Biology Department of WuXi AppTec (Shanghai) Co., Ltd.
WuXi Biology GPCR Cell Lines and Assays
Receptor G Protein Family Host Cell Line Assay Format (Human) Coupling
A1/ADORA1A Gi/Gq HEK293/Gα15 Calcium/Binding
A2A/ADORA2A Gs CHO/Gα15 Calcium/Binding Adenosine A2B/ADORA2B Gs HEK293/Gα15 Calcium/Binding
A3/ADORA3A Gi CHO/Gα15 Calcium/Binding
alpha1A/ADRA1A Gq HEK293 Calcium/Binding
alpha2A/ADRA2A Gi HEK293/Gα15 Calcium/Binding
alpha2C/ADRA2C Gi HEK293/Gα15 Calcium Adrenergic beta1/ADRA1B Gs HEK293/Gα15 Calcium/Binding
beta2/ADRA2B Gs HEK293/Gα15 Calcium/Binding
beta3/ADRA3B Gs HEK293/Gα15 Calcium
Anaphylotoxin C3aR/C3AR1 Gi HEK293/Gα15 Calcium
AT1/AGTR1 Gq CHO Calcium Angiotensin AT2/AGTR2 Gq CHO Calcium
Bombesin BB2/GRPR Gq HEK293 Calcium/Binding
B1/BDKRB1 Gi/Gq HEK293 Calcium Bradykinin B2/BDKRB2 Gi/Gq HEK293/Gα15 Calcium
CB1/CNR1 Gi HEK293/Gα15 Calcium/Binding Cannabinoid CB2/CNR2 Gi CHO/Gα15 Calcium/Binding
CCR1 Gi HEK293/Gα15 Calcium
CCR2 Gi HEK293/Gα15 Calcium Chemokine CCR4 Gi HEK293/Gα15 Calcium
CCR5 Gi HEK293/Gα15 Calcium
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CCR6 Gi HEK293/Gα15 Calcium
CCR7 Gi HEK293/Gα15 Calcium
CXCR1 Gi HEK293/Gα15 Calcium
CXCR2 Gi HEK293/Gα15 Calcium
CXCR4 Gi HEK293/Gα15 Calcium
CCKA/CCKAR Gq HEK293 Calcium/Binding Cholecystokinin CCKb/CCKBR Gq HEK293 Calcium
Class A Orphans MrgX2 Gi/Gq HEK293/Gα15 Calcium
CRF1/CRHR1 Gs HEK293/Gα15 Calcium Corticotropin Releasing Factor CRF2a/CRHR2 Gs HEK293/Gα15 Calcium
D1/DRD1 Gs HEK293/Gα15 Calcium/Binding Dopamine D2/DRD2 Gi HEK293/Gα15 Calcium/Binding
ETA/EDNRA Gq HEK293 Calcium/Binding Endothelin 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
Calcium/cAMP/Bi GCGR Gs HEK293/Gα15 nding Glucagon Calcium/cAMP/Bi GLP1/GLP1R Gs HEK293/Gα15 nding Gonadotropin- GNRHR Gq HEK293 Calcium releasing hormone
H1/HRH1 Gq HEK293 Calcium/Binding
Histamine H2/HRH2 Gs/Gq HEK293 Calcium/Binding
H3/HRH3 Gi HEK293/Gα15 Calcium
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5-HT1A/HTR1A Gi HEK293/Gα15 Calcium/Binding
5-HT2A/HTR2A Gq HEK293 Calcium/Binding 5- 5-HT1B/HTR1B Gi CHO/Gα15 cAMP/Binding Hydroxytryptamine 5-HT2B/HTR2B Gq CHO-K1 Binding
5-HT7/HTR7 Gs HEK293/Gα15 Calcium/Binding
CYSLTR2 Gq HEK293 Calcium Leukotriene LTB4R1 Gq CHO Calcium
S1P1 Gi CHO/Gα15 Calcium
Lysophospholipid S1P2 Gs/Gq CHO/Gα15 Calcium
S1P5 Gi CHO/Gα15 Calcium
MC3R Gi HEK293/Gα15 Calcium Melanocortin MC4R Gi HEK293/Gα15 Calcium
mGluR2 Gi CHO/Gα15 Calcium
mGluR3 Gi HEK293/Gα15 Calcium Metabotropic Glutamate mGluR4 Gi CHO/Gα15 Calcium
mGluR6 Gi CHO/Gα15 Calcium
Motilin MLNR Gq HEK293 Calcium
Motilin-Canis MLNR Gq HEK293 Calcium
M1/CHRM1 Gq/Gs/Gi HEK293 Calcium/Binding
M2/CHRM2 Gi HEK293/Gα15 Calcium/Binding
Muscarinic 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
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Y2/NPY2R Gi HEK293/Gα15 Calcium
NT1/NTSR1 Gq HEK293 Calcium Neurotensin NT1/NTSR1 Gq HEK293 Calcium
delta/OPRD1 Gi HEK293/Gα15 Calcium/Binding
Opioid kappa/OPRK1 Gi HEK293/Gα15 Calcium/Binding
mu/OPRM1 Gi HEK293/Gα15 Calcium/Binding
OX1/HCRTR1 Gq/Gs/Gi HEK293/Gα15 Calcium Orexin OX2/HCRTR2 Gs HEK293/Gα15 Calcium
Platelet-activating PAF/PTAFR Gq HEK293 Calcium factor
PK1/PROKR1 Gq HEK293 Calcium Prokineticin PK2/PROKR2 Gi HEK293/Gα15 Calcium
EP1/PTGER1 Gq HEK293 Calcium
Prostaglandin EP2/PTGER2 Gs CHO/Gα15 Calcium
EP4/PTGER4 Gs HEK293/Gα15 Calcium
FP/PTGFR Gq HEK293 Calcium
Prostanoid PTGIR/IP1 Gs HEK293/Gα15 Calcium
TP/TBXA2R Gq HEK293 Calcium
Somatostatin SST5 Gi HEK293/Gα15 Calcium
NK1/TACR1 Gq HEK293 Calcium
Tachykinin NK2/TACR2 Gq/Gs HEK293 Calcium
NK3/TACR3 Gq HEK293 Calcium
Thyrotropin- TRH1/TRHR Gq HEK293 Calcium releasing hormone
OT/OXTR Gq HEK293 Calcium Vasopressin/ V1B/AVPR1B Gq HEK293 Calcium Oxytocin V1A/AVPR1A Gq CHO Calcium/Binding
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V2/AVPR2 Gs HEK293/Gα15 Calcium
VPAC1/VIPR1 Gs HEK293/Gα15 Calcium
VIP and PACAP VPAC2/VIPR2 Gs HEK293/Gα15 Calcium PAC1/ADCYAP1 Gs HEK293/Gα15 Calcium R1 Version: 201802
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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.
