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Compile Data Set for Download or QSAR

Found 25 hits of ec50 for UniProtKB: P19493   
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 4


(Rattus norvegicus)
BDBM50330416
PNG
(CHEMBL1277002 | N-{(R)-2-[4'-((S)-2-Methanesulfony...)
Show SMILES C[C@@H](CNS(C)(=O)=O)c1ccc(cc1)-c1ccc(cc1)[C@H](C)CNS(C)(=O)=O |r|
Show InChI InChI=1S/C20H28N2O4S2/c1-15(13-21-27(3,23)24)17-5-9-19(10-6-17)20-11-7-18(8-12-20)16(2)14-22-28(4,25)26/h5-12,15-16,21-22H,13-14H2,1-4H3/t15-,16+
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n/an/an/an/a 870n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of rat recombinant GluR4 in cells


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
Glutamate receptor 4


(Rattus norvegicus)
BDBM50126764
PNG
((S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta...)
Show SMILES N[C@@H](CC1=CCCCc2o[nH]c(=O)c12)C(O)=O |t:3|
Show InChI InChI=1S/C11H14N2O4/c12-7(11(15)16)5-6-3-1-2-4-8-9(6)10(14)13-17-8/h3,7H,1-2,4-5,12H2,(H,13,14)(H,15,16)/t7-/m0/s1
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n/an/an/an/a 6.70E+3n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assa...


J Med Chem 52: 4911-22 (2009)

Checked by Author
Article DOI: 10.1021/jm900565c
BindingDB Entry DOI: 10.7270/Q2R49RP9
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50060635
PNG
((S)-2-Amino-3-(5-fluoro-2,4-dioxo-3,4-dihydro-2H-p...)
Show SMILES N[C@@H](Cn1cc(F)c(=O)[nH]c1=O)C(O)=O |r|
Show InChI InChI=1S/C7H8FN3O4/c8-3-1-11(2-4(9)6(13)14)7(15)10-5(3)12/h1,4H,2,9H2,(H,13,14)(H,10,12,15)/t4-/m0/s1
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n/an/an/an/a 1.19E+4n/an/an/an/a



European Research Centre for Drug Discovery and Development (NatSynDrugs)

Curated by ChEMBL


Assay Description
Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR4 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electro...


J Med Chem 51: 6614-8 (2008)


Article DOI: 10.1021/jm800865a
BindingDB Entry DOI: 10.7270/Q261117R
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 4


(Rattus norvegicus)
BDBM50002370
PNG
((R,S)-alpha-amino-3-hydroxy-5-methyl-4-isooxazole-...)
Show SMILES Cc1o[nH]c(=O)c1CC(N)C(O)=O
Show InChI InChI=1S/C7H10N2O4/c1-3-4(6(10)9-13-3)2-5(8)7(11)12/h5H,2,8H2,1H3,(H,9,10)(H,11,12)
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n/an/an/an/a 1.60E+4n/an/an/an/a



University of California

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by...


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 4


(Rattus norvegicus)
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 1.70E+4n/an/an/an/a



Universit£ degli Studi di Milano

Curated by ChEMBL


Assay Description
Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay


J Med Chem 51: 2311-5 (2008)


Article DOI: 10.1021/jm701394a
BindingDB Entry DOI: 10.7270/Q2Z320HT
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
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 1.96E+4n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at recombinant rat GluA4 receptor flip isoform expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay


J Med Chem 59: 2244-54 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01982
BindingDB Entry DOI: 10.7270/Q2PK0J1R
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
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 2.00E+4n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assa...


J Med Chem 52: 4911-22 (2009)

Checked by Author
Article DOI: 10.1021/jm900565c
BindingDB Entry DOI: 10.7270/Q2R49RP9
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
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 2.00E+4n/an/an/an/a



University of California

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by...


