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Compile Data Set for Download or QSAR

Found 45 hits of ic50 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


(Homo sapiens (Human))
BDBM50004051
PNG
(2-Amino-4-phosphono-butyric acid | 2-Amino-4-phosp...)
Show SMILES NC(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)
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n/an/a 5.10n/an/an/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8


Bioorg Med Chem Lett 15: 349-51 (2004)


Article DOI: 10.1016/j.bmcl.2004.10.093
BindingDB Entry DOI: 10.7270/Q2G161M2
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
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/a 5.70n/an/an/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8


Bioorg Med Chem Lett 15: 349-51 (2004)


Article DOI: 10.1016/j.bmcl.2004.10.093
BindingDB Entry DOI: 10.7270/Q2G161M2
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50062522
PNG
((1S,2S)-2-((S)-1-amino-1-carboxy-2-(9H-xanthen-9-y...)
Show SMILES N[C@@](CC1c2ccccc2Oc2ccccc12)([C@H]1C[C@@H]1C(O)=O)C(O)=O
Show InChI InChI=1S/C20H19NO5/c21-20(19(24)25,15-9-13(15)18(22)23)10-14-11-5-1-3-7-16(11)26-17-8-4-2-6-12(14)17/h1-8,13-15H,9-10,21H2,(H,22,23)(H,24,25)/t13-,15-,20-/m0/s1
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n/an/a 170n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072169
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES CCCCC[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C25H29NO5/c1-2-3-4-11-17-21(23(27)28)22(17)25(26,24(29)30)14-18-15-9-5-7-12-19(15)31-20-13-8-6-10-16(18)20/h5-10,12-13,17-18,21-22H,2-4,11,14,26H2,1H3,(H,27,28)(H,29,30)/t17-,21+,22+,25?/m1/s1
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n/an/a 340n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072170
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES CC(C)C[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C24H27NO5/c1-13(2)11-16-20(22(26)27)21(16)24(25,23(28)29)12-17-14-7-3-5-9-18(14)30-19-10-6-4-8-15(17)19/h3-10,13,16-17,20-21H,11-12,25H2,1-2H3,(H,26,27)(H,28,29)/t16-,20+,21+,24?/m1/s1
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n/an/a 380n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072177
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES CCCC[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C24H27NO5/c1-2-3-8-16-20(22(26)27)21(16)24(25,23(28)29)13-17-14-9-4-6-11-18(14)30-19-12-7-5-10-15(17)19/h4-7,9-12,16-17,20-21H,2-3,8,13,25H2,1H3,(H,26,27)(H,28,29)/t16-,20+,21+,24?/m1/s1
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n/an/a 490n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072173
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES CCCCCC[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C26H31NO5/c1-2-3-4-5-12-18-22(24(28)29)23(18)26(27,25(30)31)15-19-16-10-6-8-13-20(16)32-21-14-9-7-11-17(19)21/h6-11,13-14,18-19,22-23H,2-5,12,15,27H2,1H3,(H,28,29)(H,30,31)/t18-,22+,23+,26?/m1/s1
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n/an/a 750n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072176
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES NC(CC1c2ccccc2Oc2ccccc12)([C@H]1[C@H](CCc2ccccc2)[C@@H]1C(O)=O)C(O)=O
Show InChI InChI=1S/C28H27NO5/c29-28(27(32)33,25-20(24(25)26(30)31)15-14-17-8-2-1-3-9-17)16-21-18-10-4-6-12-22(18)34-23-13-7-5-11-19(21)23/h1-13,20-21,24-25H,14-16,29H2,(H,30,31)(H,32,33)/t20-,24+,25+,28?/m1/s1
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n/an/a 990n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072171
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES C[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C21H21NO5/c1-11-17(19(23)24)18(11)21(22,20(25)26)10-14-12-6-2-4-8-15(12)27-16-9-5-3-7-13(14)16/h2-9,11,14,17-18H,10,22H2,1H3,(H,23,24)(H,25,26)/t11-,17+,18+,21?/m1/s1
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n/an/a 1.23E+3n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50204257
PNG
(CHEMBL3947221)
Show SMILES [H][C@]12[C@H](C(O)=O)[C@@]1([H])[C@@](N)([C@H](OCc1ccc(Cl)c(Cl)c1)[C@H]2O)C(O)=O |r|
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/a 1.90E+3n/an/an/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant human mGlu8 receptor expressed in hamster AV12 cells co-expressing human EAAT1/Galpha1s assessed as inhibition of ...