Receptor G Protein Host Cell Family Assay Format (Human) Coupling Line Adenosine A2A/ADORA2A Gs CHO/Gα15 Calcium/Binding alpha1A/ADRA1A Gq HEK293 Calcium/Binding alpha2A/ADRA2A Gi HEK293/Gα15 Calcium/Binding Adrenergic beta1/ADRA1B Gs HEK293/Gα15 Calcium/Binding beta2/ADRA2B Gs HEK293/Gα15 Calcium/Binding CB1/CNR1 Gi CHO/Gα15 Calcium/Binding Cannabinoid CB2/CNR2 Gi CHO/Gα15 Calcium/Binding Cholecystokinin CCKA/CCKAR Gq HEK293 Calcium/Binding D1/DRD1 Gs HEK293/Gα15 Calcium/Binding Dopamine D2/DRD2 Gi HEK293/Gα15 Calcium/Binding Endothelin ETA/EDNRA Gq HEK293 Calcium/Binding H1/HRH1 Gq HEK293 Calcium/Binding Histamine H2/HRH2 Gs/Gq HEK293 Calcium/Binding 5-HT1A/HTR1A Gi HEK293/Gα15 Calcium/Binding 5- 5-HT2A/HTR2A Gq HEK293 Calcium/Binding Hydroxytryptamine 5-HT1B/HTR1B Gi CHO/Gα15 cAMP/Binding 5-HT2B/HTR2B Gq HEK293 Binding M1/CHRM1 Gq/Gs/Gi HEK293 Calcium/Binding Muscarinic M2/CHRM2 Gi HEK293/Gα15 Calcium/Binding M3/CHRM3 Gq HEK293 Calcium/Binding delta/OPRD1 Gi HEK293/Gα15 Calcium/Binding Opioid kappa/OPRK1 Gi HEK293/Gα15 Calcium/Binding mu/OPRM1 Gi HEK293/Gα15 Calcium/Binding Vasopressin V1A/AVPR1A Gq CHO Calcium/Binding Version: 201802
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ADORA2A (Adenosine A2A Receptor)
Cell Line Name: HEK293/A2A/Gα15 Species/Source: Human/Recombinant Gene Synonyms: ADORA2A ; A2aR; ADORA2; RDC8 Accession Number: NM_000675 G coupling Gs
Functional Assay-Calcium Flux Assay
ADORA2A NECA 120 Agonist NECA CPA 100 Measurement: Intracellular Ca2+ 80 Detection method: FLIPR Fluorimetry 60 Incubation 25℃ 40
Activity (%) Activity 20 Agonist effect EC50: 5.4 nM 0 -20 -2 0 2 4 6 Log [Compound] nM ADORA2A 120 Antagonist CGS-15943 CGS-15943 100 2+ ZM241385 Measurement: Intracellular Ca 80 Detection method: FLIPR Fluorimetry 60 Incubation 25℃ 40 20
Inhibition (%) Inhibition Stimulant NECA: 40 nM 0 Antagonist effect IC50: 0.22 nM -20 -4 -2 0 2 4 Log [Compound] nM
ADORA2A (Adenosine A2A Receptor)
Cellular Background: HEK293 Species/Source: Human/Recombinant Gene Synonyms: ADORA2A ; A2aR; ADORA2; RDC8 Accession Number: NM_000675
Radio ligand binding Assay
ADORA2A Ligand [3H] CGS 21680 125 NECA Ligand concentration 6 nM 100 CPA ZM241385 Kd (nM) 47.5 nM 75 CGS15943 Non specific NECA (10 μM) 50
Incubation 120 min/RT Inhibition % 25
Detection method Scintillation counting 0
Reference: NECA (IC50:82.0 nM) -4 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM
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Alpha1A (Alpha-1-adrenergic receptor)
Cell Line Name: HEK293/Alpha1A Species/Source: Human/Recombinant Gene Synonyms: ADRA1A; ADRA1C; ADRA1L1; ALPHA1AAR Accession Number: NM_000680 (isoform 1) G coupling Gq
Functional Assay-Calcium Flux Assay
Alpha1A 120 Agonist (-)Epinephrine (-)-Epinephrine (E4642) 100 A-61603 Measurement: Intracellular Ca2+ 80 60 Detection method: FLIPR Fluorimetry 40
(%) Activity Incubation 25℃ 20 0 Agonist effect EC50: 4.0 nM -2 -1 0 1 2 3 4 Log [Compound] nM
Alpha1A 5-Methylurapidil Antagonist 5-Methylurapidil 120 WB-4104 Measurement: Intracellular Ca2+ 100 Prazosin 80 BMY7378 Detection method: FLIPR Fluorimetry 60 Incubation 25℃ 40 Inhibition (%) Inhibition 20 Stimulant (-)Epinephrine : 6.3 nM 0 -2 0 2 4 6 Antagonist effect IC50: 3.6 nM Log [Compound] nM
Radio ligand binding Assay
Ligand [3H]prazosin Alpha1A 125 WB4101 Ligand concentration 0.2 nM 100 Epinephrine Prazosin Kd (nM) 0.09 nM 75 Non specific epinephrine (0.1 mM) 50
% Inhibition % 25 Incubation 60 min/RT 0 Detection method Scintillation counting -3 -2 -1 0 1 2 3 4 5 Reference: WB 4101 (IC50:0.28 Log [Compound] nM nM)
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Alpha2A (Alpha-2-adrenergic receptor) Cell Line Name: HEK293/Alpha2A/Gα15 Species/Source: Human/Recombinant Gene Synonyms: ADRA2A; ADRA2; ADRAR; ZNF32; ADRA2R; ALPHA2AAR Accession Number: NM_000681 (isoform 1) G coupling Gi
Functional Assay-Calcium Flux Assay
Alpha2A UK 14304 Agonist UK14304 120 Epinephrine (E4250) 100 Measurement: Intracellular Ca2+ 80 Detection method: FLIPR Fluorimetry 60 ℃ 40 Incubation 25 (%) Activity 20
Agonist effect EC50: 0.14 nM 0 -20 -2 0 2 Log [Compound] nM
Alpha2A 125 Antagonist Yohimbine hydrochloride Yohimbin 100 RX 821002 2+ Measurement: Intracellular Ca 75 Prazosin Detection method: FLIPR Fluorimetry 50 25
