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Compile Data Set for Download or QSAR

Found 50 hits of ec50 data for polymerid = 49000764,50002505   
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


(Mus musculus)
BDBM17657
PNG
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)
Show SMILES N[C@@H](CCC(O)=O)C(O)=O
Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1
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n/an/an/an/a 22n/an/an/an/a



CNS Research

Curated by ChEMBL


Assay Description
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse


J Med Chem 38: 1417-26 (1995)


Article DOI: 10.1021/jm00009a001
BindingDB Entry DOI: 10.7270/Q20R9Q1R
More data for this
Ligand-Target Pair
GRM8


(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


(Mus musculus)
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O
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 400n/an/an/an/a



CNS Research

Curated by ChEMBL


Assay Description
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse


J Med Chem 38: 1417-26 (1995)


Article DOI: 10.1021/jm00009a001
BindingDB Entry DOI: 10.7270/Q20R9Q1R
More data for this
Ligand-Target Pair
GRM8


(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
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
GRM8


(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
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
GRM8


(HUMAN)
BDBM50074749
PNG
((1R,4R,5S,6R)-4-Amino-2-oxa-bicyclo[3.1.0]hexane-4...)
Show SMILES N[C@]1(CO[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H9NO5/c8-7(6(11)12)1-13-4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1
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n/an/an/an/a 1.69E+3n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8


J Med Chem 42: 1027-40 (1999)


Article DOI: 10.1021/jm980616n
BindingDB Entry DOI: 10.7270/Q2WM1CKF
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50074749
PNG
((1R,4R,5S,6R)-4-Amino-2-oxa-bicyclo[3.1.0]hexane-4...)
Show SMILES N[C@]1(CO[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H9NO5/c8-7(6(11)12)1-13-4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1
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n/an/an/an/a 1.69E+3n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells


J Med Chem 50: 233-40 (2007)


Article DOI: 10.1021/jm060917u
BindingDB Entry DOI: 10.7270/Q21Z442N
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50217030
PNG
((1S,2S)-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+/m1/s1
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n/an/an/an/a 2.15E+3n/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
GRM8


(HUMAN)
BDBM50202406
PNG
((+)-(1R,2R,4S,5S,6S)-4-amino-2-thiabicyclo[3.1.0]h...)
Show SMILES N[C@]1(CS(=O)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H9NO5S/c8-7(6(11)12)1-14(13)4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+,14?/m1/s1
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n/an/an/an/a 3.07E+3n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells


J Med Chem 50: 233-40 (2007)


Article DOI: 10.1021/jm060917u
BindingDB Entry DOI: 10.7270/Q21Z442N
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50434137
PNG
(CHEMBL2381649)
Show SMILES CC(=O)N[C@H]1C[C@](N)([C@H]2[C@@H]1[C@@H]2C(O)=O)C(O)=O
Show InChI InChI=1S/C10H14N2O5/c1-3(13)12-4-2-10(11,9(16)17)7-5(4)6(7)8(14)15/h4-7H,2,11H2,1H3,(H,12,13)(H,14,15)(H,16,17)/t4-,5-,6-,7-,10-/m0/s1
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n/an/an/an/a 4.30E+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
GRM8


(HUMAN)
BDBM50089516
PNG
((1R,2S)-1-amino-2-(phosphonomethyl)cyclopropanecar...)
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-/m1/s1
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n/an/an/an/a 6.51E+3n/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
GRM8


(HUMAN)
BDBM50434136
PNG
(CHEMBL2381640)
Show SMILES N[C@]1(CC(=O)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H9NO5/c9-8(7(13)14)1-2(10)3-4(5(3)8)6(11)12/h3-5H,1,9H2,(H,11,12)(H,13,14)/t3-,4-,5-,8-/m0/s1
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n/an/an/an/a 6.53E+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
GRM8


(HUMAN)
BDBM50074750
PNG
((1R,4S,5S,6S)-4-amino-2-thia-bicyclo[3.1.0]hexane-...)
Show SMILES N[C@]1(CS[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H9NO4S/c8-7(6(11)12)1-13-4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1
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n/an/an/an/a 7.34E+3n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells


J Med Chem 50: 233-40 (2007)


Article DOI: 10.1021/jm060917u
BindingDB Entry DOI: 10.7270/Q21Z442N
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50074750
PNG
((1R,4S,5S,6S)-4-amino-2-thia-bicyclo[3.1.0]hexane-...)
Show SMILES N[C@]1(CS[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H9NO4S/c8-7(6(11)12)1-13-4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1
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n/an/an/an/a 7.34E+3n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8


J Med Chem 42: 1027-40 (1999)


Article DOI: 10.1021/jm980616n
BindingDB Entry DOI: 10.7270/Q2WM1CKF
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50132507
PNG
(CHEMBL3633943)
Show SMILES CC(=O)N1CCCn2nc(COc3ccccc3)cc12
Show InChI InChI=1S/C15H17N3O2/c1-12(19)17-8-5-9-18-15(17)10-13(16-18)11-20-14-6-3-2-4-7-14/h2-4,6-7,10H,5,8-9,11H2,1H3
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n/an/an/an/a>1.00E+4n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Effective concentration against human PPAR-alpha in Gal4 transactivation assay


Bioorg Med Chem Lett 25: 5115-20 (2015)


Article DOI: 10.1016/j.bmcl.2015.10.009
BindingDB Entry DOI: 10.7270/Q2445P80
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50064444
PNG
(CHEMBL3401195)
Show SMILES Fc1ccc(cc1)N1CCc2nc(COc3ccccc3)cn2C1=O
Show InChI InChI=1S/C19H16FN3O2/c20-14-6-8-16(9-7-14)22-11-10-18-21-15(12-23(18)19(22)24)13-25-17-4-2-1-3-5-17/h1-9,12H,10-11,13H2
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n/an/an/an/a>1.00E+4n/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation at mGluR8 (unknown origin)


Bioorg Med Chem Lett 25: 1310-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.01.038
BindingDB Entry DOI: 10.7270/Q2057HNQ
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50064463
PNG
(CHEMBL3401177)
Show SMILES Fc1ccc(cc1)-n1ccc2nc(COc3ccccc3)cn2c1=O
Show InChI InChI=1S/C19H14FN3O2/c20-14-6-8-16(9-7-14)22-11-10-18-21-15(12-23(18)19(22)24)13-25-17-4-2-1-3-5-17/h1-12H,13H2
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n/an/an/an/a>1.00E+4n/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation at mGluR8 (unknown origin)


Bioorg Med Chem Lett 25: 1310-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.01.038
BindingDB Entry DOI: 10.7270/Q2057HNQ
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50392432
PNG
(CHEMBL2151817)
Show SMILES C[C@@H](NC(=O)c1ccc(OCc2cccc(F)c2)nc1)C(C)(C)C
Show InChI InChI=1S/C19H23FN2O2/c1-13(19(2,3)4)22-18(23)15-8-9-17(21-11-15)24-12-14-6-5-7-16(20)10-14/h5-11,13H,12H2,1-4H3,(H,22,23)/t13-/m1/s1
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n/an/an/an/a>1.00E+4n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulation of mGluR8


Bioorg Med Chem Lett 22: 6481-5 (2012)


Article DOI: 10.1016/j.bmcl.2012.08.043
BindingDB Entry DOI: 10.7270/Q2KD200S
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50440205
PNG
(CHEMBL2426621)
Show SMILES O=C1CCCc2nc(sc12)C#Cc1ccccc1
Show InChI InChI=1S/C15H11NOS/c17-13-8-4-7-12-15(13)18-14(16-12)10-9-11-5-2-1-3-6-11/h1-3,5-6H,4,7-8H2
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Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human mGlu8 receptor expressed in HEK293 cells by fluorescent Ca2+ assay


J Med Chem 56: 7243-59 (2013)


