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Compile Data Set for Download or QSAR

Found 256 hits of ec50 data for polymerid = 49000764,8284   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50138784
PNG
((1R,2S,3R)-2-((S)-Amino-carboxy-methyl)-3-hydroxy-...)
Show SMILES N[C@@H]([C@H]1[C@@H](O)[C@@H]1C(O)=O)C(O)=O
Show InChI InChI=1S/C6H9NO5/c7-3(6(11)12)1-2(4(1)8)5(9)10/h1-4,8H,7H2,(H,9,10)(H,11,12)/t1-,2+,3-,4+/m0/s1
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n/an/an/an/a 10n/an/an/an/a



Lilly, SA

Curated by ChEMBL


Assay Description
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat nonneuronal cells


J Med Chem 47: 456-66 (2004)


Article DOI: 10.1021/jm030967o
BindingDB Entry DOI: 10.7270/Q2K936Z5
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50138783
PNG
(4-((S)-Amino-carboxy-methyl)-phthalic acid | 4-[am...)
Show SMILES N[C@H](C(O)=O)c1ccc(C(O)=O)c(c1)C(O)=O
Show InChI InChI=1S/C10H9NO6/c11-7(10(16)17)4-1-2-5(8(12)13)6(3-4)9(14)15/h1-3,7H,11H2,(H,12,13)(H,14,15)(H,16,17)/t7-/m0/s1
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n/an/an/an/a 23n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulati...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50138783
PNG
(4-((S)-Amino-carboxy-methyl)-phthalic acid | 4-[am...)
Show SMILES N[C@H](C(O)=O)c1ccc(C(O)=O)c(c1)C(O)=O
Show InChI InChI=1S/C10H9NO6/c11-7(10(16)17)4-1-2-5(8(12)13)6(3-4)9(14)15/h1-3,7H,11H2,(H,12,13)(H,14,15)(H,16,17)/t7-/m0/s1
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n/an/an/an/a 31n/an/an/an/a



Lilly, SA

Curated by ChEMBL


Assay Description
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat nonneuronal cells


J Med Chem 47: 456-66 (2004)


Article DOI: 10.1021/jm030967o
BindingDB Entry DOI: 10.7270/Q2K936Z5
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50138783
PNG
(4-((S)-Amino-carboxy-methyl)-phthalic acid | 4-[am...)
Show SMILES N[C@H](C(O)=O)c1ccc(C(O)=O)c(c1)C(O)=O
Show InChI InChI=1S/C10H9NO6/c11-7(10(16)17)4-1-2-5(8(12)13)6(3-4)9(14)15/h1-3,7H,11H2,(H,12,13)(H,14,15)(H,16,17)/t7-/m0/s1
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n/an/an/an/a 31n/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells


J Med Chem 61: 10040-10052 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01120
BindingDB Entry DOI: 10.7270/Q2SJ1Q0B
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50138783
PNG
(4-((S)-Amino-carboxy-methyl)-phthalic acid | 4-[am...)
Show SMILES N[C@H](C(O)=O)c1ccc(C(O)=O)c(c1)C(O)=O
Show InChI InChI=1S/C10H9NO6/c11-7(10(16)17)4-1-2-5(8(12)13)6(3-4)9(14)15/h1-3,7H,11H2,(H,12,13)(H,14,15)(H,16,17)/t7-/m0/s1
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n/an/an/an/a 44n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50220011
PNG
(CHEMBL243925 | L-(+)-2-amino-4-thiophosphonobutyri...)
Show SMILES N[C@@H](CCP(O)(O)=S)C(O)=O
Show InChI InChI=1S/C4H10NO4PS/c5-3(4(6)7)1-2-10(8,9)11/h3H,1-2,5H2,(H,6,7)(H2,8,9,11)/t3-/m0/s1
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n/an/an/an/a 54n/an/an/an/a



Université Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production


J Med Chem 50: 4656-64 (2007)


Article DOI: 10.1021/jm070400y
BindingDB Entry DOI: 10.7270/Q2XP74NQ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 60n/an/an/an/a



Lilly, SA

Curated by ChEMBL


Assay Description
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat nonneuronal cells


J Med Chem 47: 456-66 (2004)


Article DOI: 10.1021/jm030967o
BindingDB Entry DOI: 10.7270/Q2K936Z5
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 60n/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells


