alpha1A

-2 0 2 4 6

0

20

40

60

80

100

1205-Methylurapidil

Prazosin

WB-4104

BMY7378

Log [Compound] nM

Inh

ibit

ion

(%

)

Alpha1A

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125WB4101

Epinephrine

Prazosin

Log [Compound] nM

% I

nh

ibit

ion

Alpha1A

-2 -1 0 1 2 3 4

0

20

40

60

80

100

120(-)-Epinephrine (E4642)

A-61603

Log [Compound] nMA

cti

vit

y (

%)






Cell Line Name: HEK293/Alpha2A/Gα15


Gene Synonyms: ADRA2A; ADRA2; ADRAR; ZNF32; ADRA2R; ALPHA2AAR

Accession Number: NM_000681 (isoform 1)

G coupling Gi

Agonist UK14304



Incubation 25℃


Antagonist Yohimbine hydrochloride



Incubation 25℃

Stimulant UK14304 : 4.3 nM


Ligand [3H]RX 821002


Kd (nM) 0.46 nM

Non specific epinephrine (0.1 mM)



Reference: Rx81002(IC50:2.3 nM)

Alpha2A (Alpha-2-adrenergic receptor)


Alpha2A

-2 0 2-20

0

20

40

60

80

100

120UK 14304

Epinephrine (E4250)

Log [Compound] nM

Acti

vit

y (

%)

Alpha2A

-2 -1 0 1 2 3 4-25

0

25

50

75

100

125Yohimbin

RX 821002

Prazosin

Log [Compound] nM

Inh

ibit

ion

(%

)

Alpha2A

-2 -1 0 1 2 3 4 5

0

25

50

75

100

125Epinephrine

Prazosin

Yohimbin

RX821002

UK14304

Log [Compound] nM

% I

nh

ibit

ion







Cell Line Name: HEK293/Beta1/Gα15


Gene Synonyms: ADRB1; RHR; B1AR; ADRB1R; BETA1AR


G coupling Gs

Agonist (-)Epinephrine



Incubation 25℃


Antagonist Carvedilol



Incubation 25℃

Stimulant (-)-Epinephrine : 20 nM


Ligand [3H](-)CGP 12177


Kd (nM) 0.04 nM

Non specific propranolol (2 µM)



Reference: Atenolol (IC50:857 nM)

Beta1 (Beta-1 Adrenergic Receptor)



Beta1

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Atenolol

Salbutamol

Propranolol

ICI118551

Isoproternol

Log [Compound] nM

% I

nh

ibit

ion

Beta1

-2 -1 0 1 2 3 4 5-20

0

20

40

60

80

100

120(-)Epinephrine

Isoproterenol

Salbutamol hemisulfate

Log [Compound] nM

Acti

vit

y (

%)

Beta1

-2 -1 0 1 2 3 4-20

0

20

40

60

80

100

120Carvedilol

(± )-Propranolol hydrochloride

Atenolol

ICI 118 551 hydrochloride

Log [Compound] nM

Inh

ibit

ion

(%

)






Cell Line Name: HEK293/Beta2/Gα15


Gene Synonyms: ADRB2; BAR; B2AR; ADRBR; ADRB2R; BETA2AR


G coupling Gs/Gi

Agonist Adrenaline



Incubation 25℃


Antagonist Carvedilol



Incubation 25℃

Stimulant Adrenaline: 0.43 nM


Ligand [3H](-)CGP 12177


Kd (nM) 0.1 nM

Non specific propranolol (2 µM)



Reference: ICI118551(IC50:3.3 nM)

Beta2 (Beta-2 Adrenergic Receptor)



Beta2

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Atenolol

Salbutamol

Propranolol

ICI118551

Isoproternol

Log [Compound] nM

% I

nh

ibit

ion

Beta2

-4 -3 -2 -1 0 1 2 3 4-20

0

20

40

60

80

100

120

Adrenaline

Isoproterenol

Salbutamol hemisulfate

Log [Compound] nM

Acti

vit

y (

%)

Beta2

-2 -1 0 1 2 3-25

0

25

50

75

100

125

Carvedilol

(± )-Propranolol hydrochloride

ICI 118551

Log [Compound] nM

Inh

ibit

ion

(%

)






