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Compile Data Set for Download or QSAR

Found 293 hits of ec50 for UniProtKB: P42262   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50457616
PNG
(CHEMBL4218628)
Show SMILES O=S1(=O)NCN(C2CC2)c2cc(CCc3ccc4c(c3)N(CNS4(=O)=O)C3CC3)ccc12
Show InChI InChI=1S/C22H26N4O4S2/c27-31(28)21-9-3-15(11-19(21)25(13-23-31)17-5-6-17)1-2-16-4-10-22-20(12-16)26(18-7-8-18)14-24-32(22,29)30/h3-4,9-12,17-18,23-24H,1-2,5-8,13-14H2
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n/an/an/an/a 1.26n/an/an/an/a



University of Liege

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2Q flop isoform (unknown origin) expressed in HEK293 cells assessed as increase in L-glutamate induced calcium ...


J Med Chem 61: 5279-5291 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00250
BindingDB Entry DOI: 10.7270/Q20C4ZCF
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50457616
PNG
(CHEMBL4218628)
Show SMILES O=S1(=O)NCN(C2CC2)c2cc(CCc3ccc4c(c3)N(CNS4(=O)=O)C3CC3)ccc12
Show InChI InChI=1S/C22H26N4O4S2/c27-31(28)21-9-3-15(11-19(21)25(13-23-31)17-5-6-17)1-2-16-4-10-22-20(12-16)26(18-7-8-18)14-24-32(22,29)30/h3-4,9-12,17-18,23-24H,1-2,5-8,13-14H2
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n/an/an/an/a 1.30n/an/an/an/a



University of Liege

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2Q flop isoform (unknown origin) expressed in HEK293 cells assessed as increase in L-glutamate induced calcium ...


J Med Chem 61: 5279-5291 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00250
BindingDB Entry DOI: 10.7270/Q20C4ZCF
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50251236
PNG
(CHEMBL4091984)
Show SMILES COc1cccc(Oc2ccc3N(CNS(=O)(=O)c3c2)C2CC2)c1
Show InChI InChI=1S/C17H18N2O4S/c1-22-13-3-2-4-14(9-13)23-15-7-8-16-17(10-15)24(20,21)18-11-19(16)12-5-6-12/h2-4,7-10,12,18H,5-6,11H2,1H3
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n/an/an/an/a 2n/an/an/an/a



Laboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2 (Q) flop isoform (unknown origin) expressed in HEK293 cells assessed as potentiation of glutamate-evoked calc...


J Med Chem 61: 251-264 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01323
BindingDB Entry DOI: 10.7270/Q2Z89FV2
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50251236
PNG
(CHEMBL4091984)
Show SMILES COc1cccc(Oc2ccc3N(CNS(=O)(=O)c3c2)C2CC2)c1
Show InChI InChI=1S/C17H18N2O4S/c1-22-13-3-2-4-14(9-13)23-15-7-8-16-17(10-15)24(20,21)18-11-19(16)12-5-6-12/h2-4,7-10,12,18H,5-6,11H2,1H3
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n/an/an/an/a 2n/an/an/an/a



Laboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2 (Q) flop isoform (unknown origin) expressed in HEK293 cells assessed as potentiation of glutamate-evoked calc...


J Med Chem 61: 251-264 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01323
BindingDB Entry DOI: 10.7270/Q2Z89FV2
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50457614
PNG
(CHEMBL4202524)
Show SMILES CN1CNS(=O)(=O)c2ccc(CCc3ccc4c(c3)N(C)CNS4(=O)=O)cc12
Show InChI InChI=1S/C18H22N4O4S2/c1-21-11-19-27(23,24)17-7-5-13(9-15(17)21)3-4-14-6-8-18-16(10-14)22(2)12-20-28(18,25)26/h5-10,19-20H,3-4,11-12H2,1-2H3
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n/an/an/an/a 14n/an/an/an/a



University of Liege

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2Q flop isoform (unknown origin) expressed in HEK293 cells assessed as increase in L-glutamate induced calcium ...


J Med Chem 61: 5279-5291 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00250
BindingDB Entry DOI: 10.7270/Q20C4ZCF
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50457614
PNG
(CHEMBL4202524)
Show SMILES CN1CNS(=O)(=O)c2ccc(CCc3ccc4c(c3)N(C)CNS4(=O)=O)cc12
Show InChI InChI=1S/C18H22N4O4S2/c1-21-11-19-27(23,24)17-7-5-13(9-15(17)21)3-4-14-6-8-18-16(10-14)22(2)12-20-28(18,25)26/h5-10,19-20H,3-4,11-12H2,1-2H3
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n/an/an/an/a 14.5n/an/an/an/a



University of Liege

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2Q flop isoform (unknown origin) expressed in HEK293 cells assessed as increase in L-glutamate induced calcium ...


