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Compile Data Set for Download or QSAR

Found 202 hits Enz. Inhib. hit(s) with Target = 'Glutamate receptor AMPA 3/4' AND taxid = 9606   
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
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50166288
PNG
((S)-2-Amino-3-[3-hydroxy-5-(2-methyl-2H-tetrazol-5...)
Show SMILES Cn1nnc(n1)-c1o[nH]c(=O)c1C[C@H](N)C(O)=O
Show InChI InChI=1S/C8H10N6O4/c1-14-11-6(10-13-14)5-3(7(15)12-18-5)2-4(9)8(16)17/h4H,2,9H2,1H3,(H,12,15)(H,16,17)/t4-/m0/s1
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2.70n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity for ionotropic Glutamate receptor AMPA 4 expressed in Sf9 cells


J Med Chem 48: 3438-42 (2005)


Article DOI: 10.1021/jm050014l
BindingDB Entry DOI: 10.7270/Q2H70FBJ
More data for this
Ligand-Target Pair
3D
3D Structure (docked)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060628
PNG
((S)-2-Amino-3-(6-chloro-3,5-dioxo-4,5-dihydro-3H-[...)
Show SMILES N[C@@H](Cn1nc(Cl)c(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C6H7ClN4O4/c7-3-4(12)9-6(15)11(10-3)1-2(8)5(13)14/h2H,1,8H2,(H,13,14)(H,9,12,15)/t2-/m0/s1
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3.60n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060630
PNG
((S)-2-Amino-3-(6-bromo-3,5-dioxo-4,5-dihydro-3H-[1...)
Show SMILES N[C@@H](Cn1nc(Br)c(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C6H7BrN4O4/c7-3-4(12)9-6(15)11(10-3)1-2(8)5(13)14/h2H,1,8H2,(H,13,14)(H,9,12,15)/t2-/m0/s1
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7.90n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060629
PNG
((S)-2-Amino-3-(6-iodo-3,5-dioxo-4,5-dihydro-3H-[1,...)
Show SMILES N[C@@H](Cn1nc(I)c(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C6H7IN4O4/c7-3-4(12)9-6(15)11(10-3)1-2(8)5(13)14/h2H,1,8H2,(H,13,14)(H,9,12,15)/t2-/m0/s1
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20n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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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40n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 4 (GluR4) expressed in Sf 9 insect cells


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
3D
3D Structure (docked)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM17662
PNG
((2S)-2-amino-3-(3-hydroxy-5-methyl-1,2-oxazol-4-yl...)
Show SMILES Cc1o[nH]c(=O)c1C[C@H](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)/t5-/m0/s1
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40n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity for ionotropic Glutamate receptor AMPA 4 expressed in Sf9 cells


J Med Chem 48: 3438-42 (2005)


Article DOI: 10.1021/jm050014l
BindingDB Entry DOI: 10.7270/Q2H70FBJ
More data for this
Ligand-Target Pair
3D
3D Structure (docked)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50166286
PNG
((RS)-2-amino-3-[3-hydroxy-5-(2-ethyl-2H-5-tetrazol...)
Show SMILES CCn1nnc(n1)-c1o[nH]c(=O)c1CC(N)C(O)=O
Show InChI InChI=1S/C9H12N6O4/c1-2-15-12-7(11-14-15)6-4(8(16)13-19-6)3-5(10)9(17)18/h5H,2-3,10H2,1H3,(H,13,16)(H,17,18)
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44.4n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity for ionotropic Glutamate receptor AMPA 4 expressed in Sf9 cells


J Med Chem 48: 3438-42 (2005)