J Med Chem 61: 10040-10052 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01120
BindingDB Entry DOI: 10.7270/Q2SJ1Q0B
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 70n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay


J Med Chem 59: 914-24 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01333
BindingDB Entry DOI: 10.7270/Q2000408
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 110n/an/an/an/a



Univ. Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay


Bioorg Med Chem Lett 25: 2523-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.043
BindingDB Entry DOI: 10.7270/Q21Z464C
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50283487
PNG
(CHEMBL4162576)
Show SMILES Clc1ccc(Oc2ccc(NC(=O)c3ccccn3)cc2Cl)nc1
Show InChI InChI=1S/C17H11Cl2N3O2/c18-11-4-7-16(21-10-11)24-15-6-5-12(9-13(15)19)22-17(23)14-3-1-2-8-20-14/h1-10H,(H,22,23)
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n/an/an/an/a 125n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium ...


ACS Med Chem Lett 8: 1110-1115 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00317
BindingDB Entry DOI: 10.7270/Q2B85BN1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 128n/an/an/an/a



Université Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production


J Med Chem 50: 4656-64 (2007)


Article DOI: 10.1021/jm070400y
BindingDB Entry DOI: 10.7270/Q2XP74NQ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50552330
PNG
(CHEMBL4745982)
Show SMILES Cc1ccoc1C(=O)Nc1cc(C)c(cc1F)N1C(=O)c2ccccc2C1=O
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n/an/an/an/a 189n/an/an/an/a


TBA

Assay Description
Positive allosteric modulation of mGluR8 (unknown origin) by calcium mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127724
BindingDB Entry DOI: 10.7270/Q2WS8XWG
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50004881
PNG
((RS) PPG | Amino-(4-phosphono-phenyl)-acetic acid ...)
Show SMILES NC(C(O)=O)c1ccc(cc1)P(O)(O)=O
Show InChI InChI=1S/C8H10NO5P/c9-7(8(10)11)5-1-3-6(4-2-5)15(12,13)14/h1-4,7H,9H2,(H,10,11)(H2,12,13,14)
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n/an/an/an/a 210n/an/an/an/a



Lilly, SA

Curated by ChEMBL


Assay Description
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat nonneuronal cells


J Med Chem 47: 456-66 (2004)


Article DOI: 10.1021/jm030967o
BindingDB Entry DOI: 10.7270/Q2K936Z5
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 240n/an/an/an/a



Universite Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular ...


J Med Chem 53: 2797-813 (2010)


Article DOI: 10.1021/jm901523t
BindingDB Entry DOI: 10.7270/Q28W3F7Q
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM82006
PNG
(D-AP4 | D-APB | US9212196, L-AP4)
Show SMILES N[C@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m1/s1
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n/an/an/an/a 290n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 290n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulati...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 300n/an/an/an/a



Universite Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular ...


J Med Chem 53: 2797-813 (2010)


Article DOI: 10.1021/jm901523t
BindingDB Entry DOI: 10.7270/Q28W3F7Q
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255396
PNG
(CHEMBL4067923)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(o1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C9H13N2O8P/c10-5(8(12)13)3-4-20(17,18)9(14)6-1-2-7(19-6)11(15)16/h1-2,5,9,14H,3-4,10H2,(H,12,13)(H,17,18)/t5-,9?/m0/s1
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Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50217031
PNG
((1S,2R)-1-amino-2-phosphonomethylcyclopropane-carb...)
Show SMILES N[C@]1(C[C@H]1CP(O)(O)=O)C(O)=O
Show InChI InChI=1S/C5H10NO5P/c6-5(4(7)8)1-3(5)2-12(9,10)11/h3H,1-2,6H2,(H,7,8)(H2,9,10,11)/t3-,5-/m0/s1
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n/an/an/an/a 340n/an/an/an/a



University Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production


J Med Chem 50: 3585-95 (2007)


Article DOI: 10.1021/jm070262c
BindingDB Entry DOI: 10.7270/Q23R0SMQ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255292
PNG
(CHEMBL4061423)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1csc(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C9H13N2O7PS/c10-6(8(12)13)1-2-19(17,18)9(14)5-3-7(11(15)16)20-4-5/h3-4,6,9,14H,1-2,10H2,(H,12,13)(H,17,18)/t6-,9?/m0/s1
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n/an/an/an/a 380n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50034504
PNG
((1S,2S)-2-((S)-Amino-carboxy-methyl)-cyclopropanec...)
Show SMILES N[C@@H]([C@H]1C[C@@H]1C(O)=O)C(O)=O
Show InChI InChI=1S/C6H9NO4/c7-4(6(10)11)2-1-3(2)5(8)9/h2-4H,1,7H2,(H,8,9)(H,10,11)/t2-,3-,4-/m0/s1
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n/an/an/an/a 400n/an/an/an/a