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
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072168
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES CCC[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C23H25NO5/c1-2-7-15-19(21(25)26)20(15)23(24,22(27)28)12-16-13-8-3-5-10-17(13)29-18-11-6-4-9-14(16)18/h3-6,8-11,15-16,19-20H,2,7,12,24H2,1H3,(H,25,26)(H,27,28)/t15-,19+,20+,23?/m1/s1
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n/an/a 2.25E+3n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072172
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES CC[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C22H23NO5/c1-2-12-18(20(24)25)19(12)22(23,21(26)27)11-15-13-7-3-5-9-16(13)28-17-10-6-4-8-14(15)17/h3-10,12,15,18-19H,2,11,23H2,1H3,(H,24,25)(H,26,27)/t12-,18+,19+,22?/m1/s1
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n/an/a 2.52E+3n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50072174
PNG
((1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl...)
Show SMILES CCCCCCCCC[C@@H]1[C@@H]([C@H]1C(N)(CC1c2ccccc2Oc2ccccc12)C(O)=O)C(O)=O
Show InChI InChI=1S/C29H37NO5/c1-2-3-4-5-6-7-8-15-21-25(27(31)32)26(21)29(30,28(33)34)18-22-19-13-9-11-16-23(19)35-24-17-12-10-14-20(22)24/h9-14,16-17,21-22,25-26H,2-8,15,18,30H2,1H3,(H,31,32)(H,33,34)/t21-,25+,26+,29?/m1/s1
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n/an/a 5.18E+3n/an/an/an/an/an/a



Centro de Investigación Lilly, SA

Curated by ChEMBL


Assay Description
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated


Bioorg Med Chem Lett 8: 2849-54 (1999)


BindingDB Entry DOI: 10.7270/Q2Z0379C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50301804
PNG
(5-(1-(2,4-difluorophenyl)-5-methyl-1H-1,2,3-triazo...)
Show SMILES CC(C)N1Cc2cc(ccc2C1=O)-c1nnn(c1C)-c1ccc(F)cc1F
Show InChI InChI=1S/C20H18F2N4O/c1-11(2)25-10-14-8-13(4-6-16(14)20(25)27)19-12(3)26(24-23-19)18-7-5-15(21)9-17(18)22/h4-9,11H,10H2,1-3H3
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n/an/a>1.00E+4n/an/an/an/an/an/a



Tsukuba Research Institute

Curated by ChEMBL


Assay Description
Antagonist activity at human mGluR8 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FL...


Bioorg Med Chem Lett 19: 5310-3 (2009)


Article DOI: 10.1016/j.bmcl.2009.07.145
BindingDB Entry DOI: 10.7270/Q26H4HGN
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50301520
PNG
(4-fluoro-N-(4-(6-(isopropylamino)pyrimidin-4-yl)th...)
Show SMILES CC(C)Nc1cc(ncn1)-c1csc(n1)N(C)C(=O)c1ccc(F)cc1
Show InChI InChI=1S/C18H18FN5OS/c1-11(2)22-16-8-14(20-10-21-16)15-9-26-18(23-15)24(3)17(25)12-4-6-13(19)7-5-12/h4-11H,1-3H3,(H,20,21,22)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Tsukuba Research Institute

Curated by ChEMBL


Assay Description
Inhibition of human mGluR8 receptor


Bioorg Med Chem Lett 19: 5464-8 (2009)


Article DOI: 10.1016/j.bmcl.2009.07.097
BindingDB Entry DOI: 10.7270/Q2W66KTT
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50278924
PNG
(CHEMBL505105 | N-methyl-5-(phenylethynyl)pyrimidin...)
Show SMILES CNc1ncc(cn1)C#Cc1ccccc1
Show InChI InChI=1S/C13H11N3/c1-14-13-15-9-12(10-16-13)8-7-11-5-3-2-4-6-11/h2-6,9-10H,1H3,(H,14,15,16)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Antagonist activity at mGlu8 receptor


J Med Chem 52: 4103-6 (2009)