Article DOI: 10.1021/jm050014l
BindingDB Entry DOI: 10.7270/Q2H70FBJ
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060633
PNG
((S)-2-Amino-3-(6-methyl-3,5-dioxo-4,5-dihydro-3H-[...)
Show SMILES Cc1nn(C[C@H](N)C(O)=O)c(=O)[nH]c1=O
Show InChI InChI=1S/C7H10N4O4/c1-3-5(12)9-7(15)11(10-3)2-4(8)6(13)14/h4H,2,8H2,1H3,(H,13,14)(H,9,12,15)/t4-/m0/s1
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89n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM17662
PNG
((2S)-2-amino-3-(3-hydroxy-5-methyl-1,2-oxazol-4-yl...)
Show SMILES Cc1o[nH]c(=O)c1C[C@H](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)/t5-/m0/s1
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155n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
3D
3D Structure (docked)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50373890
PNG
(CHEMBL429594)
Show SMILES N[C@@H](Cc1ns[nH]c1=O)C(O)=O
Show InChI InChI=1S/C5H7N3O3S/c6-2(5(10)11)1-3-4(9)8-12-7-3/h2H,1,6H2,(H,8,9)(H,10,11)/t2-/m0/s1
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182n/an/an/an/an/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Binding affinity at iGluR4o receptor expressed in sf9 cells by radioligand binding assay


J Med Chem 51: 1459-63 (2008)


Article DOI: 10.1021/jm701126w
BindingDB Entry DOI: 10.7270/Q2S75H6Z
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060634
PNG
((S)-2-Amino-3-(3,5-dioxo-4,5-dihydro-3H-[1,2,4]tri...)
Show SMILES N[C@@H](Cn1ncc(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C6H8N4O4/c7-3(5(12)13)2-10-6(14)9-4(11)1-8-10/h1,3H,2,7H2,(H,12,13)(H,9,11,14)/t3-/m0/s1
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189n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060631
PNG
((S)-2-Amino-3-(5-nitro-2,4-dioxo-3,4-dihydro-2H-py...)
Show SMILES N[C@@H](Cn1cc([N+]([O-])=O)c(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C7H8N4O6/c8-3(6(13)14)1-10-2-4(11(16)17)5(12)9-7(10)15/h2-3H,1,8H2,(H,13,14)(H,9,12,15)/t3-/m0/s1
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207n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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
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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305n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060632
PNG
((S)-2-Amino-3-(5-chloro-2,4-dioxo-3,4-dihydro-2H-p...)
Show SMILES N[C@@H](Cn1cc(Cl)c(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C7H8ClN3O4/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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451n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060636
PNG
((S)-2-Amino-3-(5-bromo-2,4-dioxo-3,4-dihydro-2H-py...)
Show SMILES N[C@@H](Cn1cc(Br)c(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C7H8BrN3O4/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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457n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50091477
PNG
((S)-2-Amino-4-cyclopentylidene-pentanedioic acid |...)
Show SMILES N[C@@H](CC(C(O)=O)=C1CCCC1)C(O)=O
Show InChI InChI=1S/C10H15NO4/c11-8(10(14)15)5-7(9(12)13)6-3-1-2-4-6/h8H,1-5,11H2,(H,12,13)(H,14,15)/t8-/m0/s1
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533n/an/an/an/an/an/an/an/a



Eli Lilly and Company Ltd

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells


Bioorg Med Chem Lett 10: 1807-10 (2000)


Article DOI: 10.1016/s0960-894x(00)00346-2
BindingDB Entry DOI: 10.7270/Q2765FVB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50207594
PNG
(2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfon...)
Show SMILES NS(=O)(=O)c1cccc2c1c(cc1[nH]c(=O)c(=O)[nH]c21)[N+]([O-])=O
Show InChI InChI=1S/C12H8N4O6S/c13-23(21,22)8-3-1-2-5-9(8)7(16(19)20)4-6-10(5)15-12(18)11(17)14-6/h1-4H,(H,14,17)(H,15,18)(H2,13,21,22)
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600n/an/an/an/an/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 4


J Med Chem 45: 4383-6 (2002)