Lilly, SA

Curated by ChEMBL


Assay Description
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat nonneuronal cells


J Med Chem 47: 456-66 (2004)


Article DOI: 10.1021/jm030967o
BindingDB Entry DOI: 10.7270/Q2K936Z5
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255406
PNG
(CHEMBL4088782)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(cc1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H15N2O7P/c12-9(10(14)15)5-6-21(19,20)11(16)7-1-3-8(4-2-7)13(17)18/h1-4,9,11,16H,5-6,12H2,(H,14,15)(H,19,20)/t9-,11?/m0/s1
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n/an/an/an/a 490n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50283478
PNG
(CHEMBL4164141)
Show SMILES COc1cc(F)c(cc1Cl)-c1c(C)nn2c(cc(C)nc12)C(F)(F)F |(37.17,-44.14,;38.18,-42.98,;37.7,-41.52,;38.73,-40.37,;38.23,-38.91,;39.26,-37.76,;36.73,-38.6,;35.71,-39.75,;36.19,-41.21,;35.16,-42.36,;36.25,-37.14,;37.15,-35.9,;38.69,-35.89,;36.24,-34.66,;34.78,-35.14,;33.45,-34.37,;32.12,-35.14,;32.12,-36.68,;30.79,-37.46,;33.45,-37.45,;34.79,-36.67,;33.45,-32.83,;34.79,-32.05,;32.12,-32.05,;33.44,-31.28,)|
Show InChI InChI=1S/C16H12ClF4N3O/c1-7-4-13(16(19,20)21)24-15(22-7)14(8(2)23-24)9-5-10(17)12(25-3)6-11(9)18/h4-6H,1-3H3
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n/an/an/an/a 490n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium ...


ACS Med Chem Lett 8: 1110-1115 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00317
BindingDB Entry DOI: 10.7270/Q2B85BN1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50283478
PNG
(CHEMBL4164141)
Show SMILES COc1cc(F)c(cc1Cl)-c1c(C)nn2c(cc(C)nc12)C(F)(F)F |(37.17,-44.14,;38.18,-42.98,;37.7,-41.52,;38.73,-40.37,;38.23,-38.91,;39.26,-37.76,;36.73,-38.6,;35.71,-39.75,;36.19,-41.21,;35.16,-42.36,;36.25,-37.14,;37.15,-35.9,;38.69,-35.89,;36.24,-34.66,;34.78,-35.14,;33.45,-34.37,;32.12,-35.14,;32.12,-36.68,;30.79,-37.46,;33.45,-37.45,;34.79,-36.67,;33.45,-32.83,;34.79,-32.05,;32.12,-32.05,;33.44,-31.28,)|
Show InChI InChI=1S/C16H12ClF4N3O/c1-7-4-13(16(19,20)21)24-15(22-7)14(8(2)23-24)9-5-10(17)12(25-3)6-11(9)18/h4-6H,1-3H3
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n/an/an/an/a 490n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium ...


ACS Med Chem Lett 8: 1110-1115 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00317
BindingDB Entry DOI: 10.7270/Q2B85BN1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255292
PNG
(CHEMBL4061423)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1csc(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C9H13N2O7PS/c10-6(8(12)13)1-2-19(17,18)9(14)5-3-7(11(15)16)20-4-5/h3-4,6,9,14H,1-2,10H2,(H,12,13)(H,17,18)/t6-,9?/m0/s1
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n/an/an/an/a 510n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulati...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255406
PNG
(CHEMBL4088782)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(cc1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H15N2O7P/c12-9(10(14)15)5-6-21(19,20)11(16)7-1-3-8(4-2-7)13(17)18/h1-4,9,11,16H,5-6,12H2,(H,14,15)(H,19,20)/t9-,11?/m0/s1
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n/an/an/an/a 530n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 560n/an/an/an/a



University Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production


J Med Chem 50: 3585-95 (2007)