Article DOI: 10.1021/jm400650w
BindingDB Entry DOI: 10.7270/Q2F19152
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50337525
PNG
(7-(phenoxymethyl)chroman-4-one | CHEMBL1682820)
Show SMILES O=C1CCOc2cc(COc3ccccc3)ccc12
Show InChI InChI=1S/C16H14O3/c17-15-8-9-18-16-10-12(6-7-14(15)16)11-19-13-4-2-1-3-5-13/h1-7,10H,8-9,11H2
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Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human mGlu8 receptor expressed in HEK293 cells by fluorescent Ca2+ assay


J Med Chem 56: 7243-59 (2013)


Article DOI: 10.1021/jm400650w
BindingDB Entry DOI: 10.7270/Q2F19152
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM49388
PNG
(7-(benzyloxy)-2,3-dihydro-4H-chromen-4-one | 7-ben...)
Show SMILES O=C1CCOc2cc(OCc3ccccc3)ccc12
Show InChI InChI=1S/C16H14O3/c17-15-8-9-18-16-10-13(6-7-14(15)16)19-11-12-4-2-1-3-5-12/h1-7,10H,8-9,11H2
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n/an/an/an/a>1.00E+4n/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human mGlu8 receptor expressed in HEK293 cells by fluorescent Ca2+ assay


J Med Chem 56: 7243-59 (2013)


Article DOI: 10.1021/jm400650w
BindingDB Entry DOI: 10.7270/Q2F19152
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50337526
PNG
(4-oxochroman-7-yl benzoate | CHEMBL1682821)
Show SMILES O=C(Oc1ccc2C(=O)CCOc2c1)c1ccccc1
Show InChI InChI=1S/C16H12O4/c17-14-8-9-19-15-10-12(6-7-13(14)15)20-16(18)11-4-2-1-3-5-11/h1-7,10H,8-9H2
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n/an/an/an/a>1.00E+4n/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human mGlu8 receptor expressed in HEK293 cells by fluorescent Ca2+ assay


J Med Chem 56: 7243-59 (2013)


Article DOI: 10.1021/jm400650w
BindingDB Entry DOI: 10.7270/Q2F19152
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50440185
PNG
(CHEMBL2426616)
Show SMILES CN1CCc2nc(COc3ccccc3)sc2C1=O
Show InChI InChI=1S/C14H14N2O2S/c1-16-8-7-11-13(14(16)17)19-12(15-11)9-18-10-5-3-2-4-6-10/h2-6H,7-9H2,1H3
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n/an/an/an/a>1.00E+4n/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human mGlu8 receptor expressed in HEK293 cells by fluorescent Ca2+ assay


J Med Chem 56: 7243-59 (2013)


Article DOI: 10.1021/jm400650w
BindingDB Entry DOI: 10.7270/Q2F19152
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50134466
PNG
(CHEMBL3747116)
Show SMILES Fc1ccc(cc1)N1CCn2nc(OCc3ccccc3)cc2C1=O
Show InChI InChI=1S/C19H16FN3O2/c20-15-6-8-16(9-7-15)22-10-11-23-17(19(22)24)12-18(21-23)25-13-14-4-2-1-3-5-14/h1-9,12H,10-11,13H2
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n/an/an/an/a>1.00E+4n/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human mGlu8 receptor expressed in HEK293 cells assessed as calcium mobilization by fluorescence analysis


Bioorg Med Chem Lett 26: 429-34 (2016)


Article DOI: 10.1016/j.bmcl.2015.11.098
BindingDB Entry DOI: 10.7270/Q2SJ1NGS
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50134443
PNG
(CHEMBL3746457)
Show SMILES Fc1ccc(nc1)N1CCn2nc(COc3ccccc3)cc2C1=O
Show InChI InChI=1S/C18H15FN4O2/c19-13-6-7-17(20-11-13)22-8-9-23-16(18(22)24)10-14(21-23)12-25-15-4-2-1-3-5-15/h1-7,10-11H,8-9,12H2
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n/an/an/an/a>1.00E+4n/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human mGlu8 receptor expressed in HEK293 cells assessed as calcium mobilization by fluorescence analysis


Bioorg Med Chem Lett 26: 429-34 (2016)


Article DOI: 10.1016/j.bmcl.2015.11.098
BindingDB Entry DOI: 10.7270/Q2SJ1NGS
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50121643
PNG
(CHEMBL3616847)
Show SMILES N[C@]1(C[C@@H](Sc2nnc[nH]2)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C10H12N4O4S/c11-10(8(17)18)1-3(19-9-12-2-13-14-9)4-5(6(4)10)7(15)16/h2-6H,1,11H2,(H,15,16)(H,17,18)(H,12,13,14)/t3-,4+,5+,6+,10+/m1/s1
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n/an/an/an/a 1.01E+4n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 h...