Incubation 25℃ (%) Inhibition 0 Stimulant UK14304 : 4.3 nM -25 -2 -1 0 1 2 3 4 Antagonist effect IC50: 32.6 nM Log [Compound] nM
Radio ligand binding Assay
Alpha2A Ligand [3H]RX 821002 125 Epinephrine Ligand concentration 0.5 nM 100 Prazosin Yohimbin 75 Kd (nM) 0.46 nM RX821002 Non specific epinephrine (0.1 mM) 50 UK14304
Incubation 60 min/RT Inhibition % 25 0 Detection method Scintillation counting -2 -1 0 1 2 3 4 5 Reference: Rx81002(IC50:2.3 nM) Log [Compound] nM
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Beta1 (Beta-1 Adrenergic Receptor)
Cell Line Name: HEK293/Beta1/Gα15 Species/Source: Human/Recombinant Gene Synonyms: ADRB1; RHR; B1AR; ADRB1R; BETA1AR Accession Number: NM_000684 G coupling Gs
Functional Assay-Calcium Flux Assay
Beta1 (-)Epinephrine 120 Isoproterenol Agonist (-)Epinephrine 100 Salbutamol hemisulfate Measurement: Intracellular Ca2+ 80 60 Detection method: FLIPR Fluorimetry 40
Activity (%) Activity 20 Incubation 25℃ 0 Agonist effect EC50: 2.72 nM -20 -2 -1 0 1 2 3 4 5 Log [Compound] nM
Beta1 120 Antagonist Carvedilol Carvedilol 100 (± )-Propranolol hydrochloride Measurement: Intracellular Ca2+ 80 Atenolol 60 ICI 118 551 hydrochloride Detection method: FLIPR Fluorimetry 40 20
Inhibition (%) Inhibition Incubation 25℃ 0 -20 Stimulant (-)-Epinephrine : 20 nM -2 -1 0 1 2 3 4 Log [Compound] nM Antagonist effect IC50: 4.75 nM
Radio ligand binding Assay
Beta1 125 Ligand [3H](-)CGP 12177 Atenolol
Ligand concentration 0.3 nM 100 Salbutamol Propranolol 75 Kd (nM) 0.04 nM ICI118551 50 Non specific propranolol (2 µM) Isoproternol
% Inhibition % 25 Incubation 120 min/RT 0 Detection method Scintillation counting -4 -3 -2 -1 0 1 2 3 4 5 Reference: Atenolol (IC50:857 nM) Log [Compound] nM
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Beta2 (Beta-2 Adrenergic Receptor)
Cell Line Name: HEK293/Beta2/Gα15 Species/Source: Human/Recombinant Gene Synonyms: ADRB2; BAR; B2AR; ADRBR; ADRB2R; BETA2AR Accession Number: NM_000024 G coupling Gs/Gi
Functional Assay-Calcium Flux Assay
Beta2 Adrenaline Agonist Adrenaline 120 Isoproterenol 100 Salbutamol hemisulfate 2+ Measurement: Intracellular Ca 80
Detection method: FLIPR Fluorimetry 60 40
Incubation 25℃ (%) Activity 20
Agonist effect EC50: 0.11 nM 0 -20 -4 -3 -2 -1 0 1 2 3 4 Log [Compound] nM
Beta2 Carvedilol Antagonist Carvedilol 125 (± )-Propranolol hydrochloride ICI 118551 Measurement: Intracellular Ca2+ 100 75 Detection method: FLIPR Fluorimetry 50
Incubation 25℃ 25
Inhibition (%) Inhibition Stimulant Adrenaline: 0.43 nM 0 -25 Antagonist effect IC50: 7.07 nM -2 -1 0 1 2 3 Log [Compound] nM
Radio ligand binding Assay
Beta2 Ligand [3H](-)CGP 12177 125 Atenolol Ligand concentration 0.3 nM 100 Salbutamol Propranolol Kd (nM) 0.1 nM 75 ICI118551 Non specific propranolol (2 µM) 50 Isoproternol
Incubation 120 min/RT Inhibition % 25
Detection method Scintillation counting 0
Reference: ICI118551(IC50:3.3 nM) -4 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM
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CB1 (Cannabinoid Type 1 Receptor)
Cell Line Name: CHO/CB1/Gα15 Species/Source: Human/Recombinant Gene Synonyms: CNR1; CB1; CNR; CB-R; CB1A; CB1R; CANN6; CB1K5 Accession Number: NM_016083 (isoform1) G coupling Gi
Functional Assay-Calcium Flux Assay
CB1 WIN55212-2 Agonist WIN55212-2 120 CP55940 2+ 100 Anandamide Measurement: Intracellular Ca 80
Detection method: FLIPR Fluorimetry 60 40
Incubation 25℃ (%) Activity 20
Agonist effect EC50:352 nM 0 -20 -1 0 1 2 3 4 5 6 Log [Compound] nM
CB1 Antagonist Rimonabant hydrochloride Rimonabant 120 2+ AM281 Measurement: Intracellular Ca 100 AM630 Detection method: FLIPR Fluorimetry 80 60 Incubation 25℃ 40 20 Inhibition (%) Inhibition Stimulant WIN55212-2: 4000 nM 0 -20 Antagonist effect IC50: 12.5 nM -1 0 1 2 3 4 5 6 log [Con.] nM
CB1 (Cannabinoid Type 1 Receptor)
Cellular Background: CHO-K1 Species/Source: Human/Recombinant Gene Synonyms: CNR1; CB1; CNR; CB-R; CB1A; CB1R; CANN6; CB1K5 Accession Number: X54937
Radio ligand binding Assay
Ligand [3H]CP 55940 CB1 125 Ligand concentration 0.4 nM CP55940 100 WIN55212-2 AM281 Kd (nM) 3.7 nM 75 Anandamide Non specific WIN 55212-2 (5 µM) 50