Cell Line Name: CHO/CB1/Gα15


Gene Synonyms: CNR1; CB1; CNR; CB-R; CB1A; CB1R; CANN6; CB1K5

Accession Number: NM_016083 (isoform1)

G coupling Gi

Cellular Background: CHO-K1


Gene Synonyms: CNR1; CB1; CNR; CB-R; CB1A; CB1R; CANN6; CB1K5

Accession Number: X54937

Agonist WIN55212-2



Incubation 25℃

Agonist effect EC50:352 nM

Antagonist Rimonabant hydrochloride



Incubation 25℃

Stimulant WIN55212-2: 4000 nM


Ligand [3H]CP 55940


Kd (nM) 3.7 nM

Non specific WIN 55212-2 (5 µM)

Incubation 120 min/37℃


Reference: CP 55940 (0.81 nM)

CB1 (Cannabinoid Type 1 Receptor)




CB1

-1 0 1 2 3 4 5 6-20

0

20

40

60

80

100

120 CP55940

WIN55212-2

Anandamide

Log [Compound] nMA

cti

vit

y (

%)

CB1

-1 0 1 2 3 4 5 6-20

0

20

40

60

80

100

120Rimonabant

AM281

AM630

log [Con.] nM

Inh

ibit

ion

(%

)

CB1

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125CP55940

WIN55212-2

Anandamide

AM281

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: CHO/CB2/Gα15


Gene Synonyms: CNR2; CB2; CX5; CB-2


G coupling Gi

Agonist CP55940



Incubation 25℃

Agonist effect EC50: 199 nM

Antagonist AM630



Incubation 25℃

Stimulant CP55940: 300 nM

Antagonist effect IC50: 563 nM

Ligand [3H]CP 55940


Kd (nM) 5.1 nM

Non specific WIN 55212-2 (5 µM)

Incubation 120 min/37℃


Reference: WIN55212-2(IC50:

2.2nM)




CB2

-1 0 1 2 3 4 5

0

20

40

60

80

100

120CP55940

WIN55215-2

Anandamide

Log [Compound] nMA

cti

vit

y (

%)

CB2

0 1 2 3 4 5-20

0

20

40

60

80

100

120AM630

Rimonbant

AM281

Log [Compound] nM

Inh

ibit

ion

(%

)

CB2

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125CP55940

WIN55212-2

Anandomide

AM630

AM281

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: HEK293/CCKA


Gene Synonyms: CCKAR; CCK-A; CCK1R; CCKRA; CCK1-R


G coupling Gq

Cellular Background: 1321-N1


Gene Synonyms: CCKAR; CCK-A; CCK1R; CCKRA; CCK1-R

Accession Number: L19315

Agonist CCK-4



Incubation 25℃


Antagonist Lorglumide



Incubation 25℃

Stimulant CCK-4: 557 nM


Ligand [3H]CCK-8s


Kd (nM) 0.22 nM

Non specific CCK-8s (1 μM)



Reference: CCK-8s(IC50: 2.4 nM)

CCKA (Cholecystokinin A Receptor)


CCKA (Cholecystokinin A Receptor)


CCKA

-4 -2 0 2 4

0

20

40

60

80

100

120CCK-4

CCK-8s

Log [Compound] nMA

cti

vit

y (

%)

CCKA

0 1 2 3 4 5-20

0

20

40

60

80

100

120Lorglumide

Devazepide

LY 225910

Log [Compound] nM

Inh

ibit

ion

(%

)

CCKA

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125

LY225910

Devazepide

CCK8s

Log [Compound] nM

% In

hib

itio

n






Cell Line Name: HEK293/D1/Gα15


Gene Synonyms: DRD1; DADR; DRD1A


G coupling Gs

Agonist (±)-SKF-38393



Incubation 25℃


Antagonist R(+)-SCH-23390

hydrochloride



Incubation 25℃

Stimulant (±)-SKF-38393: 11 nM


Ligand [3H]SCH 23390


Kd (nM) 0.6 nM

Non specific droperidol (10 µM)



Reference: R(+)-SCH23390(IC50:1.7

nM)

D1 (Dopamine D1 Receptor)



D1

-2 0 2 4 6-20

0

20

40

60

80

100

120(± )-SKF-38393

Dopamine

7-OH-DPAT

Log [Compound] nMA

cti

vit

y (

%)