Article DOI: 10.1021/jm070262c
BindingDB Entry DOI: 10.7270/Q23R0SMQ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255390
PNG
(CHEMBL4091029)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(F)c(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H14FN2O7P/c12-7-2-1-6(5-9(7)14(18)19)11(17)22(20,21)4-3-8(13)10(15)16/h1-2,5,8,11,17H,3-4,13H2,(H,15,16)(H,20,21)/t8-,11?/m0/s1
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n/an/an/an/a 660n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50159148
PNG
(CHEMBL3786667)
Show SMILES [H][C@]1(C[C@]1(C[C@H](N)C(O)=O)C(O)=O)C(O)=O |r|
Show InChI InChI=1S/C8H11NO6/c9-4(6(12)13)2-8(7(14)15)1-3(8)5(10)11/h3-4H,1-2,9H2,(H,10,11)(H,12,13)(H,14,15)/t3-,4-,8+/m0/s1
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n/an/an/an/a 680n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay


J Med Chem 59: 914-24 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01333
BindingDB Entry DOI: 10.7270/Q2000408
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50283481
PNG
(CHEMBL4160675)
Show SMILES CCc1nn2c(cc(C)nc2c1-c1cc(F)c(OC(F)F)cc1F)C(F)(F)F |(25.69,-48.74,;24.92,-50.08,;23.38,-50.09,;22.48,-48.85,;21.02,-49.33,;19.69,-48.56,;18.36,-49.33,;18.36,-50.87,;17.03,-51.64,;19.69,-51.64,;21.03,-50.86,;22.49,-51.33,;22.97,-52.79,;21.94,-53.94,;22.43,-55.4,;21.4,-56.55,;23.94,-55.71,;24.42,-57.17,;23.4,-58.33,;23.88,-59.79,;21.89,-58.02,;24.96,-54.56,;24.47,-53.1,;25.5,-51.95,;19.69,-47.02,;21.03,-46.24,;18.36,-46.24,;19.68,-45.48,)|
Show InChI InChI=1S/C17H12F7N3O/c1-3-11-14(8-5-10(19)12(6-9(8)18)28-16(20)21)15-25-7(2)4-13(17(22,23)24)27(15)26-11/h4-6,16H,3H2,1-2H3
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n/an/an/an/a 890n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium ...


ACS Med Chem Lett 8: 1110-1115 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00317
BindingDB Entry DOI: 10.7270/Q2B85BN1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50283481
PNG
(CHEMBL4160675)
Show SMILES CCc1nn2c(cc(C)nc2c1-c1cc(F)c(OC(F)F)cc1F)C(F)(F)F |(25.69,-48.74,;24.92,-50.08,;23.38,-50.09,;22.48,-48.85,;21.02,-49.33,;19.69,-48.56,;18.36,-49.33,;18.36,-50.87,;17.03,-51.64,;19.69,-51.64,;21.03,-50.86,;22.49,-51.33,;22.97,-52.79,;21.94,-53.94,;22.43,-55.4,;21.4,-56.55,;23.94,-55.71,;24.42,-57.17,;23.4,-58.33,;23.88,-59.79,;21.89,-58.02,;24.96,-54.56,;24.47,-53.1,;25.5,-51.95,;19.69,-47.02,;21.03,-46.24,;18.36,-46.24,;19.68,-45.48,)|
Show InChI InChI=1S/C17H12F7N3O/c1-3-11-14(8-5-10(19)12(6-9(8)18)28-16(20)21)15-25-7(2)4-13(17(22,23)24)27(15)26-11/h4-6,16H,3H2,1-2H3
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n/an/an/an/a 891n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium ...


ACS Med Chem Lett 8: 1110-1115 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00317
BindingDB Entry DOI: 10.7270/Q2B85BN1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50283491
PNG
(CHEMBL1585091)
Show SMILES COC(=O)c1ccc(cc1)-n1c(C)cc(C(=O)CSc2ccc(NC(C)=O)cc2)c1C
Show InChI InChI=1S/C24H24N2O4S/c1-15-13-22(16(2)26(15)20-9-5-18(6-10-20)24(29)30-4)23(28)14-31-21-11-7-19(8-12-21)25-17(3)27/h5-13H,14H2,1-4H3,(H,25,27)
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n/an/an/an/a 900n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium ...