Article DOI: 10.1021/jm900654c
BindingDB Entry DOI: 10.7270/Q2PZ58RJ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50523865
PNG
(CHEMBL4476495)
Show SMILES COc1ccc(cc1OC)-c1nnc(o1)-c1cc(OC(F)(F)F)ccc1-n1ccnc1
Show InChI InChI=1S/C20H15F3N4O4/c1-28-16-6-3-12(9-17(16)29-2)18-25-26-19(30-18)14-10-13(31-20(21,22)23)4-5-15(14)27-8-7-24-11-27/h3-11H,1-2H3
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n/an/a>1.00E+4n/an/an/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Negative allosteric modulation of mGlu8 receptor (unknown origin)


Bioorg Med Chem Lett 29: 1211-1214 (2019)


Article DOI: 10.1016/j.bmcl.2019.03.016
BindingDB Entry DOI: 10.7270/Q2WH2TDX
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50531687
PNG
(CHEMBL4445682)
Show SMILES COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(OC(F)(F)F)ccc1-n1cncn1
Show InChI InChI=1S/C21H19F3N4O4/c1-30-19-8-14(4-7-18(19)31-10-13-2-3-13)20(29)27-16-9-15(32-21(22,23)24)5-6-17(16)28-12-25-11-26-28/h4-9,11-13H,2-3,10H2,1H3,(H,27,29)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Vanderbilt University School of Medicine

Curated by ChEMBL


Assay Description
Negative allosteric modulation of mGlu8 receptor (unknown origin)


J Med Chem 62: 1690-1695 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01810
BindingDB Entry DOI: 10.7270/Q2QC070T
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM212860
PNG
(US9278960, 2-7 | US9663506, Example 2-7)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CN3C(=O)CCC3=O)cc2n1
Show InChI InChI=1S/C21H16FN3O3/c22-14-4-2-13(3-5-14)16-10-18(21(23)28)24-17-9-12(1-6-15(16)17)11-25-19(26)7-8-20(25)27/h1-6,9-10H,7-8,11H2,(H2,23,28)
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n/an/a>1.00E+4n/an/an/an/an/an/a



Merck & Co.

Curated by ChEMBL


Assay Description
Antagonist activity at mGluR8 (unknown origin) by FLIPR assay


Bioorg Med Chem Lett 30: (2020)


Article DOI: 10.1016/j.bmcl.2020.127066
BindingDB Entry DOI: 10.7270/Q2G44TTJ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50278930
PNG
(2-(m-tolylethynyl)pyrimidine | CHEMBL496882)
Show SMILES Cc1cccc(c1)C#Cc1ncccn1
Show InChI InChI=1S/C13H10N2/c1-11-4-2-5-12(10-11)6-7-13-14-8-3-9-15-13/h2-5,8-10H,1H3
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Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Antagonist activity at mGlu8 receptor


J Med Chem 52: 4103-6 (2009)


Article DOI: 10.1021/jm900654c
BindingDB Entry DOI: 10.7270/Q2PZ58RJ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50244219
PNG
(CHEMBL4081453)
Show SMILES [H][C@]12[C@H](C(O)=O)[C@@]1([H])[C@@](N)(C[C@@H]2NC(=O)c1cccc(OC)c1)C(O)=O |r|
Show InChI InChI=1S/C16H18N2O6/c1-24-8-4-2-3-7(5-8)13(19)18-9-6-16(17,15(22)23)12-10(9)11(12)14(20)21/h2-5,9-12H,6,17H2,1H3,(H,18,19)(H,20,21)(H,22,23)/t9-,10-,11-,12-,16-/m0/s1
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TBA

Curated by ChEMBL


Assay Description
Antagonist activity at recombinant human mGlu8 receptor expressed in hamster AV12 cells co-expressing rat EAAT1/Galpha15 assessed as inhibition of gl...


J Med Chem 61: 2303-2328 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01481
BindingDB Entry DOI: 10.7270/Q2W95CM9
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50121643
PNG
(CHEMBL3616847)
Show SMILES [H][C@]12[C@H](C(O)=O)[C@@]1([H])[C@@](N)(C[C@H]2Sc1nnc[nH]1)C(O)=O |r|
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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Eli Lilly and Company

Curated by ChEMBL


Assay Description
Antagonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization afte...


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
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50558766
PNG
(CHEMBL4751065)
Show SMILES Cl.[H][C@]12[C@H](C(O)=O)[C@@]1([H])[C@@](N)([C@H](CSc1ccc(F)c(F)c1)[C@H]2O)C(O)=O |r|
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TBA

Assay Description
Agonist activity at human recombinant mGlu8 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as incr...


