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Home Screening Services Screening Platform Model Catalogs |
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| 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 |
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0.07nM (Isoproterenol) |
N/A |
¦Â2-AR |
Calcium flux |
0.045nM (Isoproterenol) |
4.84nM (Propranol) |
¦Â3-AR |
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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 |
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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 |
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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 |
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mGLu3 |
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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 |
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K + |
hERG |
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