D1

-2 0 2 4 6-50

-25

0

25

50

75

100

125L-745870

SCH-23390

Log [Compound] nM

Inh

ibit

ion

(%

)

D1

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Dopamine

7-OH-DPAT

L-745870

Droperidol

R(+)-SCH23390

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: HEK293/D2/Gα15


Gene Synonyms: DRD2; D2R; D2DR


G coupling Gi

Agonist Dopamine



Incubation 25℃


Antagonist Amisulpride



Incubation 25℃

Stimulant Dopamine: 10.5 nM


Ligand [3H]7-OH-DPAT


Kd (nM) 1.7 nM

Non specific droperidol (10 µM)



Reference: (+)-Butaclamol(IC50:1.4

nM)

D2 (Dopamine D2 Receptor)



D2

-2 -1 0 1 2 3 4-20

0

20

40

60

80

100

120Dopamine

7-OH-DPAT

Log [Compound] nM

Acti

vit

y (

%)

D2

-2 0 2 4 60

20

40

60

80

100

120 Amisulpride

Droperidol

(+)Butaclamol

(-)Butaclamol

Log [Compound] nM

Inh

ibit

ion

%

D2

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Dopamine

7-OH-DPAT

L-745870

Droperidol

R(+)-SCH23390

(+)-Butaclamol

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: HEK293/ETA


Gene Synonyms: EDNRA; ETA; ET-A; ETAR; ETRA; MFDA; ETA-R; hET-AR


G coupling Gq

Agonist Endothelin 1



Incubation 25℃


Antagonist BQ-123



Incubation 25℃

Stimulant Endothelin 1: 3.2 nM


Ligand [125I]endothelin-1


Kd (nM) 0.03 nM

Non specific endothelin-1 (0.1 μM)

Incubation 120 min/37°C


Reference: endothelin-1(IC50:0.12

nM)

Eta (Endothelin Receptor Type A)



ETa

-5 -4 -3 -2 -1 0 1 2 3 4

0

25

50

75

100

125Endothelin-1

BQ-123

BQ-788

Log [Compound, nM]

% I

nh

ibit

ion

Eta

-2 -1 0 1 2 3

0

25

50

75

100

125Endothelin 1

Endothelin 3

Log [Compound] nM

% A

cti

vit

y

Eta

-3 -2 -1 0 1 2 3 4-25

0

25

50

75

100

125

BQ-123

BQ-788

Log [Compound] nM

Inh

ibit

ion

(%

)






Cell Line Name: HEK293/H1


Gene Synonyms: HRH1; H1R; H1-R; HH1R; hisH1


G coupling Gq

Agonist Histamine



Incubation 25℃


Antagonist Pyrilamine maleate salt



Incubation 25℃

Stimulant Histamine: 6.3 nM

Antagonist effect IC50: 3.87 Nm

Ligand [3H]pyrilamine


Kd (nM) 2.3 nM

Non specific Pyrilamine (1 µM)



Reference: Pyrilamine(IC50:6.8nM)

H1 (Histamine H1 receptor)


-2 0 2 4-25

0

25

50

75

100

125

H1histamine

2-PEA

Log [Compound] nM

% A

cti

vit

y

H1

-2 0 2 4 6-25

0

25

50

75

100

125Pyrilamine

Clobenpropit

Cimetidine

Log [Compound] nM

Inh

ibit

ion

(%

)

H1

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Pyrilamine

Histamine

Clobenpropit

Cimetdine

Log [Compound] nM

% I

nh

ibit

ion







Cell Line Name: HEK293/H2


Gene Synonyms: H2; HRH2; H2R


G coupling Gq

Agonist Amthamine

dihydrobromide



Incubation 25℃


Antagonist Cimetidine



Incubation 25℃

Stimulant Amthamine

dihydrobromide: 8000 nM


Ligand [3H]Tiotidine


Kd (nM) 0.8 nM

Non specific Cimetdine(10uM)



Reference: Cimetdine(IC50:472.7nM)

H2 (Histamine H2 receptor)



H2

0 1 2 3 4 5

0

25

50

75

100

125

Cimetidine

Ratinidine

Log [Compound] nM

%in

hib

itio

n

H2

0 1 2 3 4 5-20

0

20

40

60

80

100

120Imetit

Histamine

Amthamine

Log [Compound] nM

Acti

vit

y (

%)