ACS Med Chem Lett 8: 1110-1115 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00317
BindingDB Entry DOI: 10.7270/Q2B85BN1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50314794
PNG
((3S)-2-[((3-Amino-3-carboxy)propyl)(hydroxy)phosph...)
Show SMILES N[C@@H](CCP(O)(=O)CC(O)=O)C(O)=O |r|
Show InChI InChI=1S/C6H12NO6P/c7-4(6(10)11)1-2-14(12,13)3-5(8)9/h4H,1-3,7H2,(H,8,9)(H,10,11)(H,12,13)/t4-/m0/s1
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n/an/an/an/a 910n/an/an/an/a



Universite Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular ...


J Med Chem 53: 2797-813 (2010)


Article DOI: 10.1021/jm901523t
BindingDB Entry DOI: 10.7270/Q28W3F7Q
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255415
PNG
(CHEMBL4078629)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(c(c1)C(F)(F)F)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C12H14F3N2O7P/c13-12(14,15)7-5-6(1-2-9(7)17(21)22)11(20)25(23,24)4-3-8(16)10(18)19/h1-2,5,8,11,20H,3-4,16H2,(H,18,19)(H,23,24)/t8-,11?/m0/s1
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n/an/an/an/a 980n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255336
PNG
(CHEMBL4064187)
Show SMILES N[C@@H](CCP(O)(=O)Cc1cccc(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H15N2O6P/c12-10(11(14)15)4-5-20(18,19)7-8-2-1-3-9(6-8)13(16)17/h1-3,6,10H,4-5,7,12H2,(H,14,15)(H,18,19)/t10-/m0/s1
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n/an/an/an/a 1.00E+3n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50601004
PNG
(CHEMBL5202739)
Show SMILES Fc1ccc(N2CCN(CC2)C(=O)c2cnc3n(CC4CC4)ncc3c2C(F)(F)F)c(F)c1
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n/an/an/an/a>1.00E+3n/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00593
BindingDB Entry DOI: 10.7270/Q2FB571B
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255388
PNG
(CHEMBL4093492)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1cccc(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H15N2O7P/c12-9(10(14)15)4-5-21(19,20)11(16)7-2-1-3-8(6-7)13(17)18/h1-3,6,9,11,16H,4-5,12H2,(H,14,15)(H,19,20)/t9-,11?/m0/s1
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n/an/an/an/a 1.20E+3n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50116515
PNG
(CHEMBL3609729)
Show SMILES Cc1sc(Nc2nccc(C)n2)nc1-c1cn[nH]c1
Show InChI InChI=1S/C12H12N6S/c1-7-3-4-13-11(16-7)18-12-17-10(8(2)19-12)9-5-14-15-6-9/h3-6H,1-2H3,(H,14,15)(H,13,16,17,18)
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n/an/an/an/a 1.20E+3n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium ...


ACS Med Chem Lett 8: 1110-1115 (2017)


Article DOI: 10.1021/acsmedchemlett.7b00317
BindingDB Entry DOI: 10.7270/Q2B85BN1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM196930
PNG
(US9212196, Derivative 26)
Show SMILES N[C@H](CCP(O)(=O)C(O)c1ccc(SCC(O)=O)cc1)C(O)=O |r|
Show InChI InChI=1S/C13H18NO7PS/c14-10(12(17)18)5-6-22(20,21)13(19)8-1-3-9(4-2-8)23-7-11(15)16/h1-4,10,13,19H,5-7,14H2,(H,15,16)(H,17,18)(H,20,21)/t10-,13?/m1/s1
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n/an/an/an/a 1.23E+3n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255389
PNG
(CHEMBL4072781)
Show SMILES N[C@@H](CCP(O)(=O)[C@H](O)c1cccc(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H15N2O7P/c12-9(10(14)15)4-5-21(19,20)11(16)7-2-1-3-8(6-7)13(17)18/h1-3,6,9,11,16H,4-5,12H2,(H,14,15)(H,19,20)/t9-,11-/m0/s1
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n/an/an/an/a 1.25E+3n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50088290
PNG
(CHEMBL3427499)
Show SMILES NC1(CC1(F)CP(O)(O)=O)C(O)=O
Show InChI InChI=1S/C5H9FNO5P/c6-4(2-13(10,11)12)1-5(4,7)3(8)9/h1-2,7H2,(H,8,9)(H2,10,11,12)
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n/an/an/an/a 1.25E+3n/an/an/an/a