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 4


(Rattus norvegicus)
BDBM50252920
PNG
((S)-1-[2'-Amino-2'-carboxyethyl]-5,7-dihydrothieno...)
Show SMILES N[C@@H](Cn1c2CSCc2c(=O)[nH]c1=O)C(O)=O |r|
Show InChI InChI=1S/C9H11N3O4S/c10-5(8(14)15)1-12-6-3-17-2-4(6)7(13)11-9(12)16/h5H,1-3,10H2,(H,14,15)(H,11,13,16)/t5-/m0/s1
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n/an/an/an/a 2.42E+4n/an/an/an/a



European Research Centre for Drug Discovery and Development (NatSynDrugs)

Curated by ChEMBL


Assay Description
Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR4 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electro...


J Med Chem 51: 6614-8 (2008)


Article DOI: 10.1021/jm800865a
BindingDB Entry DOI: 10.7270/Q261117R
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 4


(Rattus norvegicus)
BDBM50373180
PNG
(CHEMBL260328)
Show SMILES N[C@@H]([C@@H]1CC(O)=NO1)C(O)=O |c:5|
Show InChI InChI=1S/C5H8N2O4/c6-4(5(9)10)2-1-3(8)7-11-2/h2,4H,1,6H2,(H,7,8)(H,9,10)/t2-,4-/m0/s1
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n/an/an/an/a 3.00E+4n/an/an/an/a



Universit£ degli Studi di Milano

Curated by ChEMBL


Assay Description
Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay


J Med Chem 51: 2311-5 (2008)


Article DOI: 10.1021/jm701394a
BindingDB Entry DOI: 10.7270/Q2Z320HT
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50107595
PNG
((S)-1-(2-Amino-2-carboxyethyl)-6,7-dihydro-1H-cycl...)
Show SMILES N[C@@H](Cn1c2CCCc2c(=O)[nH]c1=O)C(O)=O |r|
Show InChI InChI=1S/C10H13N3O4/c11-6(9(15)16)4-13-7-3-1-2-5(7)8(14)12-10(13)17/h6H,1-4,11H2,(H,15,16)(H,12,14,17)/t6-/m0/s1
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n/an/an/an/a 3.43E+4n/an/an/an/a



Universita' degli Studi di Siena

Curated by ChEMBL


Assay Description
The potency at recombinant rat AMPA-R was measured on GluR4 receptor expressed in Xenopus Laevis oocytes


J Med Chem 44: 4501-4 (2001)


BindingDB Entry DOI: 10.7270/Q2MC8Z9N
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 4


(Rattus norvegicus)
BDBM50107595
PNG
((S)-1-(2-Amino-2-carboxyethyl)-6,7-dihydro-1H-cycl...)
Show SMILES N[C@@H](Cn1c2CCCc2c(=O)[nH]c1=O)C(O)=O |r|
Show InChI InChI=1S/C10H13N3O4/c11-6(9(15)16)4-13-7-3-1-2-5(7)8(14)12-10(13)17/h6H,1-4,11H2,(H,15,16)(H,12,14,17)/t6-/m0/s1
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n/an/an/an/a 3.43E+4n/an/an/an/a



European Research Centre for Drug Discovery and Development (NatSynDrugs)

Curated by ChEMBL


Assay Description
Agonist activity at cyclothiazide-desensitized rat recombinant flop iGluR4c expressed in Xenopus laevis oocytes by two electrode voltage-clamp electr...


J Med Chem 51: 6614-8 (2008)


Article DOI: 10.1021/jm800865a
BindingDB Entry DOI: 10.7270/Q261117R
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 4


(Rattus norvegicus)
BDBM50295042
PNG
((S)-2-Amino-3-((RS)-3-hydroxy-8-methyl-7,8-dihydro...)
Show SMILES CC1CCC=C(C[C@H](N)C(O)=O)c2c1o[nH]c2=O |r,t:4|
Show InChI InChI=1S/C12H16N2O4/c1-6-3-2-4-7(5-8(13)12(16)17)9-10(6)18-14-11(9)15/h4,6,8H,2-3,5,13H2,1H3,(H,14,15)(H,16,17)/t6?,8-/m0/s1
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n/an/an/an/a 3.50E+4n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assa...