H2

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Histamine

Clobenpropit

Cimetdine

Imetit

Log [Compound] nM

% In

hib

itio

n






Cell Line Name: HEK293/5-HT1A/Gα15


Gene Synonyms: HTR1A; G-21; 5HT1a; PFMCD; 5-HT1A; 5-HT-1A; ADRBRL1; ADRB2RL1


G coupling Gi

Agonist 5-CT



Incubation 25℃


Antagonist Methiothepin mesylate salt



Incubation 25℃

Stimulant 5-CT: 20 nM


Ligand [3H]8-OH-DPAT


Kd (nM) 0.6 nM

Non specific 8-OH-DPAT (10 µM)



Reference: 8-OH-DPAT(IC50:1.6nM)

5HT1A (5-HT1A Receptor)



5HT1A

-3 -2 -1 0 1 2 3 4 5-20

0

20

40

60

80

100

120Serotonin

5-CT

8-OH-DPAT

Log [Compound] nMA

cti

vit

y (

%)

5HT1A

0 2 4 6-25

0

25

50

75

100

125

Methiothepin

WAY-100635

Ketanserin

Log [Compound] nM

Inh

ibit

ion

(%

)

5HT1A

-5 -4 -3 -2 -1 0 1 2 3 4

0

25

50

75

100

1255-CT

Serotonin

8-OH-DPAT

WAY-100635

Ketanserin

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: CHO-K1/5-HT1B


Gene Synonyms: 5-HT-1B; 5-HT-1D-beta; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12


G coupling Gi

Agonist 5-HT

Measurement: cAMP Assay

Detection method: HTRF

Incubation 25℃


Cellular Background: Chem-1


Gene Synonyms: 5-HT-1B; 5-HT-1D-beta; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12


Antagonist GR127935

Measurement: cAMP Assay

Detection method: HTRF

Incubation 25℃

Stimulant 5-HT: 20 nM


Ligand [3H]GR125743


Kd (nM) 4.7 nM

Non specific Serotonin (10 μM)



Reference: Serotonin(IC50:85.4 nM)

5HT1B (5-HT1B Receptor)




5HT1B

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Serotonin

Ketanserin

8-OH-DPAT

GR127935

Log [Compound] nM

% I

nh

ibit

ion

5-HT1B

-2 0 2 4 6-20

0

20

40

60

80

100

120

140GR127935

Yohimbine hydrochloride

Ketanserin

Log [Compound] nM

% I

nh

ibit

ion

5-HT1B

-2 0 2 4 6-40

-20

0

20

40

60

80

100

1205-HT

5-CT

8-OH-DPAT

Log [Compound] nM

% A

cti

vit

y






Cell Line Name: HEK293/5-HT2A


Gene Synonyms: HTR2A; HTR2; 5-HT2A


G coupling Gq

Agonist 5-CT



Incubation 25℃




Gene Synonyms: HTR2A; HTR2; 5-HT2A





Incubation 25℃

Stimulant 5-CT: 47 nM


Ligand [3H]-Ketanserin


Kd (nM) 0.6 nM

Non specific (±)DOI (1 µM)



Reference: (±)DOI (IC50:41.0nM)





5HT2A

-4 -2 0 2 4-20

0

20

40

60

80

100

120 5-CT

Serotonin

(± )-DOI hydrochloride

5-Methoxytryptamine

Log [Compound] nMA

cti

vit

y (

%)

5HT2A

-2 0 2 4 6-25

0

25

50

75

100

125Methiothepin mesylate salt

Ketanserin

Log [Compound] nM

Inh

ibit

ion

(%

)

5HT2A

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125(±)DOI

5-Methoxytryptamine

Serotonin

BW723C86

Ketanserin

SB206553

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: HEK293/5-HT2B


Gene Synonyms: 5-HT (2B); 5-HT-2B; 5-HT2B


G coupling Gq

Agonist BW-723C86



Incubation 25℃




Gene Synonyms: 5-HT (2B); 5-HT-2B; 5-HT2B





Incubation 25℃

Stimulant BW-723C86: 20 nM


Ligand [3H]LSD


Kd (nM) 0.93 nM

Non specific Serotonin (50 μM)



Reference: (±)DOI (IC50: 34.1 nM)