Incubation 120 min/37℃ Inhibition % 25 0 Detection method Scintillation counting -3 -2 -1 0 1 2 3 4 5 Reference: CP 55940 (0.81 nM) Log [Compound] nM
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CB2 (Cannabinoid Type 2 Receptor)
Cell Line Name: CHO/CB2/Gα15 Species/Source: Human/Recombinant Gene Synonyms: CNR2; CB2; CX5; CB-2 Accession Number: NM_001841 G coupling Gi
Functional Assay-Calcium Flux Assay
CB2 120 Agonist CP55940 CP55940 2+ 100 WIN55215-2 Measurement: Intracellular Ca 80 Anandamide Detection method: FLIPR Fluorimetry 60 40
℃ Activity (%) Incubation 25 20 Agonist effect EC50: 199 nM 0 -1 0 1 2 3 4 5 Log [Compound] nM
Antagonist AM630 CB2 120 2+ AM630 Measurement: Intracellular Ca 100 AM281 Detection method: FLIPR Fluorimetry 80 Rimonbant 60 Incubation 25℃ 40 20 Stimulant CP55940: 300 nM (%) Inhibition 0 Antagonist effect IC50: 563 nM -20 0 1 2 3 4 5 Log [Compound] nM
Radio ligand binding Assay
Ligand [3H]CP 55940 CB2 125 Ligand concentration 0.5 nM CP55940 100 WIN55212-2 Anandomide Kd (nM) 5.1 nM 75 AM630 Non specific WIN 55212-2 (5 µM) 50 AM281
% Inhibition % 25 Incubation 120 min/37℃ 0
Detection method Scintillation counting -3 -2 -1 0 1 2 3 4 5 Reference: WIN55212-2(IC50: Log [Compound] nM 2.2nM)
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CCKA (Cholecystokinin A Receptor)
Cell Line Name: HEK293/CCKA Species/Source: Human/Recombinant Gene Synonyms: CCKAR; CCK-A; CCK1R; CCKRA; CCK1-R Accession Number: NM_000730 G coupling Gq
Functional Assay-Calcium Flux Assay
CCKA Agonist CCK-4 120 CCK-4 2+ Measurement: Intracellular Ca 100 CCK-8s 80 Detection method: FLIPR Fluorimetry 60 Incubation 25℃ 40 (%) Activity Agonist effect EC50: 80 nM 20 0 -4 -2 0 2 4 Log [Compound] nM CCKA Antagonist Lorglumide Lorglumide 120 2+ Devazepide Measurement: Intracellular Ca 100 LY 225910 Detection method: FLIPR Fluorimetry 80 60 Incubation 25℃ 40 20 Stimulant CCK-4: 557 nM (%) Inhibition 0 Antagonist effect IC50: 635 nM -20 0 1 2 3 4 5 Log [Compound] nM CCKA (Cholecystokinin A Receptor) Cellular Background: 1321-N1 Species/Source: Human/Recombinant Gene Synonyms: CCKAR; CCK-A; CCK1R; CCKRA; CCK1-R Accession Number: L19315
Radio ligand binding Assay
Ligand [3H]CCK-8s CCKA 125 Ligand concentration 0.5 nM CCK8s 100 Devazepide LY225910 Kd (nM) 0.22 nM 75
Non specific CCK-8s (1 μM) 50
% Inhibition 25 Incubation 60 min/RT 0 Detection method Scintillation counting -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM Reference: CCK-8s(IC50: 2.4 nM)
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D1 (Dopamine D1 Receptor)
Cell Line Name: HEK293/D1/Gα15 Species/Source: Human/Recombinant Gene Synonyms: DRD1; DADR; DRD1A Accession Number: NM_000794 G coupling Gs
Functional Assay-Calcium Flux Assay
D1 (± )-SKF-38393 120 Agonist (±)-SKF-38393 Dopamine 100 2+ 7-OH-DPAT Measurement: Intracellular Ca 80
Detection method: FLIPR Fluorimetry 60 40
Incubation 25℃ (%) Activity 20
Agonist effect EC50: 5.1 nM 0 -20 -2 0 2 4 6 Log [Compound] nM
D1 Antagonist R(+)-SCH-23390 125 L-745870 hydrochloride 100 SCH-23390 75 2+ Measurement: Intracellular Ca 50 Detection method: FLIPR Fluorimetry 25 0
Inhibition (%) Inhibition Incubation 25℃ -25 -2 0 2 4 6 -50 Stimulant (±)-SKF-38393: 11 nM Log [Compound] nM Antagonist effect IC50: 1.3 nM
Radio ligand binding Assay
D1 125 Ligand [3H]SCH 23390 Dopamine 100 7-OH-DPAT Ligand concentration 0.3 nM L-745870 75 Kd (nM) 0.6 nM Droperidol 50 R(+)-SCH23390 Non specific droperidol (10 µM)
% Inhibition % 25
Incubation 60 min/RT 0
Detection method Scintillation counting -4 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM Reference: R(+)-SCH23390(IC50:1.7 nM)
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D2 (Dopamine D2 Receptor)
Cell Line Name: HEK293/D2/Gα15 Species/Source: Human/Recombinant Gene Synonyms: DRD2; D2R; D2DR Accession Number: NM_000795 G coupling Gi
Functional Assay-Calcium Flux Assay
D2 Dopamine 120 7-OH-DPAT Agonist Dopamine 100
Measurement: Intracellular Ca2+ 80 60 Detection method: FLIPR Fluorimetry 40
(%) Activity Incubation 25℃ 20 0 Agonist effect EC50: 3.1 nM -20 -2 -1 0 1 2 3 4 Log [Compound] nM
D2 120 Amisulpride Antagonist Amisulpride Droperidol 100 Measurement: Intracellular Ca2+ (+)Butaclamol 80 (-)Butaclamol Detection method: FLIPR Fluorimetry 60 40 Incubation 25℃ Inhibition% 20