J Med Chem 52: 4911-22 (2009)

Checked by Author
Article DOI: 10.1021/jm900565c
BindingDB Entry DOI: 10.7270/Q2R49RP9
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50017244
PNG
((R,S)-2-amino-3-(4-bromo-3-hydroxy-5-isoxazolyl)pr...)
Show SMILES NC(Cc1o[nH]c(=O)c1Br)C(O)=O
Show InChI InChI=1S/C6H7BrN2O4/c7-4-3(13-9-5(4)10)1-2(8)6(11)12/h2H,1,8H2,(H,9,10)(H,11,12)
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n/an/an/an/a 3.80E+4n/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Effective concentration of compound was determined for electrophysiological properties on Ionotropic glutamate receptor AMPA 4 (GluR4) using rat cort...


J Med Chem 46: 2246-9 (2003)


Article DOI: 10.1021/jm020588f
BindingDB Entry DOI: 10.7270/Q26T0M06
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50002369
PNG
((2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methyleth...)
Show SMILES CC(=C)[C@H]1CN[C@@H]([C@H]1CC(O)=O)C(O)=O |r|
Show InChI InChI=1S/C10H15NO4/c1-5(2)7-4-11-9(10(14)15)6(7)3-8(12)13/h6-7,9,11H,1,3-4H2,2H3,(H,12,13)(H,14,15)/t6-,7+,9-/m0/s1
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n/an/an/an/a 4.70E+4n/an/an/an/a



University of California

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by...


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
3D
3D Structure (crystal)
Glutamate receptor 4


(Rattus norvegicus)
BDBM50002369
PNG
((2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methyleth...)
Show SMILES CC(=C)[C@H]1CN[C@@H]([C@H]1CC(O)=O)C(O)=O |r|
Show InChI InChI=1S/C10H15NO4/c1-5(2)7-4-11-9(10(14)15)6(7)3-8(12)13/h6-7,9,11H,1,3-4H2,2H3,(H,12,13)(H,14,15)/t6-,7+,9-/m0/s1
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n/an/an/an/a 4.70E+4n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assa...


J Med Chem 52: 4911-22 (2009)

Checked by Author
Article DOI: 10.1021/jm900565c
BindingDB Entry DOI: 10.7270/Q2R49RP9
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 4


(Rattus norvegicus)
BDBM50252922
PNG
((S)-1-(2'-Amino-2'-carboxyethyl)thieno[3,2-d]pyrim...)
Show SMILES N[C@@H](Cn1c2ccsc2c(=O)[nH]c1=O)C(O)=O |r|
Show InChI InChI=1S/C9H9N3O4S/c10-4(8(14)15)3-12-5-1-2-17-6(5)7(13)11-9(12)16/h1-2,4H,3,10H2,(H,14,15)(H,11,13,16)/t4-/m0/s1
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n/an/an/an/a 9.00E+4n/an/an/an/a



European Research Centre for Drug Discovery and Development (NatSynDrugs)

Curated by ChEMBL


Assay Description
Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR4 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electro...


J Med Chem 51: 6614-8 (2008)


Article DOI: 10.1021/jm800865a
BindingDB Entry DOI: 10.7270/Q261117R
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50159745
PNG
(CHEMBL3786901)
Show SMILES NCc1cccc(Cn2nnc(n2)-c2onc(O)c2C[C@H](N)C(O)=O)c1 |r|
Show InChI InChI=1S/C15H17N7O4/c16-6-8-2-1-3-9(4-8)7-22-19-13(18-21-22)12-10(14(23)20-26-12)5-11(17)15(24)25/h1-4,11H,5-7,16-17H2,(H,20,23)(H,24,25)/t11-/m0/s1
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n/an/an/an/a 1.29E+5n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at recombinant rat GluA4 receptor flip isoform expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay


J Med Chem 59: 2244-54 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01982
BindingDB Entry DOI: 10.7270/Q2PK0J1R
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor 4


(Rattus norvegicus)
BDBM50027828
PNG
((7S)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]p...)
Show SMILES [O-]C(=O)C1[NH2+]CCc2c1o[nH]c2=O
Show InChI InChI=1S/C7H8N2O4/c10-6-3-1-2-8-4(7(11)12)5(3)13-9-6/h4,8H,1-2H2,(H,9,10)(H,11,12)
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n/an/an/an/a>1.00E+6n/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluA4i expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay


J Med Chem 53: 8354-8361 (2010)


Article DOI: 10.1021/jm101218a
BindingDB Entry DOI: 10.7270/Q20Z73HW
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50373181
PNG
(CHEMBL406621)
Show SMILES N[C@H]([C@@H]1CC(O)=NO1)C(O)=O |c:5|
Show InChI InChI=1S/C5H8N2O4/c6-4(5(9)10)2-1-3(8)7-11-2/h2,4H,1,6H2,(H,7,8)(H,9,10)/t2-,4+/m0/s1
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n/an/an/an/a>1.00E+6n/an/an/an/a



Universit£ degli Studi di Milano

Curated by ChEMBL


Assay Description
Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay


J Med Chem 51: 2311-5 (2008)


Article DOI: 10.1021/jm701394a
BindingDB Entry DOI: 10.7270/Q2Z320HT
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
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+6n/an/an/an/a



Universit£ degli Studi di Milano

Curated by ChEMBL


Assay Description
Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay


J Med Chem 51: 2311-5 (2008)


Article DOI: 10.1021/jm701394a
BindingDB Entry DOI: 10.7270/Q2Z320HT
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50373179
PNG
(CHEMBL260327)
Show SMILES N[C@H]([C@H]1CC(O)=NO1)C(O)=O |c:5|
Show InChI InChI=1S/C5H8N2O4/c6-4(5(9)10)2-1-3(8)7-11-2/h2,4H,1,6H2,(H,7,8)(H,9,10)/t2-,4-/m1/s1
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n/an/an/an/a>1.00E+6n/an/an/an/a



Universit£ degli Studi di Milano

Curated by ChEMBL


Assay Description
Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay


J Med Chem 51: 2311-5 (2008)


Article DOI: 10.1021/jm701394a
BindingDB Entry DOI: 10.7270/Q2Z320HT
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50373182
PNG
(CHEMBL260122)
Show SMILES N[C@@H]([C@H]1CC(O)=NO1)C(O)=O |c:5|
Show InChI InChI=1S/C5H8N2O4/c6-4(5(9)10)2-1-3(8)7-11-2/h2,4H,1,6H2,(H,7,8)(H,9,10)/t2-,4+/m1/s1
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n/an/an/an/a>1.00E+6n/an/an/an/a



Universit£ degli Studi di Milano

Curated by ChEMBL


Assay Description
Activity at rat cloned iGluR4 expressed in human HEK293 cells by calcium imaging assay


J Med Chem 51: 2311-5 (2008)


Article DOI: 10.1021/jm701394a
BindingDB Entry DOI: 10.7270/Q2Z320HT
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50128264
PNG
((R,S)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)p...)
Show SMILES NC(Cc1o[nH]c(=O)c1Cl)C(O)=O
Show InChI InChI=1S/C6H7ClN2O4/c7-4-3(13-9-5(4)10)1-2(8)6(11)12/h2H,1,8H2,(H,9,10)(H,11,12)
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n/an/an/an/a 1.30E+6n/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Agonist activity at rat recombinant GluA4i expressed in Xenopus laevis oocytes by two-electrode voltage clamp assay


J Med Chem 53: 8354-8361 (2010)


Article DOI: 10.1021/jm101218a
BindingDB Entry DOI: 10.7270/Q20Z73HW
More data for this
Ligand-Target Pair
Glutamate receptor 4


(Rattus norvegicus)
BDBM50128264
PNG
((R,S)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)p...)
Show SMILES NC(Cc1o[nH]c(=O)c1Cl)C(O)=O
Show InChI InChI=1S/C6H7ClN2O4/c7-4-3(13-9-5(4)10)1-2(8)6(11)12/h2H,1,8H2,(H,9,10)(H,11,12)
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n/an/an/an/a 1.30E+6n/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Effective concentration of compound was determined for electrophysiological properties on Ionotropic glutamate receptor AMPA 4 (GluR4) using rat cort...


J Med Chem 46: 2246-9 (2003)


Article DOI: 10.1021/jm020588f
BindingDB Entry DOI: 10.7270/Q26T0M06
More data for this
Ligand-Target Pair