Citation and Details

BindingDB Entry DOI: 10.7270/Q2611419
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50116512
PNG
(CHEMBL3609741)
Show SMILES FCOc1cc(NC(=O)c2ccccn2)ccc1Cl
Show InChI InChI=1S/C13H10ClFN2O2/c14-10-5-4-9(7-12(10)19-8-15)17-13(18)11-3-1-2-6-16-11/h1-7H,8H2,(H,17,18)
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Massachusetts General Hospital

Curated by ChEMBL


Assay Description
Activity at mGlu8 receptor (unknown origin) expressed in HEK293 cells pre-treated for 15 mins before addition of EC80 concentration of reference agon...


Bioorg Med Chem Lett 25: 3956-60 (2015)


Article DOI: 10.1016/j.bmcl.2015.07.031
BindingDB Entry DOI: 10.7270/Q28C9Z1B
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50553603
PNG
(CHEMBL1349403)
Show SMILES CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(CC1)c1ccccc1OC
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TBA

Assay Description
Negative allosteric modulation of mGlu8 receptor (unknown origin)


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127529
BindingDB Entry DOI: 10.7270/Q28K7DQ0
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50339075
PNG
(Adamantan-1-yl-(4-pyridin-2-yl-piperazin-1-yl)-met...)
Show SMILES O=C(N1CCN(CC1)c1nccs1)C12CC3CC(CC(C3)C1)C2 |TLB:16:17:14.15.20:21,THB:16:15:21:22.17.18,18:17:14:20.19.21,18:19:14:22.16.17|
Show InChI InChI=1S/C18H25N3OS/c22-16(18-10-13-7-14(11-18)9-15(8-13)12-18)20-2-4-21(5-3-20)17-19-1-6-23-17/h1,6,13-15H,2-5,7-12H2
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Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Inhibition of mGluR8


Bioorg Med Chem Lett 19: 3209-13 (2009)


Article DOI: 10.1016/j.bmcl.2009.04.110
BindingDB Entry DOI: 10.7270/Q29S1RCR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50094841
PNG
((+)-2-Amino-3-fluoro-bicyclo[3.1.0]hexane-2,6-dica...)
Show SMILES N[C@@]1([C@H]2[C@@H](C[C@@H]1F)[C@@H]2C(O)=O)C(O)=O
Show InChI InChI=1S/C8H10FNO4/c9-3-1-2-4(6(11)12)5(2)8(3,10)7(13)14/h2-5H,1,10H2,(H,11,12)(H,13,14)/t2-,3-,4-,5-,8-/m0/s1
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TBA

Assay Description
Antagonist activity at human mGlu8 receptor expressed in CHO cell membranes in presence of glutamate by GTPgammaS binding assay


Citation and Details

Article DOI: 10.1016/j.ejmech.2020.112521
BindingDB Entry DOI: 10.7270/Q2CR5Z03
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50526873
PNG
(CHEMBL4461592)
Show SMILES Fc1cc(NC(=O)Nc2ccc(Cl)cn2)cc(c1)C#N
Show InChI InChI=1S/C13H8ClFN4O/c14-9-1-2-12(17-7-9)19-13(20)18-11-4-8(6-16)3-10(15)5-11/h1-5,7H,(H2,17,18,19,20)
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Purdue University

Curated by ChEMBL


Assay Description
Inhibition of mGluR8 (unknown origin)


J Med Chem 63: 2751-2788 (2020)


Article DOI: 10.1021/acs.jmedchem.9b01541
BindingDB Entry DOI: 10.7270/Q2QN6B6S
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50346073
PNG
(CHEMBL1783985 | cyclobutyl(2-azaspiro[5.5]undecan-...)
Show SMILES O=C(C1CCC1)N1CCCC2(CCCCC2)C1
Show InChI InChI=1S/C15H25NO/c17-14(13-6-4-7-13)16-11-5-10-15(12-16)8-2-1-3-9-15/h13H,1-12H2
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Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Inhibition of mGluR8


Bioorg Med Chem Lett 19: 3209-13 (2009)


Article DOI: 10.1016/j.bmcl.2009.04.110
BindingDB Entry DOI: 10.7270/Q29S1RCR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50547329
PNG
(CHEMBL1527295)
Show SMILES CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(CC1)c1ccccc1F
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TBA

Assay Description
Negative allosteric modulation of mGlu8 receptor (unknown origin)