Article DOI: 10.1021/jm025548q
BindingDB Entry DOI: 10.7270/Q2XP75N4
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50166285
PNG
((RS)-2-amino-3-[3-hydroxy-5-(2-propyl-2H-5-tetrazo...)
Show SMILES CCCn1nnc(n1)-c1o[nH]c(=O)c1CC(N)C(O)=O
Show InChI InChI=1S/C10H14N6O4/c1-2-3-16-13-8(12-15-16)7-5(9(17)14-20-7)4-6(11)10(18)19/h6H,2-4,11H2,1H3,(H,14,17)(H,18,19)
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732n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity for ionotropic Glutamate receptor AMPA 4 expressed in Sf9 cells


J Med Chem 48: 3438-42 (2005)


Article DOI: 10.1021/jm050014l
BindingDB Entry DOI: 10.7270/Q2H70FBJ
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM26431
PNG
((2R)-2-aminopentanedioic acid | CHEMBL76232 | D-Gl...)
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-/m1/s1
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868n/an/an/an/an/an/an/an/a



Lilly, S.A.

Curated by ChEMBL


Assay Description
Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 4 in HEK293 cells using [3H]-AMPA as radioligand


J Med Chem 43: 1958-68 (2000)


Article DOI: 10.1021/jm9911682
BindingDB Entry DOI: 10.7270/Q2FX78QB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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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868n/an/an/an/an/an/an/an/a



Eli Lilly and Company Ltd

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells


Bioorg Med Chem Lett 10: 1807-10 (2000)


Article DOI: 10.1016/s0960-894x(00)00346-2
BindingDB Entry DOI: 10.7270/Q2765FVB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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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PubMed
868n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50060627
PNG
((S)-2-Amino-3-(5-iodo-2,4-dioxo-3,4-dihydro-2H-pyr...)
Show SMILES N[C@@H](Cn1cc(I)c(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C7H8IN3O4/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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PubMed
972n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50373889
PNG
(CHEMBL402444)
Show SMILES N[C@H](Cc1ns[nH]c1=O)C(O)=O
Show InChI InChI=1S/C5H7N3O3S/c6-2(5(10)11)1-3-4(9)8-12-7-3/h2H,1,6H2,(H,8,9)(H,10,11)/t2-/m1/s1
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PubMed
1.06E+3n/an/an/an/an/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Binding affinity at iGluR4o receptor expressed in sf9 cells by radioligand binding assay


J Med Chem 51: 1459-63 (2008)


Article DOI: 10.1021/jm701126w
BindingDB Entry DOI: 10.7270/Q2S75H6Z
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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
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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PubMed
1.71E+3n/an/an/an/an/an/an/an/a



Eli Lilly and Company Ltd

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells


Bioorg Med Chem Lett 10: 1807-10 (2000)


Article DOI: 10.1016/s0960-894x(00)00346-2
BindingDB Entry DOI: 10.7270/Q2765FVB
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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
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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1.71E+3n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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
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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PubMed
1.71E+3n/an/an/an/an/an/an/an/a



Lilly, S.A.

Curated by ChEMBL


Assay Description
Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 4 in HEK293 cells using [3H]-AMPA as radioligand


J Med Chem 43: 1958-68 (2000)


Article DOI: 10.1021/jm9911682
BindingDB Entry DOI: 10.7270/Q2FX78QB
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50166287
PNG
((RS)-2-amino-3-[3-hydroxy-5-(2-isopropyl-2H-5-tetr...)
Show SMILES CC(C)n1nnc(n1)-c1o[nH]c(=O)c1CC(N)C(O)=O
Show InChI InChI=1S/C10H14N6O4/c1-4(2)16-13-8(12-15-16)7-5(9(17)14-20-7)3-6(11)10(18)19/h4,6H,3,11H2,1-2H3,(H,14,17)(H,18,19)
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2.35E+3n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity for ionotropic Glutamate receptor AMPA 4 expressed in Sf9 cells


J Med Chem 48: 3438-42 (2005)