Univ. Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay


Bioorg Med Chem Lett 25: 2523-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.043
BindingDB Entry DOI: 10.7270/Q21Z464C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255390
PNG
(CHEMBL4091029)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(F)c(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H14FN2O7P/c12-7-2-1-6(5-9(7)14(18)19)11(17)22(20,21)4-3-8(13)10(15)16/h1-2,5,8,11,17H,3-4,13H2,(H,15,16)(H,20,21)/t8-,11?/m0/s1
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n/an/an/an/a 1.30E+3n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255437
PNG
(CHEMBL4085750)
Show SMILES N[C@@H](CCP(O)(=O)[C@@H](O)c1cccc(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H15N2O7P/c12-9(10(14)15)4-5-21(19,20)11(16)7-2-1-3-8(6-7)13(17)18/h1-3,6,9,11,16H,4-5,12H2,(H,14,15)(H,19,20)/t9-,11+/m0/s1
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n/an/an/an/a 1.30E+3n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM50138781
PNG
((1S,2S,3R)-2-((S)-Amino-carboxy-methyl)-3-methyl-c...)
Show SMILES C[C@@H]1[C@H]([C@H](N)C(O)=O)[C@H]1C(O)=O
Show InChI InChI=1S/C7H11NO4/c1-2-3(4(2)6(9)10)5(8)7(11)12/h2-5H,8H2,1H3,(H,9,10)(H,11,12)/t2-,3+,4+,5+/m1/s1
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n/an/an/an/a 1.32E+3n/an/an/an/a



Lilly, SA

Curated by ChEMBL


Assay Description
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat nonneuronal cells


J Med Chem 47: 456-66 (2004)


Article DOI: 10.1021/jm030967o
BindingDB Entry DOI: 10.7270/Q2K936Z5
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255388
PNG
(CHEMBL4093492)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1cccc(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C11H15N2O7P/c12-9(10(14)15)4-5-21(19,20)11(16)7-2-1-3-8(6-7)13(17)18/h1-3,6,9,11,16H,4-5,12H2,(H,14,15)(H,19,20)/t9-,11?/m0/s1
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n/an/an/an/a 1.50E+3n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulati...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50255337
PNG
(CHEMBL4063142)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(c(c1)[N+]([O-])=O)C(F)(F)F)C(O)=O |r|
Show InChI InChI=1S/C12H14F3N2O7P/c13-12(14,15)7-2-1-6(5-9(7)17(21)22)11(20)25(23,24)4-3-8(16)10(18)19/h1-2,5,8,11,20H,3-4,16H2,(H,18,19)(H,23,24)/t8-,11?/m0/s1
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n/an/an/an/a 1.54E+3n/an/an/an/a



Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques , CNRS UMR 8601, Université Paris Descartes, Sorbonne Paris Cité , 45 rue des Saints-Pères , 75270 Paris Cedex 06 , France.

Curated by ChEMBL


Assay Description
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium...


J Med Chem 61: 1969-1989 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01438
BindingDB Entry DOI: 10.7270/Q2DZ0BR0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50434134
PNG
(CHEMBL2381641)
Show SMILES N[C@]1(CC(=C)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O |r|
Show InChI InChI=1S/C9H11NO4/c1-3-2-9(10,8(13)14)6-4(3)5(6)7(11)12/h4-6H,1-2,10H2,(H,11,12)(H,13,14)/t4-,5-,6-,9-/m0/s1
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n/an/an/an/a 1.59E+3n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay


J Med Chem 56: 4442-55 (2013)


Article DOI: 10.1021/jm4000165
BindingDB Entry DOI: 10.7270/Q20003G4
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Rattus norvegicus (Rat))
BDBM196928
PNG
(US9212196, Derivative 24)
Show SMILES N[C@H](CCP(O)(=O)C(O)c1ccc(OCC(O)=O)c(c1)[N+]([O-])=O)C(O)=O |r|
Show InChI InChI=1S/C13H17N2O10P/c14-8(12(18)19)3-4-26(23,24)13(20)7-1-2-10(25-6-11(16)17)9(5-7)15(21)22/h1-2,5,8,13,20H,3-4,6,14H2,(H,16,17)(H,18,19)(H,23,24)/t8-,13?/m1/s1
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n/an/an/an/a 1.59E+3n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
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