J Med Chem 61: 5279-5291 (2018)


Article DOI: 10.1021/acs.jmedchem.8b00250
BindingDB Entry DOI: 10.7270/Q20C4ZCF
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191961
PNG
(4-cyano-5-ethyl-1-methyl-3-(2'-methylsulfanyl-biph...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1SC
Show InChI InChI=1S/C22H20N2O2S/c1-4-18-17(13-23)20(21(22(25)26)24(18)2)15-11-9-14(10-12-15)16-7-5-6-8-19(16)27-3/h5-12H,4H2,1-3H3,(H,25,26)
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n/an/an/an/a 32n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flop expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191957
PNG
(4-cyano-3-(2'-ethoxy-biphenyl-4-yl)-5-ethyl-1-meth...)
Show SMILES CCOc1ccccc1-c1ccc(cc1)-c1c(C#N)c(CC)n(C)c1C(O)=O
Show InChI InChI=1S/C23H22N2O3/c1-4-19-18(14-24)21(22(23(26)27)25(19)3)16-12-10-15(11-13-16)17-8-6-7-9-20(17)28-5-2/h6-13H,4-5H2,1-3H3,(H,26,27)
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n/an/an/an/a 36n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flop expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191954
PNG
(3-(2'-chloro-biphenyl-4-yl)-4-cyano-5-ethyl-1-meth...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1Cl
Show InChI InChI=1S/C21H17ClN2O2/c1-3-18-16(12-23)19(20(21(25)26)24(18)2)14-10-8-13(9-11-14)15-6-4-5-7-17(15)22/h4-11H,3H2,1-2H3,(H,25,26)
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n/an/an/an/a 42n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50251237
PNG
(CHEMBL4062524)
Show SMILES Cc1cccc(Oc2ccc3N(CNS(=O)(=O)c3c2)C2CC2)c1
Show InChI InChI=1S/C17H18N2O3S/c1-12-3-2-4-14(9-12)22-15-7-8-16-17(10-15)23(20,21)18-11-19(16)13-5-6-13/h2-4,7-10,13,18H,5-6,11H2,1H3
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n/an/an/an/a 46n/an/an/an/a



Laboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2 (Q) flop isoform (unknown origin) expressed in HEK293 cells assessed as potentiation of glutamate-evoked calc...


J Med Chem 61: 251-264 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01323
BindingDB Entry DOI: 10.7270/Q2Z89FV2
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50192216
PNG
(3-(4-tert-butylphenyl)-4-cyano-5-ethylthiophene-2-...)
Show SMILES CCc1sc(C(O)=O)c(c1C#N)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C18H19NO2S/c1-5-14-13(10-19)15(16(22-14)17(20)21)11-6-8-12(9-7-11)18(2,3)4/h6-9H,5H2,1-4H3,(H,20,21)
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n/an/an/an/a 47n/an/an/an/a



Lilly S.A.

Curated by ChEMBL


Assay Description
Activity against human GLUR2 flip expressed in HEK293 cells assesed as glutamate-stimulated calcium influx by FLIPR assay


Bioorg Med Chem Lett 16: 5057-61 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.035
BindingDB Entry DOI: 10.7270/Q24749H7
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50164477
PNG
(CHEMBL3800556)
Show SMILES Cc1sc2nc(Cn3nc(cc3Cl)C(F)(F)F)cc(=O)n2c1[C@@H]1C[C@H]1CO |r|
Show InChI InChI=1S/C16H14ClF3N4O2S/c1-7-14(10-2-8(10)6-25)24-13(26)3-9(21-15(24)27-7)5-23-12(17)4-11(22-23)16(18,19)20/h3-4,8,10,25H,2,5-6H2,1H3/t8-,10+/m0/s1
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n/an/an/an/a 48n/an/an/an/a



Pharmaron-Beijing Co. Ltd.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 AMPAR flop isomer expressed in Dox-inducible cells measured every 5 mins by BD calcium indicator dye ba...


J Med Chem 59: 2760-79 (2016)


Article DOI: 10.1021/acs.jmedchem.5b02010
BindingDB Entry DOI: 10.7270/Q2N87CQW
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50251237
PNG
(CHEMBL4062524)
Show SMILES Cc1cccc(Oc2ccc3N(CNS(=O)(=O)c3c2)C2CC2)c1
Show InChI InChI=1S/C17H18N2O3S/c1-12-3-2-4-14(9-12)22-15-7-8-16-17(10-15)23(20,21)18-11-19(16)13-5-6-13/h2-4,7-10,13,18H,5-6,11H2,1H3
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n/an/an/an/a 50n/an/an/an/a



Laboratory of Medicinal Chemistry, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège , Quartier Hôpital B36 Av. Hippocrate 15 B-4000 Liège, Belgium.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of GluA2 (Q) flop isoform (unknown origin) expressed in HEK293 cells assessed as potentiation of glutamate-evoked calc...