Stimulant Dopamine: 10.5 nM 0 -2 0 2 4 6 Antagonist effect IC50: 4.8 nM Log [Compound] nM
Radio ligand binding Assay
Ligand [3H]7-OH-DPAT D2 125 Dopamine Ligand concentration 1 nM 100 7-OH-DPAT L-745870 Kd (nM) 1.7 nM 75 Droperidol Non specific droperidol (10 µM) 50 R(+)-SCH23390 (+)-Butaclamol Incubation 60 min/RT Inhibition % 25 0 Detection method Scintillation counting -4 -3 -2 -1 0 1 2 3 4 5 Reference: (+)-Butaclamol(IC50:1.4 Log [Compound] nM nM)
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Eta (Endothelin Receptor Type A)
Cell Line Name: HEK293/ETA Species/Source: Human/Recombinant Gene Synonyms: EDNRA; ETA; ET-A; ETAR; ETRA; MFDA; ETA-R; hET-AR Accession Number: NM_001957 G coupling Gq
Functional Assay-Calcium Flux Assay
Eta 125 Agonist Endothelin 1 Endothelin 1 Measurement: Intracellular Ca2+ 100 Endothelin 3 75 Detection method: FLIPR Fluorimetry 50 ℃
Incubation 25 % Activity 25 Agonist effect EC50: 1.6 nM 0 -2 -1 0 1 2 3 Log [Compound] nM
Eta BQ-123 Antagonist BQ-123 125 BQ-788 100 Measurement: Intracellular Ca2+ 75 Detection method: FLIPR Fluorimetry 50
Incubation ℃ 25 25 (%) Inhibition 0 Stimulant Endothelin 1: 3.2 nM -25 Antagonist effect IC50: 3.0 nM -3 -2 -1 0 1 2 3 4 Log [Compound] nM
Radio ligand binding Assay
ETa Ligand [125I]endothelin-1 125 Ligand concentration 0.03 nM Endothelin-1 100 BQ-123 BQ-788 Kd (nM) 0.03 nM 75 Non specific endothelin-1 (0.1 μM) 50
Incubation 120 min/37°C Inhibition % 25 Detection method Scintillation counting 0 -5 -4 -3 -2 -1 0 1 2 3 4 Reference: endothelin-1(IC50:0.12 Log [Compound, nM] nM)
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Cell Line Name: HEK293/H1 Species/Source: Human/Recombinant Gene Synonyms: HRH1; H1R; H1-R; HH1R; hisH1 Accession Number: NM_000861 G coupling Gq
Functional Assay-Calcium Flux Assay
H1 histamine 125 2-PEA Agonist Histamine 100 2+ Measurement: Intracellular Ca 75
Detection method: FLIPR Fluorimetry 50
Incubation 25℃ % Activity 25 0 Agonist effect EC50: 2.39 nM -25 -2 0 2 4 Log [Compound] nM Antagonist Pyrilamine maleate salt H1 125 Measurement: Intracellular Ca2+ Pyrilamine 100 Clobenpropit Detection method: FLIPR Fluorimetry 75 Cimetidine Incubation 25℃ 50 25
Stimulant Histamine: 6.3 nM (%) Inhibition 0 Antagonist effect IC50: 3.87 Nm -25 -2 0 2 4 6 Log [Compound] nM
Radio ligand binding Assay
H1 Ligand [3H]pyrilamine 125 Pyrilamine Ligand concentration 1 nM 100 Histamine Clobenpropit 75 Kd (nM) 2.3 nM Cimetdine Non specific Pyrilamine (1 µM) 50
% Inhibition % 25 Incubation 60 min/RT 0
Detection method Scintillation counting -4 -3 -2 -1 0 1 2 3 4 5 Reference: Pyrilamine(IC50:6.8nM) Log [Compound] nM
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Cell Line Name: HEK293/H2 Species/Source: Human/Recombinant Gene Synonyms: H2; HRH2; H2R Accession Number: NM_022304 G coupling Gq
Functional Assay-Calcium Flux Assay
H2 Imetit Agonist Amthamine 120 Amthamine 100 dihydrobromide Histamine 80 2+ Measurement: Intracellular Ca 60 40 Detection method: FLIPR Fluorimetry (%) Activity 20 Incubation 25℃ 0 -20 Agonist effect EC50: 1125 nM 0 1 2 3 4 5 Log [Compound] nM
H2 Cimetidine Antagonist Cimetidine 125 Ratinidine Measurement: Intracellular Ca2+ 100 75 Detection method: FLIPR Fluorimetry 50 Incubation 25℃
%inhibition 25 Stimulant Amthamine 0 dihydrobromide: 8000 nM 0 1 2 3 4 5 Antagonist effect IC50: 111.8 nM Log [Compound] nM
Radio ligand binding Assay
H2 Ligand [3H]Tiotidine 125 Histamine Ligand concentration 1 nM 100 Clobenpropit Cimetdine Kd (nM) 0.8 nM 75 Imetit Non specific Cimetdine(10uM) 50
Incubation 60 min/RT Inhibition % 25
Detection method Scintillation counting 0
Reference: Cimetdine(IC50:472.7nM) -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM
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5HT1A (5-HT1A Receptor)
Cell Line Name: HEK293/5-HT1A/Gα15 Species/Source: Human/Recombinant Gene Synonyms: HTR1A; G-21; 5HT1a; PFMCD; 5-HT1A; 5-HT-1A; ADRBRL1; ADRB2RL1 Accession Number: NM_000524 G coupling Gi
Functional Assay-Calcium Flux Assay
Agonist 5-CT 5HT1A 120 5-CT 2+ Serotonin Measurement: Intracellular Ca 100 8-OH-DPAT Detection method: FLIPR Fluorimetry 80 60 Incubation 25℃ 40