J Med Chem 58: 7526-48 (2015)


Article DOI: 10.1021/acs.jmedchem.5b01124
BindingDB Entry DOI: 10.7270/Q29S1ST0
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50056272
PNG
((1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dic...)
Show SMILES N[C@]1(CC[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1
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n/an/an/an/a 1.15E+4n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells


J Med Chem 50: 233-40 (2007)


Article DOI: 10.1021/jm060917u
BindingDB Entry DOI: 10.7270/Q21Z442N
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50056272
PNG
((1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dic...)
Show SMILES N[C@]1(CC[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1
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n/an/an/an/a 1.15E+4n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8


J Med Chem 42: 1027-40 (1999)


Article DOI: 10.1021/jm980616n
BindingDB Entry DOI: 10.7270/Q2WM1CKF
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50434135
PNG
(CHEMBL2381652)
Show SMILES N[C@]1(C[C@@H](F)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H10FNO4/c9-2-1-8(10,7(13)14)5-3(2)4(5)6(11)12/h2-5H,1,10H2,(H,11,12)(H,13,14)/t2-,3+,4+,5+,8+/m1/s1
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n/an/an/an/a 1.15E+4n/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
GRM8


(HUMAN)
BDBM50434130
PNG
(CHEMBL2381645)
Show SMILES N[C@]1(C[C@H](N=[N+]=[N-])[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H10N4O4/c9-8(7(15)16)1-2(11-12-10)3-4(5(3)8)6(13)14/h2-5H,1,9H2,(H,13,14)(H,15,16)/t2-,3-,4-,5-,8-/m0/s1
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n/an/an/an/a 1.20E+4n/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
GRM8


(HUMAN)
BDBM50434131
PNG
(CHEMBL2381644)
Show SMILES N[C@]1(C[C@@H](N=[N+]=[N-])[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H10N4O4/c9-8(7(15)16)1-2(11-12-10)3-4(5(3)8)6(13)14/h2-5H,1,9H2,(H,13,14)(H,15,16)/t2-,3+,4+,5+,8+/m1/s1
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n/an/an/an/a 1.24E+4n/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
GRM8


(HUMAN)
BDBM50056272
PNG
((1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dic...)
Show SMILES N[C@]1(CC[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50434140
PNG
(CHEMBL2381648)
Show SMILES CC(=O)N[C@@H]1C[C@](N)([C@H]2[C@@H]1[C@@H]2C(O)=O)C(O)=O
Show InChI InChI=1S/C10H14N2O5/c1-3(13)12-4-2-10(11,9(16)17)7-5(4)6(7)8(14)15/h4-7H,2,11H2,1H3,(H,12,13)(H,14,15)(H,16,17)/t4-,5+,6+,7+,10+/m1/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50121643
PNG
(CHEMBL3616847)
Show SMILES N[C@]1(C[C@@H](Sc2nnc[nH]2)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C10H12N4O4S/c11-10(8(17)18)1-3(19-9-12-2-13-14-9)4-5(6(4)10)7(15)16/h2-6H,1,11H2,(H,15,16)(H,17,18)(H,12,13,14)/t3-,4+,5+,6+,10+/m1/s1
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n/an/an/an/a>2.50E+4n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assa...