J Med Chem 61: 251-264 (2018)


Article DOI: 10.1021/acs.jmedchem.7b01323
BindingDB Entry DOI: 10.7270/Q2Z89FV2
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191954
PNG
(3-(2'-chloro-biphenyl-4-yl)-4-cyano-5-ethyl-1-meth...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1Cl
Show InChI InChI=1S/C21H17ClN2O2/c1-3-18-16(12-23)19(20(21(25)26)24(18)2)14-10-8-13(9-11-14)15-6-4-5-7-17(15)22/h4-11H,3H2,1-2H3,(H,25,26)
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n/an/an/an/a 55n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flop expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191961
PNG
(4-cyano-5-ethyl-1-methyl-3-(2'-methylsulfanyl-biph...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1SC
Show InChI InChI=1S/C22H20N2O2S/c1-4-18-17(13-23)20(21(22(25)26)24(18)2)15-11-9-14(10-12-15)16-7-5-6-8-19(16)27-3/h5-12H,4H2,1-3H3,(H,25,26)
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n/an/an/an/a 57n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50164380
PNG
(CHEMBL3799878)
Show SMILES Cc1sc2nc(Cn3nc(cc3Cl)C(F)(F)F)cc(=O)n2c1[C@@H]1C[C@H]1C#N |r|
Show InChI InChI=1S/C16H11ClF3N5OS/c1-7-14(10-2-8(10)5-21)25-13(26)3-9(22-15(25)27-7)6-24-12(17)4-11(23-24)16(18,19)20/h3-4,8,10H,2,6H2,1H3/t8-,10+/m0/s1
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n/an/an/an/a 73n/an/an/an/a



Genentech, Inc.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 receptor flop isoform assessed as increase in glutamate-induced calcium flux measured at time interval ...


ACS Med Chem Lett 8: 84-89 (2017)


Article DOI: 10.1021/acsmedchemlett.6b00388
BindingDB Entry DOI: 10.7270/Q2VX0JH1
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50164380
PNG
(CHEMBL3799878)
Show SMILES Cc1sc2nc(Cn3nc(cc3Cl)C(F)(F)F)cc(=O)n2c1[C@@H]1C[C@H]1C#N |r|
Show InChI InChI=1S/C16H11ClF3N5OS/c1-7-14(10-2-8(10)5-21)25-13(26)3-9(22-15(25)27-7)6-24-12(17)4-11(23-24)16(18,19)20/h3-4,8,10H,2,6H2,1H3/t8-,10+/m0/s1
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n/an/an/an/a 73n/an/an/an/a



Pharmaron-Beijing Co. Ltd.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 AMPAR flop isomer expressed in Dox-inducible cells measured every 5 mins by BD calcium indicator dye ba...


J Med Chem 59: 2760-79 (2016)


Article DOI: 10.1021/acs.jmedchem.5b02010
BindingDB Entry DOI: 10.7270/Q2N87CQW
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191952
PNG
(4-cyano-3-(2'-cyano-biphenyl-4-yl)-5-ethyl-1-methy...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1C#N
Show InChI InChI=1S/C22H17N3O2/c1-3-19-18(13-24)20(21(22(26)27)25(19)2)15-10-8-14(9-11-15)17-7-5-4-6-16(17)12-23/h4-11H,3H2,1-2H3,(H,26,27)
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n/an/an/an/a 73n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flop expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50192221
PNG
(3-(4-tert-butylphenyl)-4-cyano-5-(trifluoromethyl)...)
Show SMILES CC(C)(C)c1ccc(cc1)-c1c(sc(c1C#N)C(F)(F)F)C(O)=O
Show InChI InChI=1S/C17H14F3NO2S/c1-16(2,3)10-6-4-9(5-7-10)12-11(8-21)14(17(18,19)20)24-13(12)15(22)23/h4-7H,1-3H3,(H,22,23)
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n/an/an/an/a 78n/an/an/an/a



Lilly S.A.