Agonist effect EC50: 0.72 nM (%) Activity 20 0 -20 -3 -2 -1 0 1 2 3 4 5 Antagonist Methiothepin mesylate salt Log [Compound] nM 5HT1A Methiothepin 2+ Measurement: Intracellular Ca 125 WAY-100635 Ketanserin Detection method: FLIPR Fluorimetry 100 Incubation 25℃ 75 Stimulant 5-CT: 20 nM 50 25
Inhibition (%) Inhibition Antagonist effect IC50: 42.3 nM 0 0 2 4 6 -25 Log [Compound] nM
Radio ligand binding Assay
Ligand [3H]8-OH-DPAT 5HT1A 125 Ligand concentration 0.3 nM 5-CT 100 Serotonin 8-OH-DPAT Kd (nM) 0.6 nM 75 WAY-100635 Non specific 8-OH-DPAT (10 µM) 50 Ketanserin
Incubation 60 min/RT Inhibition % 25 0
Detection method Scintillation counting -5 -4 -3 -2 -1 0 1 2 3 4 Reference: 8-OH-DPAT(IC50:1.6nM) Log [Compound] nM
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5HT1B (5-HT1B Receptor) Cell Line Name: CHO-K1/5-HT1B Species/Source: Human/Recombinant Gene Synonyms: 5-HT-1B; 5-HT-1D-beta; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12 Accession Number: NM_000863 G coupling Gi
Functional Assay-Calcium Flux Assay
Agonist 5-HT 5-HT1B 120 5-HT Measurement: cAMP Assay 100 5-CT 80 Detection method: HTRF 8-OH-DPAT 60 Incubation 25℃ 40 20 Agonist effect EC50: 3.75 nM Activity % 0 -20 -40 -2 0 2 4 6 Log [Compound] nM
5-HT1B Antagonist GR127935 140 GR127935 Measurement: cAMP Assay 120 Yohimbine hydrochloride 100 Detection method: HTRF Ketanserin 80 Incubation 25℃ 60 40
Stimulant 5-HT: 20 nM Inhibition % 20 Antagonist effect IC50: 0.92 nM 0 -20 -2 0 2 4 6 Log [Compound] nM
5HT1B (5-HT1B Receptor) Cellular Background: Chem-1 Species/Source: Human/Recombinant Gene Synonyms: 5-HT-1B; 5-HT-1D-beta; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12 Accession Number: NM_000863
Radio ligand binding Assay
Ligand [3H]GR125743 5HT1B 125 Ligand concentration 4 nM Serotonin 100 Ketanserin Kd (nM) 4.7 nM 8-OH-DPAT 75 Non specific Serotonin (10 μM) GR127935 50 Incubation 120 min/RT
% Inhibition % 25
Detection method Scintillation counting 0
Reference: Serotonin(IC50:85.4 nM) -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM
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5HT2A (5-HT2A Receptor)
Cell Line Name: HEK293/5-HT2A Species/Source: Human/Recombinant Gene Synonyms: HTR2A; HTR2; 5-HT2A Accession Number: NM_000621 G coupling Gq
Functional Assay-Calcium Flux Assay
Agonist 5-CT 5HT2A Measurement: Intracellular Ca2+ 120 5-CT 100 Serotonin (± )-DOI hydrochloride 80 Detection method: FLIPR Fluorimetry 5-Methoxytryptamine 60 Incubation 25℃ 40
Agonist effect EC50: 25.5 nM (%) Activity 20 0 -20 -4 -2 0 2 4 Log [Compound] nM Antagonist Methiothepin mesylate salt 5HT2A 125 2+ Methiothepin mesylate salt Measurement: Intracellular Ca 100 Ketanserin Detection method: FLIPR Fluorimetry 75 50
Incubation 25℃ 25
Inhibition (%) Inhibition Stimulant 5-CT: 47 nM 0 -25 Antagonist effect IC50: 138.5 nM -2 0 2 4 6 Log [Compound] nM
5HT2A (5-HT2A Receptor)
Cellular Background: CHO-K1 Species/Source: Human/Recombinant Gene Synonyms: HTR2A; HTR2; 5-HT2A Accession Number: X57830
Radio ligand binding Assay
Ligand [3H]-Ketanserin 5HT2A 125 Ligand concentration 0.5 nM (±)DOI 100 5-Methoxytryptamine Serotonin Kd (nM) 0.6 nM 75 BW723C86 Non specific (±)DOI (1 µM) 50 Ketanserin SB206553 Incubation 60 min/RT Inhibition % 25 0 Detection method Scintillation counting -4 -3 -2 -1 0 1 2 3 4 5 Reference: (±)DOI (IC50:41.0nM) Log [Compound] nM
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5HT2B (5-HT2B Receptor) Cell Line Name: HEK293/5-HT2B Species/Source: Human/Recombinant Gene Synonyms: 5-HT (2B); 5-HT-2B; 5-HT2B Accession Number: NM_000867 G coupling Gq
Functional Assay-Calcium Flux Assay
5HT2B 125 Agonist BW-723C86 Methiothepin 100 Measurement: Intracellular Ca2+ 75 Detection method: FLIPR Fluorimetry 50 Incubation 25℃
% Inhibition % 25
Agonist effect EC50: 4.827 nM 0
-2 -1 0 1 2 3 4 5 Log [Compound] nM 5HT2B 125 Antagonist Methiothepin mesylate salt BW-723C86 100 Measurement: Intracellular Ca2+ 75
Detection method: FLIPR Fluorimetry 50
Incubation 25℃ Activity % 25 Stimulant BW-723C86: 20 nM 0
Antagonist effect IC50: 34.6 nM -2 -1 0 1 2 3 4 5 Log [Compound] nM
5HT2B (5-HT2B Receptor) Cellular Background: CHO-K1 Species/Source: Human/Recombinant Gene Synonyms: 5-HT (2B); 5-HT-2B; 5-HT2B Accession Number: X77307
Radio ligand binding Assay