5HT2B

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125(±)DOI

5-Methoxytryptamine

Serotonin

BW723C86

Ketanserin

SB206553

Log [Compound] nM

% I

nh

ibit

ion

-2 -1 0 1 2 3 4 5

0

25

50

75

100

125

5HT2B

BW-723C86

Log [Compound] nM

% A

cti

vit

y

-2 -1 0 1 2 3 4 5

0

25

50

75

100

1255HT2B

Methiothepin

Log [Compound] nM

% I

nh

ibit

ion






Cell Line Name: HEK293/M1


Gene Synonyms: CHRM1; M1; HM1; M1R


G coupling Gq/Gi/Gs

Agonist Arecaidine propargyl

ester



Incubation 25℃


Antagonist Pirenzepine

dihydrochloride



Incubation 25℃

Stimulant Arecaidine

propargylester : 1.4 nM


Ligand [3H]NMS


Kd (nM) 0.07 nM

Non specific Atropine (1 μM)



Reference: Pirenzepine (IC50:13.2

nM)

M1 (Muscarinic Acetylcholine M1 Receptor)



M1

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Atropine

4-DAMP

Pirenzepine

Methocatramine

Log [Compound] nM

Inh

ibit

ion

%

M1

-3 -2 -1 0 1 2 3 4-20

0

20

40

60

80

100

120Acetylcholine

Arecaidine propargylester

Carbachol

Log [Compound] nM

Acti

vit

y (

%)

M1

-2 0 2 4 6-25

0

25

50

75

100

125Atropine

4-DAMP

Pirenzepine

Methoctramine

log [Con.] nM

Inh

ibit

ion

%






Cell Line Name: HEK293/M2/Gα15


Gene Synonyms: CHRM2; M2; HM2


G coupling Gi


ester



Incubation 25℃


Antagonist Atropine



Incubation 25℃


propargylester : 89 nM


Ligand [3H]NMS


Kd (nM) 0.19 nM




Reference: Methoctramine (IC50:1.4

nM)

M2 (Muscarinic Acetylcholine M2 Receptor)



M2

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Atropine

4-DAMP

Pirenzepine

Methoctramine

Log [Compound] nM

Inh

ibit

ion

%

M2

-2 -1 0 1 2 3 4 5-20

0

20

40

60

80

100

120APL

Carbachol

Acetylcholine

Log [Compound] nM

Acti

vit

y (

%)

M2

-2 0 2 4 6-25

0

25

50

75

100

125Atropine

4-DAMP

Pirenzepoine

Methoctramine

Log [Compound] nM

Acti

vit

y (

%)






Cell Line Name: HEK293/M3


Gene Synonyms: CHRM3; M3; HM3; EGBRS


G coupling Gq


ester



Incubation 25℃


Antagonist Atropine



Incubation 25℃


propargylester : 1.0 nM


Ligand [3H]NMS


Kd (nM) 0.18 nM




Reference: 4-DAMP (IC50:1.1 nM)

M3 (Cholinergic/Acetylcholine M3 Receptor)



M3

-4 -2 0 2 4-20

0

20

40

60

80

100

120 Arecaidine propargylester

Carbachol

Acetylcholine

Log [Compound] nM

Acti

vit

y (

%)

M3

-4 -2 0 2 4 6-25

0

25

50

75

100

125

Atropine

4-DAMP

Pirenzepine

Log [Compound] nM

Inh

ibit

ion

(%

)

M3

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125Atropine

4-DAMP

Pirenzepine

Methocatramine

Log [Compound] nM

Inh

ibit

ion

%






Cell Line Name: HEK293/delta/Gα15


Gene Synonyms: OPRD1; OPRD


G coupling Gi

Agonist DPDPE



Incubation 25℃


Antagonist Naltrindole



Incubation 25℃

Stimulant DPDPE: 10 nM


Ligand [3H]DADLE


Kd (nM) 0.7 nM

Non specific naltrindole (1 µM)