Curated by ChEMBL


Assay Description
Activity against human GLUR2 flip expressed in HEK293 cells assesed as glutamate-stimulated calcium influx by FLIPR assay


Bioorg Med Chem Lett 16: 5057-61 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.035
BindingDB Entry DOI: 10.7270/Q24749H7
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191952
PNG
(4-cyano-3-(2'-cyano-biphenyl-4-yl)-5-ethyl-1-methy...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1C#N
Show InChI InChI=1S/C22H17N3O2/c1-3-19-18(13-24)20(21(22(26)27)25(19)2)15-10-8-14(9-11-15)17-7-5-4-6-16(17)12-23/h4-11H,3H2,1-2H3,(H,26,27)
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n/an/an/an/a 82n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191957
PNG
(4-cyano-3-(2'-ethoxy-biphenyl-4-yl)-5-ethyl-1-meth...)
Show SMILES CCOc1ccccc1-c1ccc(cc1)-c1c(C#N)c(CC)n(C)c1C(O)=O
Show InChI InChI=1S/C23H22N2O3/c1-4-19-18(14-24)21(22(23(26)27)25(19)3)16-12-10-15(11-13-16)17-8-6-7-9-20(17)28-5-2/h6-13H,4-5H2,1-3H3,(H,26,27)
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n/an/an/an/a 83n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191959
PNG
(3-(4-tert-butylphenyl)-4-cyano-5-(methylthio)thiop...)
Show SMILES CSc1sc(C(O)=O)c(c1C#N)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C17H17NO2S2/c1-17(2,3)11-7-5-10(6-8-11)13-12(9-18)16(21-4)22-14(13)15(19)20/h5-8H,1-4H3,(H,19,20)
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n/an/an/an/a 97n/an/an/an/a



Lilly S.A.

Curated by ChEMBL


Assay Description
Activity against human GLUR2 flip expressed in HEK293 cells assesed as glutamate-stimulated calcium influx by FLIPR assay


Bioorg Med Chem Lett 16: 5057-61 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.035
BindingDB Entry DOI: 10.7270/Q24749H7
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191959
PNG
(3-(4-tert-butylphenyl)-4-cyano-5-(methylthio)thiop...)
Show SMILES CSc1sc(C(O)=O)c(c1C#N)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C17H17NO2S2/c1-17(2,3)11-7-5-10(6-8-11)13-12(9-18)16(21-4)22-14(13)15(19)20/h5-8H,1-4H3,(H,19,20)
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n/an/an/an/a 97n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50417564
PNG
(CHEMBL1642168)
Show SMILES CC(C)S(=O)(=O)NC1CCc2cc(Cn3cc(CO)c(n3)C(F)(F)F)ccc12
Show InChI InChI=1S/C18H22F3N3O3S/c1-11(2)28(26,27)23-16-6-4-13-7-12(3-5-15(13)16)8-24-9-14(10-25)17(22-24)18(19,20)21/h3,5,7,9,11,16,23,25H,4,6,8,10H2,1-2H3
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n/an/an/an/a 100n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Modulatory activity at GluA2 receptor LBD


Bioorg Med Chem Lett 21: 805-11 (2011)


Article DOI: 10.1016/j.bmcl.2010.11.098
BindingDB Entry DOI: 10.7270/Q2Q52QWZ
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50417574
PNG
(CHEMBL1642155)
Show SMILES CC(C)S(=O)(=O)N[C@H]1Cc2ccc(Cn3nc(cc3C(F)(F)F)C(F)(F)F)cc2C1 |r|
Show InChI InChI=1S/C18H19F6N3O2S/c1-10(2)30(28,29)26-14-6-12-4-3-11(5-13(12)7-14)9-27-16(18(22,23)24)8-15(25-27)17(19,20)21/h3-5,8,10,14,26H,6-7,9H2,1-2H3/t14-/m0/s1
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n/an/an/an/a 100n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Modulatory activity at GluA2 receptor LBD


Bioorg Med Chem Lett 21: 805-11 (2011)


Article DOI: 10.1016/j.bmcl.2010.11.098
BindingDB Entry DOI: 10.7270/Q2Q52QWZ
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50331386
PNG
(CHEMBL1289293 | N-((3S,4S)-4-(3'-acetylbiphenyl-4-...)
Show SMILES CC(C)S(=O)(=O)N[C@@H]1COC[C@@H]1c1ccc(cc1)-c1cccc(c1)C(C)=O |r|
Show InChI InChI=1S/C21H25NO4S/c1-14(2)27(24,25)22-21-13-26-12-20(21)17-9-7-16(8-10-17)19-6-4-5-18(11-19)15(3)23/h4-11,14,20-22H,12-13H2,1-3H3/t20-,21-/m1/s1
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n/an/an/an/a 100n/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Positive modulation of human GluA2 flip receptor by FLIPR assay