Citation and Details

Article DOI: 10.1021/acsmedchemlett.0c00432
BindingDB Entry DOI: 10.7270/Q2ZG6WTX
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM430126
PNG
(4-(4-fluorophenyl)-5-((1-methyl-1H-pyrazol-3-yl)me...)
Show SMILES Cn1ccc(COc2cnc(cc2-c2ccc(F)cc2)C(N)=O)n1
Show InChI InChI=1S/C17H15FN4O2/c1-22-7-6-13(21-22)10-24-16-9-20-15(17(19)23)8-14(16)11-2-4-12(18)5-3-11/h2-9H,10H2,1H3,(H2,19,23)
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Vanderbilt University School of Medicine

Curated by ChEMBL


Assay Description
Negative allosteric modulation of mGlu8R (unknown origin)


J Med Chem 62: 378-384 (2019)


Article DOI: 10.1021/acs.jmedchem.8b01266
BindingDB Entry DOI: 10.7270/Q2125WWX
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071165
PNG
((2R,4R)-4-Amino-1-(2-chloro-benzyl)-pyrrolidine-2,...)
Show SMILES N[C@@]1(C[C@@H](N(Cc2ccccc2Cl)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C13H15ClN2O4/c14-9-4-2-1-3-8(9)6-16-7-13(15,12(19)20)5-10(16)11(17)18/h1-4,10H,5-7,15H2,(H,17,18)(H,19,20)/t10-,13-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071150
PNG
((2R,4R)-4-Amino-1-biphenyl-2-ylmethyl-pyrrolidine-...)
Show SMILES N[C@@]1(C[C@@H](N(Cc2ccccc2-c2ccccc2)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C19H20N2O4/c20-19(18(24)25)10-16(17(22)23)21(12-19)11-14-8-4-5-9-15(14)13-6-2-1-3-7-13/h1-9,16H,10-12,20H2,(H,22,23)(H,24,25)/t16-,19-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071164
PNG
((2R,4R)-4-Amino-1-methyl-pyrrolidine-2,4-dicarboxy...)
Show SMILES CN1C[C@](N)(C[C@@H]1C(O)=O)C(O)=O
Show InChI InChI=1S/C7H12N2O4/c1-9-3-7(8,6(12)13)2-4(9)5(10)11/h4H,2-3,8H2,1H3,(H,10,11)(H,12,13)/t4-,7-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50049748
PNG
((2S,4S)-2-Amino-4-(4,4-diphenyl-butyl)-pentanedioi...)
Show SMILES N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(O)=O)C(O)=O
Show InChI InChI=1S/C21H25NO4/c22-19(21(25)26)14-17(20(23)24)12-7-13-18(15-8-3-1-4-9-15)16-10-5-2-6-11-16/h1-6,8-11,17-19H,7,12-14,22H2,(H,23,24)(H,25,26)/t17-,19-/m0/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071167
PNG
((2R,4R)-4-Amino-1-(2,6-dichloro-benzyl)-pyrrolidin...)
Show SMILES N[C@@]1(C[C@@H](N(Cc2c(Cl)cccc2Cl)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C13H14Cl2N2O4/c14-8-2-1-3-9(15)7(8)5-17-6-13(16,12(20)21)4-10(17)11(18)19/h1-3,10H,4-6,16H2,(H,18,19)(H,20,21)/t10-,13-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071151
PNG
((2R,4R)-4-Amino-1-(2,2-diphenyl-ethyl)-pyrrolidine...)
Show SMILES N[C@@]1(C[C@@H](N(CC(c2ccccc2)c2ccccc2)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C20H22N2O4/c21-20(19(25)26)11-17(18(23)24)22(13-20)12-16(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-10,16-17H,11-13,21H2,(H,23,24)(H,25,26)/t17-,20-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071168
PNG
((2R,4R)-4-Amino-1-(3-chloro-benzyl)-pyrrolidine-2,...)
Show SMILES N[C@@]1(C[C@@H](N(Cc2cccc(Cl)c2)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C13H15ClN2O4/c14-9-3-1-2-8(4-9)6-16-7-13(15,12(19)20)5-10(16)11(17)18/h1-4,10H,5-7,15H2,(H,17,18)(H,19,20)/t10-,13-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071159
PNG
((2R,4R)-4-Amino-1-naphthalen-1-ylmethyl-pyrrolidin...)
Show SMILES N[C@@]1(C[C@@H](N(Cc2cccc3ccccc23)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C17H18N2O4/c18-17(16(22)23)8-14(15(20)21)19(10-17)9-12-6-3-5-11-4-1-2-7-13(11)12/h1-7,14H,8-10,18H2,(H,20,21)(H,22,23)/t14-,17-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071161
PNG
((2R,4R)-4-Amino-1-benzyl-pyrrolidine-2,4-dicarboxy...)
Show SMILES N[C@@]1(C[C@@H](N(Cc2ccccc2)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C13H16N2O4/c14-13(12(18)19)6-10(11(16)17)15(8-13)7-9-4-2-1-3-5-9/h1-5,10H,6-8,14H2,(H,16,17)(H,18,19)/t10-,13-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071155
PNG
((2R,4R)-4-Amino-1-naphthalen-2-ylmethyl-pyrrolidin...)
Show SMILES N[C@@]1(C[C@@H](N(Cc2ccc3ccccc3c2)C1)C(O)=O)C(O)=O
Show InChI InChI=1S/C17H18N2O4/c18-17(16(22)23)8-14(15(20)21)19(10-17)9-11-5-6-12-3-1-2-4-13(12)7-11/h1-7,14H,8-10,18H2,(H,20,21)(H,22,23)/t14-,17-/m1/s1
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Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071156
PNG
((2R,4R)-4-Amino-1-ethyl-pyrrolidine-2,4-dicarboxyl...)
Show SMILES CCN1C[C@](N)(C[C@@H]1C(O)=O)C(O)=O
Show InChI InChI=1S/C8H14N2O4/c1-2-10-4-8(9,7(13)14)3-5(10)6(11)12/h5H,2-4,9H2,1H3,(H,11,12)(H,13,14)/t5-,8-/m1/s1
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n/an/a>3.00E+5n/an/an/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50049748
PNG
((2S,4S)-2-Amino-4-(4,4-diphenyl-butyl)-pentanedioi...)
Show SMILES N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(O)=O)C(O)=O
Show InChI InChI=1S/C21H25NO4/c22-19(21(25)26)14-17(20(23)24)12-7-13-18(15-8-3-1-4-9-15)16-10-5-2-6-11-16/h1-6,8-11,17-19H,7,12-14,22H2,(H,23,24)(H,25,26)/t17-,19-/m0/s1
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Centro de Investigación Lilly