Reference: Naltrindole(IC50:0.2nM)

op-delta (δ-opioid Receptor)



op-delta

-2 0 2 4 6-20

0

20

40

60

80

100

120DPDPE

DAMGO

U-50488

Log [Compound] nM

Acti

vit

y (

%)

op-delta

-2 -1 0 1 2 3 4 5-20

0

20

40

60

80

100

120

nor-BNI

Naltrindole

Log [Compound] nM

Inh

ibit

ion

(%

)

op-delta

-4 -3 -2 -1 0 1 2 3 4 5-25

0

25

50

75

100

125Naltrindole

DPDPE

(± )trans-U-50488

Log [Compound] nM

% In

hib

itio

n






Cell Line Name: HEK293/Kappa/Gα15


Gene Synonyms: OPRK1; KOR; OPRK; KOR-1; K-OR-1


G coupling Gi

op-kappa

-3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125DPDPE

(± )trans-U-50488

U69593

Log [Compound] nM

% I

nh

ibit

ion

Agonist U69593



Incubation 25℃

Agonist effect EC50: 11.9nM

Antagonist nor-

Binaltorphiminedihydrochlo

ride



Incubation 25℃

Stimulant U69593: 20 nM

Antagonist effect IC50: 0.60nM

Ligand [3H]Diprenorphine


Kd (nM) 0.14 nM

Non specific trans-U-50488 (5 µM)



Reference: U-50488 (IC50:41.8nM)

op-kappa(κ-opioidReceptor)



op-kappa

-1 0 1 2 3 4 5-20

0

20

40

60

80

100

120

U69593

U-50488

DPDPE

DAMGO

log [Compound] nM

Acti

vit

y (

%)

op-kappa

-4 -2 0 2 4 6-20

0

20

40

60

80

100

120

naloxone

nor-Binaltorphimine dihydrochl

5'-GNTI

Log [Compound] nM

Inh

ibit

ion

(%

)






Cell Line Name: HEK293/Mu/Gα15


Gene Synonyms: OPRM1; MOP; MOR; LMOR; MOR1; OPRM; M-OR-1


G coupling Gi

Agonist DAMGO



Incubation 25℃


Antagonist CTOP



Incubation 25℃

Stimulant DAMGO: 20 nM


Ligand [3H]DAMGO


Kd (nM) 0.3 nM

Non specific naltrindole (1 µM)



Reference: DAMGO(IC50:1.7 nM)

op-mu (Μ-opioid Receptor)



op-mu

-4 -2 0 2 4 6-20

0

20

40

60

80

100

120DPDPE

DAMGO

Log [Compound] nM

Acti

vit

y (

%)

op-mu

-1 0 1 2 3 4 5-20

0

20

40

60

80

100

120CTOP

Naltrindole hydrochloride

Log [Compound] nM

Inh

ibit

ion

(%

)

op-mu

-4 -3 -2 -1 0 1 2 3 4 5

0

25

50

75

100

125CTOP

Naltrindole

DPDPE

DAMGO

Log [Compound] nM

% In

hib

itio

n






Cell Line Name: CHO/V1A


Gene Synonyms: AVPR1A; V1aR; AVPR1; AVPR; V1a


G coupling Gq

Agonist [Arg8]Vasopressin acetate



Incubation 25℃


Antagonist [β-Mercapto-β,β-

cyclopentamethylenepropi

onyl1, O-Et-Tyr2, Val4,

Arg8]-Vasopressin



Incubation 25℃

Stimulant [Arg8]Vasopressin acetate:

0.12 nM


Ligand [3H]AVP


Kd (nM) 0.26 nM

Non specific AVP (1 µM)



Reference: [d(CH2)5,Tyr(Me)2]-AVP

(IC50:0.92 nM)

V1A (Arginine Vasopressin Receptor 1A)



V1A

-4 -3 -2 -1 0 1 2 3 4-20

0

20

40

60

80

100

120AVP

Oxytocin

Log [Compound] nM

Acti

vit

y (

%)

V1A

-2 -1 0 1 2 3 4-20

0

20

40

60

80

100

120[β -Mercapto-β β -cyclopentame

[d(CH2)5Tyr(Me)2]-AVP

Log [Compound] nM

Inh

ibit

ion

(%

)

V1A

-4 -3 -2 -1 0 1 2 3 4

0

25

50

75

100

125AVP

[d(CH2)5Tyr(Me)2]-AVP

Oxytocin

Log [Compound] nM

% I

nh

ibit

ion



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WuXi Biology GPCR Cell Lines and Assaysrsd.wuxiapptec.com/Media/Default/ServicesSolutionsImages... · 2018-08-06 · Biology Department of WuXi AppTec (Shanghai) Co., Ltd. 288 Fute