Bioorg Med Chem Lett 20: 7116-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.09.062
BindingDB Entry DOI: 10.7270/Q2WQ042G
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191955
PNG
(3-biphenyl-4-yl-4-cyano-5-ethyl-1-methyl-1H-pyrrol...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1
Show InChI InChI=1S/C21H18N2O2/c1-3-18-17(13-22)19(20(21(24)25)23(18)2)16-11-9-15(10-12-16)14-7-5-4-6-8-14/h4-12H,3H2,1-2H3,(H,24,25)
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n/an/an/an/a 103n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191948
PNG
(4-cyano-5-ethyl-3-(2'-fluoro-biphenyl-4-yl)-1-meth...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1F
Show InChI InChI=1S/C21H17FN2O2/c1-3-18-16(12-23)19(20(21(25)26)24(18)2)14-10-8-13(9-11-14)15-6-4-5-7-17(15)22/h4-11H,3H2,1-2H3,(H,25,26)
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n/an/an/an/a 111n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191956
PNG
(3-(4'-chloro-biphenyl-4-yl)-4-cyano-5-ethyl-1-meth...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C21H17ClN2O2/c1-3-18-17(12-23)19(20(21(25)26)24(18)2)15-6-4-13(5-7-15)14-8-10-16(22)11-9-14/h4-11H,3H2,1-2H3,(H,25,26)
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n/an/an/an/a 142n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191948
PNG
(4-cyano-5-ethyl-3-(2'-fluoro-biphenyl-4-yl)-1-meth...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1F
Show InChI InChI=1S/C21H17FN2O2/c1-3-18-16(12-23)19(20(21(25)26)24(18)2)14-10-8-13(9-11-14)15-6-4-5-7-17(15)22/h4-11H,3H2,1-2H3,(H,25,26)
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n/an/an/an/a 143n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flop expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50316375
PNG
(CHEMBL1097939 | LY-404187 | N-[2-(4'-cyanobiphenyl...)
Show SMILES CC(C)S(=O)(=O)NCC(C)C1CCC(CC1)c1ccc(cc1)C#N |(35.08,-18.3,;35.1,-19.84,;36.44,-20.59,;33.78,-20.62,;32.99,-21.94,;34.53,-21.94,;32.44,-19.86,;31.11,-20.63,;29.77,-19.86,;29.77,-18.32,;28.44,-20.63,;28.44,-22.17,;27.12,-22.94,;25.78,-22.17,;25.77,-20.64,;27.1,-19.86,;24.45,-22.95,;23.11,-22.18,;21.79,-22.95,;21.79,-24.5,;23.12,-25.27,;24.46,-24.5,;20.45,-25.27,;19.11,-26.03,)|
Show InChI InChI=1S/C19H28N2O2S/c1-14(2)24(22,23)21-13-15(3)17-8-10-19(11-9-17)18-6-4-16(12-20)5-7-18/h4-7,14-15,17,19,21H,8-11,13H2,1-3H3
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n/an/an/an/a 150n/an/an/an/a



University of California

Curated by ChEMBL


Assay Description
Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM...


Bioorg Med Chem 18: 1381-7 (2010)


Article DOI: 10.1016/j.bmc.2009.12.072
BindingDB Entry DOI: 10.7270/Q27W6CB2
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50094024
PNG
((+/-) Propane-2-sulfonic acid [2-(4'-cyano-bipheny...)
Show SMILES CC(C)S(=O)(=O)NCC(C)c1ccc(cc1)-c1ccc(cc1)C#N
Show InChI InChI=1S/C19H22N2O2S/c1-14(2)24(22,23)21-13-15(3)17-8-10-19(11-9-17)18-6-4-16(12-20)5-7-18/h4-11,14-15,21H,13H2,1-3H3
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n/an/an/an/a 150n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at GluR2 receptor


J Med Chem 53: 7271-9 (2010)


Article DOI: 10.1021/jm1000419
BindingDB Entry DOI: 10.7270/Q2W0965T
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50164477
PNG
(CHEMBL3800556)
Show SMILES Cc1sc2nc(Cn3nc(cc3Cl)C(F)(F)F)cc(=O)n2c1[C@@H]1C[C@H]1CO |r|
Show InChI InChI=1S/C16H14ClF3N4O2S/c1-7-14(10-2-8(10)6-25)24-13(26)3-9(21-15(24)27-7)5-23-12(17)4-11(22-23)16(18,19)20/h3-4,8,10,25H,2,5-6H2,1H3/t8-,10+/m0/s1
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n/an/an/an/a 150n/an/an/an/a



Pharmaron-Beijing Co. Ltd.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 AMPAR flip isomer expressed in Dox-inducible cells measured every 5 mins by BD calcium indicator dye ba...