Ligand [3H]LSD 5HT2B 125 Ligand concentration 1 nM (±)DOI 100 5-Methoxytryptamine Kd (nM) 0.93 nM Serotonin 75 Non specific Serotonin (50 μM) BW723C86 50 Ketanserin Incubation 60 min/RT SB206553
% Inhibition % 25
Detection method Scintillation counting 0
Reference: (±)DOI (IC50: 34.1 nM) -4 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM
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M1 (Muscarinic Acetylcholine M1 Receptor)
Cell Line Name: HEK293/M1 Species/Source: Human/Recombinant Gene Synonyms: CHRM1; M1; HM1; M1R Accession Number: NM_000738 G coupling Gq/Gi/Gs
Functional Assay-Calcium Flux Assay
M1 Arecaidine propargylester 120 Agonist Arecaidine propargyl Acetylcholine 100 Carbachol ester 80 60 Measurement: Intracellular Ca2+ 40 Detection method: FLIPR Fluorimetry (%) Activity 20 0 Incubation 25℃ -20 -3 -2 -1 0 1 2 3 4 Agonist effect EC50: 0.95 nM Log [Compound] nM
M1 Atropine Antagonist Pirenzepine 125 Pirenzepine dihydrochloride 100 Methoctramine 4-DAMP Measurement: Intracellular Ca2+ 75 50
Detection method: FLIPR Fluorimetry 25
Inhibition% Incubation 25℃ 0 -2 0 2 4 6 Stimulant Arecaidine -25 log [Con.] nM propargylester : 1.4 nM Antagonist effect IC50: 34 nM
Radio ligand binding Assay
M1 Ligand [3H]NMS 125 Atropine Ligand concentration 0.2 nM 100 4-DAMP Pirenzepine Kd (nM) 0.07 nM 75 Methocatramine Non specific Atropine (1 μM) 50
Incubation 60 min/RT Inhibition% 25
Detection method Scintillation counting 0
Reference: Pirenzepine (IC50:13.2 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM nM)
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M2 (Muscarinic Acetylcholine M2 Receptor)
Cell Line Name: HEK293/M2/Gα15 Species/Source: Human/Recombinant Gene Synonyms: CHRM2; M2; HM2 Accession Number: NM_000739 G coupling Gi
Functional Assay-Calcium Flux Assay
M2
Agonist Arecaidine propargyl 120 APL 100 Carbachol ester 80 Acetylcholine
Measurement: Intracellular Ca2+ 60 40
Detection method: FLIPR Fluorimetry (%) Activity 20
Incubation 25℃ 0 -20 Agonist effect EC50: 25.2 nM -2 -1 0 1 2 3 4 5 Log [Compound] nM
M2 Atropine 125 Pirenzepoine Antagonist Atropine 100 Methoctramine Measurement: Intracellular Ca2+ 75 4-DAMP 50 Detection method: FLIPR Fluorimetry 25
Activity (%) Activity Incubation 25℃ 0 Stimulant Arecaidine -25 -2 0 2 4 6 propargylester : 89 nM Log [Compound] nM Antagonist effect IC50: 0.14 nM
Radio ligand binding Assay
M2 Ligand [3H]NMS 125 Atropine Ligand concentration 0.2 nM 100 4-DAMP Pirenzepine Kd (nM) 0.19 nM 75 Methoctramine Non specific Atropine (1 μM) 50
Inhibition% Incubation 60 min/RT 25 0 Detection method Scintillation counting
Reference: Methoctramine (IC50:1.4 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM nM)
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M3 (Cholinergic/Acetylcholine M3 Receptor)
Cell Line Name: HEK293/M3 Species/Source: Human/Recombinant Gene Synonyms: CHRM3; M3; HM3; EGBRS Accession Number: NM_000740 G coupling Gq
Functional Assay-Calcium Flux Assay
M3
120 Arecaidine propargylester Agonist Arecaidine propargyl 100 Carbachol
ester 80 Acetylcholine 60 Measurement: Intracellular Ca2+ 40 Detection method: FLIPR Fluorimetry (%) Activity 20 0 Incubation ℃ 25 -20 -4 -2 0 2 4 Agonist effect EC50: 0.36 nM Log [Compound] nM
M3 Atropine Antagonist Atropine 125 4-DAMP Pirenzepine Measurement: Intracellular Ca2+ 100 Detection method: FLIPR Fluorimetry 75 50 Incubation 25℃ 25
Inhibition (%) Inhibition Stimulant Arecaidine 0 propargylester : 1.0 nM -25 -4 -2 0 2 4 6 Antagonist effect IC50: 1.4 nM Log [Compound] nM
Radio ligand binding Assay
M3 125 Ligand [3H]NMS Atropine 100 Ligand concentration 0.2 nM 4-DAMP Pirenzepine 75 Kd (nM) 0.18 nM Methocatramine 50 Non specific Atropine (1 μM) Inhibition% 25 Incubation 60 min/RT 0 Detection method Scintillation counting -3 -2 -1 0 1 2 3 4 5 Reference: 4-DAMP (IC50:1.1 nM) Log [Compound] nM
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op-delta (δ-opioid Receptor)
Cell Line Name: HEK293/delta/Gα15 Species/Source: Human/Recombinant Gene Synonyms: OPRD1; OPRD Accession Number: NM_000911 G coupling Gi
Functional Assay-Calcium Flux Assay
op-delta DPDPE 120 DAMGO Agonist DPDPE 100 U-50488 Measurement: Intracellular Ca2+ 80 60 Detection method: FLIPR Fluorimetry 40 Incubation 25℃ (%) Activity 20 0 Agonist effect EC50: 0.5 nM -20 -2 0 2 4 6 Log [Compound] nM