Curated by ChEMBL


Assay Description
Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 8 by measuring L-AP4 (0.3 uM of forskolin) (...


Bioorg Med Chem Lett 8: 765-70 (1999)


BindingDB Entry DOI: 10.7270/Q2T152SF
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50069111
PNG
((2S,4S)-2-Amino-4-(2,2-diphenyl-ethyl)-pentanedioi...)
Show SMILES N[C@@H](C[C@H](CC(c1ccccc1)c1ccccc1)C(O)=O)C(O)=O
Show InChI InChI=1S/C19H21NO4/c20-17(19(23)24)12-15(18(21)22)11-16(13-7-3-1-4-8-13)14-9-5-2-6-10-14/h1-10,15-17H,11-12,20H2,(H,21,22)(H,23,24)/t15-,17-/m0/s1
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n/an/a>3.00E+5n/an/an/an/an/an/a



Centro de Investigación Lilly

Curated by ChEMBL


Assay Description
Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 8 by measuring L-AP4 (0.3 uM of forskolin) (...


Bioorg Med Chem Lett 8: 765-70 (1999)


BindingDB Entry DOI: 10.7270/Q2T152SF
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 8


(Homo sapiens (Human))
BDBM50071162
PNG
(4-((S)-1-Carboxy-ethylamino)-benzoic acid | CHEMBL...)
Show SMILES C[C@H](Nc1ccc(cc1)C(O)=O)C(O)=O
Show InChI InChI=1S/C10H11NO4/c1-6(9(12)13)11-8-4-2-7(3-5-8)10(14)15/h2-6,11H,1H3,(H,12,13)(H,14,15)/t6-/m0/s1
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n/an/a>1.00E+6n/an/an/an/an/an/a



Eli Lilly and Company

Curated by ChEMBL


Assay Description
In vitro antagonist activity at recombinant Metabotropic glutamate receptor 8 expressed in RGT cells.


Bioorg Med Chem Lett 8: 1985-90 (1999)


BindingDB Entry DOI: 10.7270/Q2K35V5D
More data for this
Ligand-Target Pair