J Med Chem 59: 2760-79 (2016)


Article DOI: 10.1021/acs.jmedchem.5b02010
BindingDB Entry DOI: 10.7270/Q2N87CQW
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50417565
PNG
(CHEMBL1642169)
Show SMILES OCc1cn(Cc2ccc3C(CCc3c2)NS(=O)(=O)C2CC2)nc1C(F)(F)F
Show InChI InChI=1S/C18H20F3N3O3S/c19-18(20,21)17-13(10-25)9-24(22-17)8-11-1-5-15-12(7-11)2-6-16(15)23-28(26,27)14-3-4-14/h1,5,7,9,14,16,23,25H,2-4,6,8,10H2
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n/an/an/an/a 158n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Modulatory activity at GluA2 receptor LBD


Bioorg Med Chem Lett 21: 805-11 (2011)


Article DOI: 10.1016/j.bmcl.2010.11.098
BindingDB Entry DOI: 10.7270/Q2Q52QWZ
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191962
PNG
(3-biphenyl-4-yl-4-cyano-1-methyl-5-methylsulfanyl-...)
Show SMILES CSc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1
Show InChI InChI=1S/C20H16N2O2S/c1-22-18(20(23)24)17(16(12-21)19(22)25-2)15-10-8-14(9-11-15)13-6-4-3-5-7-13/h3-11H,1-2H3,(H,23,24)
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n/an/an/an/a 174n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191962
PNG
(3-biphenyl-4-yl-4-cyano-1-methyl-5-methylsulfanyl-...)
Show SMILES CSc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1
Show InChI InChI=1S/C20H16N2O2S/c1-22-18(20(23)24)17(16(12-21)19(22)25-2)15-10-8-14(9-11-15)13-6-4-3-5-7-13/h3-11H,1-2H3,(H,23,24)
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n/an/an/an/a 174n/an/an/an/a



Lilly S.A.

Curated by ChEMBL


Assay Description
Activity against human GLUR2 flip expressed in HEK293 cells assesed as glutamate-stimulated calcium influx by FLIPR assay


Bioorg Med Chem Lett 16: 5057-61 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.035
BindingDB Entry DOI: 10.7270/Q24749H7
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50192222
PNG
(3-(4-tert-butylphenyl)-4-cyano-5-(dimethylamino)th...)
Show SMILES CN(C)c1sc(C(O)=O)c(c1C#N)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C18H20N2O2S/c1-18(2,3)12-8-6-11(7-9-12)14-13(10-19)16(20(4)5)23-15(14)17(21)22/h6-9H,1-5H3,(H,21,22)
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n/an/an/an/a 176n/an/an/an/a



Lilly S.A.

Curated by ChEMBL


Assay Description
Activity against human GLUR2 flip expressed in HEK293 cells assesed as glutamate-stimulated calcium influx by FLIPR assay


Bioorg Med Chem Lett 16: 5057-61 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.035
BindingDB Entry DOI: 10.7270/Q24749H7
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191964
PNG
(3-(3'-chloro-biphenyl-4-yl)-4-cyano-5-ethyl-1-meth...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1cccc(Cl)c1
Show InChI InChI=1S/C21H17ClN2O2/c1-3-18-17(12-23)19(20(21(25)26)24(18)2)14-9-7-13(8-10-14)15-5-4-6-16(22)11-15/h4-11H,3H2,1-2H3,(H,25,26)
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n/an/an/an/a 186n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50164485
PNG
(CHEMBL3799657)
Show SMILES CCN(Cc1cc(=O)n2c([C@@H]3C[C@H]3CO)c(C)sc2n1)c1ccc(F)cc1 |r|
Show InChI InChI=1S/C20H22FN3O2S/c1-3-23(16-6-4-14(21)5-7-16)10-15-9-18(26)24-19(17-8-13(17)11-25)12(2)27-20(24)22-15/h4-7,9,13,17,25H,3,8,10-11H2,1-2H3/t13-,17+/m0/s1
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n/an/an/an/a 204n/an/an/an/a



Pharmaron-Beijing Co. Ltd.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 AMPAR flop isomer expressed in Dox-inducible cells measured every 5 mins by BD calcium indicator dye ba...