J Med Chem 58: 7526-48 (2015)


Article DOI: 10.1021/acs.jmedchem.5b01124
BindingDB Entry DOI: 10.7270/Q29S1ST0
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50167032
PNG
((1S,2S,4R,5R,6S)-2-Amino-4-methyl-bicyclo[3.1.0]he...)
Show SMILES C[C@@H]1C[C@](N)([C@H]2[C@@H]1[C@@H]2C(O)=O)C(O)=O
Show InChI InChI=1S/C9H13NO4/c1-3-2-9(10,8(13)14)6-4(3)5(6)7(11)12/h3-6H,2,10H2,1H3,(H,11,12)(H,13,14)/t3-,4+,5+,6+,9+/m1/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50167034
PNG
((1S,2S,4S,5R,6S)-2-Amino-4-methyl-bicyclo[3.1.0]he...)
Show SMILES C[C@H]1C[C@](N)([C@H]2[C@@H]1[C@@H]2C(O)=O)C(O)=O
Show InChI InChI=1S/C9H13NO4/c1-3-2-9(10,8(13)14)6-4(3)5(6)7(11)12/h3-6H,2,10H2,1H3,(H,11,12)(H,13,14)/t3-,4-,5-,6-,9-/m0/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50434132
PNG
(CHEMBL2381642)
Show SMILES N[C@]1(C[C@@H](O)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H11NO5/c9-8(7(13)14)1-2(10)3-4(5(3)8)6(11)12/h2-5,10H,1,9H2,(H,11,12)(H,13,14)/t2-,3+,4+,5+,8+/m1/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50434133
PNG
(CHEMBL2381643)
Show SMILES N[C@]1(C[C@H](O)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C8H11NO5/c9-8(7(13)14)1-2(10)3-4(5(3)8)6(11)12/h2-5,10H,1,9H2,(H,11,12)(H,13,14)/t2-,3-,4-,5-,8-/m0/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50434128
PNG
(CHEMBL2381646)
Show SMILES N[C@@H]1C[C@](N)([C@H]2[C@@H]1[C@@H]2C(O)=O)C(O)=O
Show InChI InChI=1S/C8H12N2O4/c9-2-1-8(10,7(13)14)5-3(2)4(5)6(11)12/h2-5H,1,9-10H2,(H,11,12)(H,13,14)/t2-,3+,4+,5+,8+/m1/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50434129
PNG
(CHEMBL2381647)
Show SMILES N[C@H]1C[C@](N)([C@H]2[C@@H]1[C@@H]2C(O)=O)C(O)=O
Show InChI InChI=1S/C8H12N2O4/c9-2-1-8(10,7(13)14)5-3(2)4(5)6(11)12/h2-5H,1,9-10H2,(H,11,12)(H,13,14)/t2-,3-,4-,5-,8-/m0/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50434138
PNG
(CHEMBL2381651)
Show SMILES N[C@]1(C[C@H](Sc2ccccc2)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C14H15NO4S/c15-14(13(18)19)6-8(9-10(11(9)14)12(16)17)20-7-4-2-1-3-5-7/h1-5,8-11H,6,15H2,(H,16,17)(H,18,19)/t8-,9-,10-,11-,14-/m0/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50434139
PNG
(CHEMBL2381650)
Show SMILES N[C@]1(C[C@@H](Sc2ccccc2)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C14H15NO4S/c15-14(13(18)19)6-8(9-10(11(9)14)12(16)17)20-7-4-2-1-3-5-7/h1-5,8-11H,6,15H2,(H,16,17)(H,18,19)/t8-,9+,10+,11+,14+/m1/s1
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n/an/an/an/a>2.50E+4n/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
GRM8


(HUMAN)
BDBM50388941
PNG
(CHEMBL2063423)
Show SMILES O=NC1[C@@H]2C[C@@]2(Oc2ccccc12)C(=O)Nc1ccccn1
Show InChI InChI=1S/C16H13N3O3/c20-15(18-13-7-3-4-8-17-13)16-9-11(16)14(19-21)10-5-1-2-6-12(10)22-16/h1-8,11,14H,9H2,(H,17,18,20)/t11-,14?,16-/m0/s1
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n/an/an/an/a>3.00E+4n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulation activity at mGlu8 receptor


J Med Chem 55: 1445-64 (2012)


Article DOI: 10.1021/jm201139r
BindingDB Entry DOI: 10.7270/Q25D8SWH
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50202407
PNG
((-)-(1R,4S,5S,6S)-4-amino-2-thiabicyclo[3.1.0]hexa...)
Show SMILES N[C@]1(CS(=O)(=O)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H9NO6S/c8-7(6(11)12)1-15(13,14)4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1
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n/an/an/an/a 4.78E+4n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells


J Med Chem 50: 233-40 (2007)


Article DOI: 10.1021/jm060917u
BindingDB Entry DOI: 10.7270/Q21Z442N
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50204257
PNG
(CHEMBL3947221)
Show SMILES N[C@@]1([C@H]2[C@H]([C@@H]2C(O)=O)[C@H](O)[C@H]1OCc1ccc(Cl)c(Cl)c1)C(O)=O
Show InChI InChI=1S/C15H15Cl2NO6/c16-6-2-1-5(3-7(6)17)4-24-12-11(19)8-9(13(20)21)10(8)15(12,18)14(22)23/h1-3,8-12,19H,4,18H2,(H,20,21)(H,22,23)/t8-,9-,10-,11-,12+,15+/m0/s1
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n/an/an/an/a>5.00E+4n/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at recombinant human mGlu8 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as induction of forskolin-sti...


Bioorg Med Chem Lett 26: 5663-5668 (2016)


Article DOI: 10.1016/j.bmcl.2016.10.067
BindingDB Entry DOI: 10.7270/Q2JS9SDT
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50202406
PNG
((+)-(1R,2R,4S,5S,6S)-4-amino-2-thiabicyclo[3.1.0]h...)
Show SMILES N[C@]1(CS(=O)[C@H]2[C@@H]([C@@H]12)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H9NO5S/c8-7(6(11)12)1-14(13)4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+,14?/m1/s1
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n/an/an/an/a>1.00E+5n/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells


J Med Chem 50: 233-40 (2007)


Article DOI: 10.1021/jm060917u
BindingDB Entry DOI: 10.7270/Q21Z442N
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Mus musculus)
BDBM66976
PNG
((1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid;...)
Show SMILES N[C@]1(CC[C@H](C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C7H11NO4/c8-7(6(11)12)2-1-4(3-7)5(9)10/h4H,1-3,8H2,(H,9,10)(H,11,12)/t4-,7+/m1/s1
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n/an/an/an/a>1.00E+5n/an/an/an/a



CNS Research

Curated by ChEMBL


Assay Description
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse


J Med Chem 38: 1417-26 (1995)


Article DOI: 10.1021/jm00009a001
BindingDB Entry DOI: 10.7270/Q20R9Q1R
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Mus musculus)
BDBM17660
PNG
((2S)-2-amino-3-(3,5-dioxo-1,2,4-oxadiazolidin-2-yl...)
Show SMILES N[C@@H](Cn1oc(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C5H7N3O5/c6-2(3(9)10)1-8-4(11)7-5(12)13-8/h2H,1,6H2,(H,9,10)(H,7,11,12)/t2-/m0/s1
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n/an/an/an/a>1.00E+5n/an/an/an/a



CNS Research

Curated by ChEMBL


Assay Description
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse


J Med Chem 38: 1417-26 (1995)


Article DOI: 10.1021/jm00009a001
BindingDB Entry DOI: 10.7270/Q20R9Q1R
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Mus musculus)
BDBM50034501
PNG
((S)-Amino-(3-hydroxy-isoxazol-5-yl)-acetic acid | ...)
Show SMILES N[C@H](C(O)=O)c1cc(=O)[nH]o1
Show InChI InChI=1S/C5H6N2O4/c6-4(5(9)10)2-1-3(8)7-11-2/h1,4H,6H2,(H,7,8)(H,9,10)/t4-/m0/s1
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n/an/an/an/a>1.00E+5n/an/an/an/a



CNS Research

Curated by ChEMBL


Assay Description
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse


J Med Chem 38: 1417-26 (1995)


Article DOI: 10.1021/jm00009a001
BindingDB Entry DOI: 10.7270/Q20R9Q1R
More data for this
Ligand-Target Pair
GRM8


(HUMAN)
BDBM50089518
PNG
((1R,2R)-1-amino-2-(phosphonomethyl)cyclopropanecar...)
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>3.00E+5n/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