Article DOI: 10.1021/jm050014l
BindingDB Entry DOI: 10.7270/Q2H70FBJ
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50091473
PNG
((S)-2-Amino-4-(1-ethyl-propylidene)-pentanedioic a...)
Show SMILES CCC(CC)=C(C[C@H](N)C(O)=O)C(O)=O
Show InChI InChI=1S/C10H17NO4/c1-3-6(4-2)7(9(12)13)5-8(11)10(14)15/h8H,3-5,11H2,1-2H3,(H,12,13)(H,14,15)/t8-/m0/s1
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4.71E+3n/an/an/an/an/an/an/an/a



Eli Lilly and Company Ltd

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells


Bioorg Med Chem Lett 10: 1807-10 (2000)


Article DOI: 10.1016/s0960-894x(00)00346-2
BindingDB Entry DOI: 10.7270/Q2765FVB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50091474
PNG
((2S,4E)-2-amino-4-(2-methylpropylidene)pentanedioi...)
Show SMILES CC(C)\C=C(/C[C@H](N)C(O)=O)C(O)=O
Show InChI InChI=1S/C9H15NO4/c1-5(2)3-6(8(11)12)4-7(10)9(13)14/h3,5,7H,4,10H2,1-2H3,(H,11,12)(H,13,14)/b6-3+/t7-/m0/s1
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PubMed
5.60E+3n/an/an/an/an/an/an/an/a



Eli Lilly and Company Ltd

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells


Bioorg Med Chem Lett 10: 1807-10 (2000)


Article DOI: 10.1016/s0960-894x(00)00346-2
BindingDB Entry DOI: 10.7270/Q2765FVB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM17661
PNG
((2S)-2-amino-3-(2,4-dioxo-1,2,3,4-tetrahydropyrimi...)
Show SMILES N[C@@H](Cn1ccc(=O)[nH]c1=O)C(O)=O
Show InChI InChI=1S/C7H9N3O4/c8-4(6(12)13)3-10-2-1-5(11)9-7(10)14/h1-2,4H,3,8H2,(H,12,13)(H,9,11,14)/t4-/m0/s1
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8.85E+3n/an/an/an/an/an/an/an/a



University of Bristol

Curated by ChEMBL


Assay Description
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells


J Med Chem 40: 3645-50 (1997)


Article DOI: 10.1021/jm9702387
BindingDB Entry DOI: 10.7270/Q28G8MCB
More data for this
Ligand-Target Pair
GRIA4


(Homo sapiens)
BDBM86751
PNG
(CHEMBL14935 | LY 293558 | LY-293558)
Show SMILES OC(=O)[C@@H]1C[C@H]2C[C@@H](CCc3nnn[nH]3)CC[C@H]2CN1
Show InChI InChI=1S/C13H21N5O2/c19-13(20)11-6-10-5-8(1-3-9(10)7-14-11)2-4-12-15-17-18-16-12/h8-11,14H,1-7H2,(H,19,20)(H,15,16,17,18)/t8-,9+,10-,11+/m1/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Eli Lilly and Company

Curated by PDSP Ki Database




J Pharmacol Exp Ther 318: 772-81 (2006)


Article DOI: 10.1124/jpet.106.101428
BindingDB Entry DOI: 10.7270/Q2NP230D
More data for this
Ligand-Target Pair
GRIA4


(Homo sapiens)
BDBM50168962
PNG
((3S,4aR,6S,8aR)-6-(4-Carboxy-benzyl)-decahydro-iso...)
Show SMILES OC(=O)[C@@H]1C[C@H]2C[C@@H](Cc3ccc(cc3)C(O)=O)CC[C@H]2CN1
Show InChI InChI=1S/C18H23NO4/c20-17(21)13-4-1-11(2-5-13)7-12-3-6-14-10-19-16(18(22)23)9-15(14)8-12/h1-2,4-5,12,14-16,19H,3,6-10H2,(H,20,21)(H,22,23)/t12-,14+,15-,16+/m1/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Eli Lilly and Company

Curated by PDSP Ki Database




J Pharmacol Exp Ther 318: 772-81 (2006)