op-delta nor-BNI 120 Antagonist Naltrindole Naltrindole 100 2+ Measurement: Intracellular Ca 80 60 Detection method: FLIPR Fluorimetry 40 20 Incubation 25℃ (%) Inhibition 0 Stimulant DPDPE: 10 nM -20 -2 -1 0 1 2 3 4 5 Antagonist effect IC50: 1.62 nM Log [Compound] nM
Radio ligand binding Assay
Ligand [3H]DADLE op-delta Ligand concentration 0.5 nM 125 Naltrindole Kd (nM) 0.7 nM 100 DPDPE 75 (± )trans-U-50488 Non specific naltrindole (1 µM) 50 Incubation 60 min/RT 25 % Inhibition Detection method Scintillation counting 0 -25 Reference: Naltrindole(IC50:0.2nM) -4 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM
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op-kappa(κ-opioidReceptor)
Cell Line Name: HEK293/Kappa/Gα15 Species/Source: Human/Recombinant Gene Synonyms: OPRK1; KOR; OPRK; KOR-1; K-OR-1 Accession Number: NM_000912 G coupling Gi
Functional Assay-Calcium Flux Assay
op-kappa U69593 120 U-50488 Agonist U69593 DPDPE 100 2+ DAMGO Measurement: Intracellular Ca 80 Detection method: FLIPR Fluorimetry 60 40
Incubation 25℃ (%) Activity 20 0 Agonist effect EC50: 11.9nM -20 -1 0 1 2 3 4 5 log [Compound] nM
nor-Binaltorphimine dihydrochl op-kappa Antagonist nor- naloxone Binaltorphiminedihydrochlo 120 5'-GNTI 100 ride 80 Measurement: Intracellular Ca2+ 60 40 20 Detection method: FLIPR Fluorimetry (%) Inhibition Incubation 25℃ 0 -20 -4 -2 0 2 4 6 Stimulant U69593: 20 nM Log [Compound] nM Antagonist effect IC50: 0.60nM
Radio ligand binding Assay
Ligand [3H]Diprenorphine op-kappa 125 DPDPE Ligand concentration 0.3 nM 100 (± )trans-U-50488 U69593 Kd (nM) 0.14 nM 75 50 Non specific trans-U-50488 (5 µM)
% Inhibition % 25
Incubation 60 min/RT 0
Detection method Scintillation counting -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM Reference: U-50488 (IC50:41.8nM)
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op-mu (Μ-opioid Receptor)
Cell Line Name: HEK293/Mu/Gα15 Species/Source: Human/Recombinant Gene Synonyms: OPRM1; MOP; MOR; LMOR; MOR1; OPRM; M-OR-1 Accession Number: NM_000914 G coupling Gi
Functional Assay-Calcium Flux Assay
op-mu DAMGO Agonist DAMGO 120 DPDPE Measurement: Intracellular Ca2+ 100 80 Detection method: FLIPR Fluorimetry 60 Incubation 25℃ 40 (%) Activity 20 Agonist effect EC50: 3.6 nM 0 -20 -4 -2 0 2 4 6 Log [Compound] nM
op-mu CTOP Antagonist CTOP 120 Naltrindole hydrochloride Measurement: Intracellular Ca2+ 100 80 Detection method: FLIPR Fluorimetry 60 Incubation 25℃ 40 20 Inhibition (%) Inhibition Stimulant DAMGO: 20 nM 0 -20 Antagonist effect IC50: 62.3 nM -1 0 1 2 3 4 5 Log [Compound] nM
Radio ligand binding Assay
Ligand [3H]DAMGO op-mu 125 CTOP Ligand concentration 0.5 nM 100 Naltrindole DPDPE 75 Kd (nM) 0.3 nM DAMGO 50 Non specific naltrindole (1 µM) % Inhibition 25 Incubation 60 min/RT 0
Detection method Scintillation counting -4 -3 -2 -1 0 1 2 3 4 5 Log [Compound] nM Reference: DAMGO(IC50:1.7 nM)
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V1A (Arginine Vasopressin Receptor 1A)
Cell Line Name: CHO/V1A Species/Source: Human/Recombinant Gene Synonyms: AVPR1A; V1aR; AVPR1; AVPR; V1a Accession Number: NM_000706 G coupling Gq
Functional Assay-Calcium Flux Assay
V1A AVP Agonist [Arg8]Vasopressin acetate 120 Oxytocin Measurement: Intracellular Ca2+ 100 80 Detection method: FLIPR Fluorimetry 60
Incubation 25℃ 40 (%) Activity 20 Agonist effect EC50: 0.0034 nM 0 -20 -4 -3 -2 -1 0 1 2 3 4 Log [Compound] nM
Antagonist [β-Mercapto-β,β-
cyclopentamethylenepropi
onyl1, O-Et-Tyr2, Val4, V1A 120 [β -Mercapto-β β -cyclopentame Arg8]-Vasopressin 100 [d(CH2)5Tyr(Me)2]-AVP 80 Measurement: Intracellular Ca2+ 60 Detection method: FLIPR Fluorimetry 40 20 (%) Inhibition Incubation 25℃ 0 Stimulant [Arg8]Vasopressin acetate: -20 -2 -1 0 1 2 3 4 0.12 nM Log [Compound] nM
Antagonist effect IC50: 6.551 nM
Radio ligand binding Assay
V1A Ligand [3H]AVP 125 AVP Ligand concentration 0.3 nM 100 [d(CH2)5Tyr(Me)2]-AVP Oxytocin Kd (nM) 0.26 nM 75 Non specific AVP (1 µM) 50
Incubation 60 min/RT Inhibition % 25 Detection method Scintillation counting 0 Reference: [d(CH2)5,Tyr(Me)2]-AVP -4 -3 -2 -1 0 1 2 3 4 Log [Compound] nM (IC50:0.92 nM)
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