J Med Chem 59: 2760-79 (2016)


Article DOI: 10.1021/acs.jmedchem.5b02010
BindingDB Entry DOI: 10.7270/Q2N87CQW
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50205852
PNG
(CHEMBL3976578 | US10280165, Example 38)
Show SMILES Cc1cc([C@@H]2C[C@H]2C#N)n2c(c1)nc(Cn1nc(cc1Cl)C(F)(F)F)cc2=O |r|
Show InChI InChI=1S/C18H13ClF3N5O/c1-9-2-13(12-4-10(12)7-23)27-16(3-9)24-11(5-17(27)28)8-26-15(19)6-14(25-26)18(20,21)22/h2-3,5-6,10,12H,4,8H2,1H3/t10-,12+/m0/s1
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n/an/an/an/a 210n/an/an/an/a



Genentech, Inc.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 receptor flop isoform assessed as increase in glutamate-induced calcium flux measured at time interval ...


ACS Med Chem Lett 8: 84-89 (2017)


Article DOI: 10.1021/acsmedchemlett.6b00388
BindingDB Entry DOI: 10.7270/Q2VX0JH1
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50205852
PNG
(CHEMBL3976578 | US10280165, Example 38)
Show SMILES Cc1cc([C@@H]2C[C@H]2C#N)n2c(c1)nc(Cn1nc(cc1Cl)C(F)(F)F)cc2=O |r|
Show InChI InChI=1S/C18H13ClF3N5O/c1-9-2-13(12-4-10(12)7-23)27-16(3-9)24-11(5-17(27)28)8-26-15(19)6-14(25-26)18(20,21)22/h2-3,5-6,10,12H,4,8H2,1H3/t10-,12+/m0/s1
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n/an/an/an/a 210n/an/an/an/a



Genentech, Inc.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 receptor flop isoform assessed as increase in glutamate-induced calcium flux measured at time interval ...


ACS Med Chem Lett 8: 84-89 (2017)


Article DOI: 10.1021/acsmedchemlett.6b00388
BindingDB Entry DOI: 10.7270/Q2VX0JH1
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50192216
PNG
(3-(4-tert-butylphenyl)-4-cyano-5-ethylthiophene-2-...)
Show SMILES CCc1sc(C(O)=O)c(c1C#N)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C18H19NO2S/c1-5-14-13(10-19)15(16(22-14)17(20)21)11-6-8-12(9-7-11)18(2,3)4/h6-9H,5H2,1-4H3,(H,20,21)
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n/an/an/an/a 216n/an/an/an/a



Lilly S.A.

Curated by ChEMBL


Assay Description
Activity against human GLUR2 flop expressed in HEK293 cells assesed as glutamate-stimulated calcium influx by FLIPR assay


Bioorg Med Chem Lett 16: 5057-61 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.035
BindingDB Entry DOI: 10.7270/Q24749H7
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50192221
PNG
(3-(4-tert-butylphenyl)-4-cyano-5-(trifluoromethyl)...)
Show SMILES CC(C)(C)c1ccc(cc1)-c1c(sc(c1C#N)C(F)(F)F)C(O)=O
Show InChI InChI=1S/C17H14F3NO2S/c1-16(2,3)10-6-4-9(5-7-10)12-11(8-21)14(17(18,19)20)24-13(12)15(22)23/h4-7H,1-3H3,(H,22,23)
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n/an/an/an/a 231n/an/an/an/a



Lilly S.A.

Curated by ChEMBL


Assay Description
Activity against human GLUR2 flop expressed in HEK293 cells assesed as glutamate-stimulated calcium influx by FLIPR assay


Bioorg Med Chem Lett 16: 5057-61 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.035
BindingDB Entry DOI: 10.7270/Q24749H7
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50164476
PNG
(CHEMBL3799732)
Show SMILES CCN(Cc1cc(=O)n2cc(C)sc2n1)c1ccc(F)cc1
Show InChI InChI=1S/C16H16FN3OS/c1-3-19(14-6-4-12(17)5-7-14)10-13-8-15(21)20-9-11(2)22-16(20)18-13/h4-9H,3,10H2,1-2H3
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n/an/an/an/a 245n/an/an/an/a



Pharmaron-Beijing Co. Ltd.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 AMPAR flop isomer expressed in Dox-inducible cells measured every 5 mins by BD calcium indicator dye ba...


J Med Chem 59: 2760-79 (2016)


Article DOI: 10.1021/acs.jmedchem.5b02010
BindingDB Entry DOI: 10.7270/Q2N87CQW
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50164476
PNG
(CHEMBL3799732)
Show SMILES CCN(Cc1cc(=O)n2cc(C)sc2n1)c1ccc(F)cc1
Show InChI InChI=1S/C16H16FN3OS/c1-3-19(14-6-4-12(17)5-7-14)10-13-8-15(21)20-9-11(2)22-16(20)18-13/h4-9H,3,10H2,1-2H3
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n/an/an/an/a 252n/an/an/an/a



Pharmaron-Beijing Co. Ltd.