Article DOI: 10.1124/jpet.106.101428
BindingDB Entry DOI: 10.7270/Q2NP230D
More data for this
Ligand-Target Pair
GRIA4


(Homo sapiens)
BDBM86754
PNG
(LY 466195 | LY-466195)
Show SMILES OC(=O)C1CC(F)(F)CN1C[C@H]1CC[C@H]2CN[C@@H](C[C@H]2C1)C(O)=O
Show InChI InChI=1S/C16H24F2N2O4/c17-16(18)5-13(15(23)24)20(8-16)7-9-1-2-10-6-19-12(14(21)22)4-11(10)3-9/h9-13,19H,1-8H2,(H,21,22)(H,23,24)/t9-,10-,11+,12-,13?/m0/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Eli Lilly and Company

Curated by PDSP Ki Database




J Pharmacol Exp Ther 318: 772-81 (2006)


Article DOI: 10.1124/jpet.106.101428
BindingDB Entry DOI: 10.7270/Q2NP230D
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50088222
PNG
((2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pe...)
Show SMILES N[C@@H](C[C@@H](C\C=C\c1ccc2ccccc2c1)C(O)=O)C(O)=O
Show InChI InChI=1S/C18H19NO4/c19-16(18(22)23)11-15(17(20)21)7-3-4-12-8-9-13-5-1-2-6-14(13)10-12/h1-6,8-10,15-16H,7,11,19H2,(H,20,21)(H,22,23)/b4-3+/t15-,16+/m1/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Lilly, S.A.

Curated by ChEMBL


Assay Description
Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 4 in HEK293 cells using [3H]-AMPA as radioligand


J Med Chem 43: 1958-68 (2000)


Article DOI: 10.1021/jm9911682
BindingDB Entry DOI: 10.7270/Q2FX78QB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50088216
PNG
(CHEMBL59284 | E-2-Amino-4-[3-(2-methoxy-phenyl)-al...)
Show SMILES COc1ccccc1\C=C\C[C@H](C[C@H](N)C(O)=O)C(O)=O
Show InChI InChI=1S/C15H19NO5/c1-21-13-8-3-2-5-10(13)6-4-7-11(14(17)18)9-12(16)15(19)20/h2-6,8,11-12H,7,9,16H2,1H3,(H,17,18)(H,19,20)/b6-4+/t11-,12+/m1/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Lilly, S.A.

Curated by ChEMBL


Assay Description
Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 4 in HEK293 cells using [3H]-AMPA as radioligand


J Med Chem 43: 1958-68 (2000)


Article DOI: 10.1021/jm9911682
BindingDB Entry DOI: 10.7270/Q2FX78QB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50088222
PNG
((2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pe...)
Show SMILES N[C@@H](C[C@@H](C\C=C\c1ccc2ccccc2c1)C(O)=O)C(O)=O
Show InChI InChI=1S/C18H19NO4/c19-16(18(22)23)11-15(17(20)21)7-3-4-12-8-9-13-5-1-2-6-14(13)10-12/h1-6,8-10,15-16H,7,11,19H2,(H,20,21)(H,22,23)/b4-3+/t15-,16+/m1/s1
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>1.00E+4n/an/an/an/an/an/an/an/a



Eli Lilly and Company Ltd

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells


Bioorg Med Chem Lett 10: 1807-10 (2000)


Article DOI: 10.1016/s0960-894x(00)00346-2
BindingDB Entry DOI: 10.7270/Q2765FVB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50091475
PNG
((2S,4Z)-2-amino-4-(2-methylpropylidene)pentanedioi...)
Show SMILES CC(C)\C=C(\C[C@H](N)C(O)=O)C(O)=O
Show InChI InChI=1S/C9H15NO4/c1-5(2)3-6(8(11)12)4-7(10)9(13)14/h3,5,7H,4,10H2,1-2H3,(H,11,12)(H,13,14)/b6-3-/t7-/m0/s1
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1.03E+4n/an/an/an/an/an/an/an/a



