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Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
Shanghai Fudan-zhangjiang Bio-Pharmaceutical
 Home  Screening Services  Screening Platform  Model Catalogs
Currently more than 30 GPCR cell lines covering 11 GPCR families are available for screening, which are listed below.

Receptor family

Subtype

Assay

EC 50(agonist)

IC 50(agonist)

Serotonin

5-HT4R

cAMP

0.23 nM (5-HT)

N/A

Adrenergic

¦Á 1A AR

Calcium flux

7.47nM(Phenylephrine)

0.29nM (Tamsulosin)

¦Á 1BAR

Calcium flux

4.11nM (Phenylephrine)

6.33nM (Tamsulosin)

¦Á1D AR

Calcium flux

1.94nM (Phenylephrine)

N/A

¦Â1-AR

 

0.07nM (Isoproterenol)  

 N/A 

¦Â2-AR

Calcium flux

0.045nM (Isoproterenol)

4.84nM (Propranol)

¦Â3-AR

 

  15.7nM (Isoproterenol)

N/A  

Cannabinoid

CB1R

Calcium flux

2.91nM (CP55940)

17.97nM (Rimonabant)

Ligand-receptor binding

N/A

2.81 nM, Ki=0.77nM (Rimonabant)

CB2R

Calcium flux

8.19nM
(CP55940)

2.64 ¦ÌM (Rimonabant)

Ligand-receptor binding

N/A

0.81 ¦ÌM, Ki=0.12 ¦ÌM (Rimonabant)

Chemokine

CCR1

[ 35 S]GTP ¦Ã S binding

 

 

CCR2

Calcium flux

8.43 nM (MCP-1)

9.56 nM (TDXX1)

CCR3

[ 35 S]GTP ¦Ã S binding

3.11nM (Eotaxin)

N/A

CCR4

[ 35S]GTP ¦Ã S binding

7.18nM (MDC)

N/A

CCR5

Calcium flux

4.82nM (RANTES)

3.41nM(TD-0579)

[ 35S]GTP ¦Ã S binding

N/A

2.21nM(TD-0579)

CXCR1

[ 35S]GTP ¦Ã S binding

9.78nM (IL-8)

N/A

CXCR2

[ 35 S]GTP ¦Ã S binding

1nM (IL-8)

N/A

CXCR3

[ 35S]GTP ¦Ã S binding

7.47nM (IP-10)

N/A

CXCR4

Calcium flux

18.00nM (SDF-1)

25.26nM(T140)

[ 35S]GTP ¦Ã S binding

N/A

2.21nM(T140)

Dopamine

DR-D1

 

 

 

DR-D2

Calcium flux

6.3 nM (Dopamine)

N/A

DR-D5

Calcium flux

0.34nM(Dopamine)

N/A

Glucagon

GCGR

Calcium flux

27.1nM (Glucagon)

26.32nM ([des-His1,Glu9]-Glucagon)

GLP-1R

Calcium flux

1.07nM(GLP-1)

N/A

Luciferase- reporter gene

1.35nM(GLP-1)

N/A

Melanocortin

MCR3

Luciferase- reporter gene

14.78nM (¦Á-MSH)

N/A

MCR4

Luciferase- reporter gene

6.05nM (¦Á-MSH)

N/A

Melatonin

MT1R

Ligand-receptor binding

1.95nM, Ki=1.94nM (Melatonin)

N/A

MT2R

Ligand-receptor binding

4.16nM, Ki=4.14nM (Melatonin)

N/A

Metabotropic glutamate

mGLu2

 

 

 

mGLu3

 

 

 

Opioid

DOR

Calcium flux

4.0nM(DPDPE)

1.6nM (Naltrindole)

Ligand-receptor binding

N/A

1.7nM, Ki=0.8nM (Naltrindole)

MOR

Calcium flux

3.6nM(DAGO)

2.6nM (¦Â-Funaltrexamine)

KOR

Calcium flux

0.6nM(U50488)

13.5nM(Naloxone)

ION CHANNEL

 

 

 

 

K +

hERG

 

 

 

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