Curated by ChEMBL


Assay Description
Positive allosteric modulation of human GluA2 AMPAR flip isomer expressed in Dox-inducible cells measured every 5 mins by BD calcium indicator dye ba...


J Med Chem 59: 2760-79 (2016)


Article DOI: 10.1021/acs.jmedchem.5b02010
BindingDB Entry DOI: 10.7270/Q2N87CQW
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191965
PNG
(4-cyano-5-ethyl-1-methyl-3-(2'-methyl-biphenyl-4-y...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1C
Show InChI InChI=1S/C22H20N2O2/c1-4-19-18(13-23)20(21(22(25)26)24(19)3)16-11-9-15(10-12-16)17-8-6-5-7-14(17)2/h5-12H,4H2,1-3H3,(H,25,26)
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n/an/an/an/a 270n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50191958
PNG
(4-cyano-5-ethyl-3-(2'-methoxy-biphenyl-4-yl)-1-met...)
Show SMILES CCc1c(C#N)c(c(C(O)=O)n1C)-c1ccc(cc1)-c1ccccc1OC
Show InChI InChI=1S/C22H20N2O3/c1-4-18-17(13-23)20(21(22(25)26)24(18)2)15-11-9-14(10-12-15)16-7-5-6-8-19(16)27-3/h5-12H,4H2,1-3H3,(H,25,26)
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n/an/an/an/a 280n/an/an/an/a



Eli Lilly and Co

Curated by ChEMBL


Assay Description
Activity at human recombinant iGluR2 flip expressed in HEK293 cells measured as change in intracellular calcium ion concentration in presence of glut...


Bioorg Med Chem Lett 16: 5203-6 (2006)


Article DOI: 10.1016/j.bmcl.2006.07.012
BindingDB Entry DOI: 10.7270/Q21G0KWF
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50331389
PNG
(CHEMBL1289409 | N-((3S,4S)-4-(4-(5-fluoropyridin-2...)
Show SMILES CC(C)S(=O)(=O)N[C@@H]1COC[C@@H]1c1ccc(cc1)-c1ccc(F)cn1 |r|
Show InChI InChI=1S/C18H21FN2O3S/c1-12(2)25(22,23)21-18-11-24-10-16(18)13-3-5-14(6-4-13)17-8-7-15(19)9-20-17/h3-9,12,16,18,21H,10-11H2,1-2H3/t16-,18-/m1/s1
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Positive modulation of human GluA2 flip receptor by FLIPR assay


Bioorg Med Chem Lett 20: 7116-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.09.062
BindingDB Entry DOI: 10.7270/Q2WQ042G
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50331387
PNG
(CHEMBL1289294 | N-((3S,4S)-4-(4-(6-fluoropyridin-3...)
Show SMILES CC(C)S(=O)(=O)N[C@@H]1COC[C@@H]1c1ccc(cc1)-c1ccc(F)nc1 |r|
Show InChI InChI=1S/C18H21FN2O3S/c1-12(2)25(22,23)21-17-11-24-10-16(17)14-5-3-13(4-6-14)15-7-8-18(19)20-9-15/h3-9,12,16-17,21H,10-11H2,1-2H3/t16-,17-/m1/s1
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GlaxoSmithKline

Curated by ChEMBL


Assay Description
Positive modulation of human GluA2 flip receptor by FLIPR assay


Bioorg Med Chem Lett 20: 7116-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.09.062
BindingDB Entry DOI: 10.7270/Q2WQ042G
More data for this
Ligand-Target Pair
Glutamate receptor 2


(Homo sapiens (Human))
BDBM50331388
PNG
(CHEMBL1289408 | N-((3S,4S)-4-(4-(5-fluoropyridin-3...)
Show SMILES CC(C)S(=O)(=O)N[C@@H]1COC[C@@H]1c1ccc(cc1)-c1cncc(F)c1 |r|
Show InChI InChI=1S/C18H21FN2O3S/c1-12(2)25(22,23)21-18-11-24-10-17(18)14-5-3-13(4-6-14)15-7-16(19)9-20-8-15/h3-9,12,17-18,21H,10-11H2,1-2H3/t17-,18-/m1/s1
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n/an/an/an/a 300n/an/an/an/a



GlaxoSmithKline

Curated by ChEMBL


Assay Description
Positive modulation of human GluA2 flip receptor by FLIPR assay


Bioorg Med Chem Lett 20: 7116-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.09.062
BindingDB Entry DOI: 10.7270/Q2WQ042G
More data for this
Ligand-Target Pair
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