Eli Lilly and Company Ltd

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells


Bioorg Med Chem Lett 10: 1807-10 (2000)


Article DOI: 10.1016/s0960-894x(00)00346-2
BindingDB Entry DOI: 10.7270/Q2765FVB
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
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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1.17E+4n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 4 (GluR4) expressed in Sf 9 insect cells


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 ionotropic AMPA


(Homo sapiens)
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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1.19E+4n/an/an/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 4 (GluR4) expressed in Sf 9 insect cells


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 ionotropic AMPA


(Homo sapiens)
BDBM86751
PNG
(CHEMBL14935 | LY 293558 | LY-293558)
Show SMILES OC(=O)[C@@H]1C[C@H]2C[C@@H](CCc3nnn[nH]3)CC[C@H]2CN1
Show InChI InChI=1S/C13H21N5O2/c19-13(20)11-6-10-5-8(1-3-9(10)7-14-11)2-4-12-15-17-18-16-12/h8-11,14H,1-7H2,(H,19,20)(H,15,16,17,18)/t8-,9+,10-,11+/m1/s1
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5.00E+4n/an/an/an/an/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 4


J Med Chem 45: 4383-6 (2002)


Article DOI: 10.1021/jm025548q
BindingDB Entry DOI: 10.7270/Q2XP75N4
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM86751
PNG
(CHEMBL14935 | LY 293558 | LY-293558)
Show SMILES OC(=O)[C@@H]1C[C@H]2C[C@@H](CCc3nnn[nH]3)CC[C@H]2CN1
Show InChI InChI=1S/C13H21N5O2/c19-13(20)11-6-10-5-8(1-3-9(10)7-14-11)2-4-12-15-17-18-16-12/h8-11,14H,1-7H2,(H,19,20)(H,15,16,17,18)/t8-,9+,10-,11+/m1/s1
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5.05E+4n/an/an/an/an/an/an/an/a



Novartis Pharma AG

Curated by ChEMBL


Assay Description
Binding affinity to GluR4


J Med Chem 53: 5367-82 (2010)


Article DOI: 10.1021/jm901688m
BindingDB Entry DOI: 10.7270/Q2FX79NV
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50118701
PNG
(6-(4-Carboxy-imidazol-1-ylmethyl)-decahydro-isoqui...)
Show SMILES OC(=O)[C@@H]1C[C@H]2C[C@@H](Cn3cnc(c3)C(O)=O)CC[C@H]2CN1
Show InChI InChI=1S/C15H21N3O4/c19-14(20)12-4-11-3-9(1-2-10(11)5-16-12)6-18-7-13(15(21)22)17-8-18/h7-12,16H,1-6H2,(H,19,20)(H,21,22)/t9-,10-,11+,12-/m0/s1
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2.62E+5n/an/an/an/an/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 4


J Med Chem 45: 4383-6 (2002)


Article DOI: 10.1021/jm025548q
BindingDB Entry DOI: 10.7270/Q2XP75N4
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50316373
PNG
(Argiotoxin-636 | CHEMBL1098240)
Show SMILES N[C@@H](CCCN=C(N)N)C(=O)NCCCNCCCNCCCCCNC(=O)[C@H](CC(N)=O)NC(=O)Cc1ccc(O)cc1O
Show InChI InChI=1S/C29H52N10O6/c30-22(7-4-15-38-29(32)33)27(44)36-16-6-13-35-12-5-11-34-10-2-1-3-14-37-28(45)23(19-25(31)42)39-26(43)17-20-8-9-21(40)18-24(20)41/h8-9,18,22-23,34-35,40-41H,1-7,10-17,19,30H2,(H2,31,42)(H,36,44)(H,37,45)(H,39,43)(H4,32,33,38)/t22-,23-/m0/s1
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n/an/a 430n/an/an/an/an/an/a



University of California

Curated by ChEMBL


Assay Description
Inhibition of GluA4 receptor expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiologica...


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 ionotropic AMPA


(Homo sapiens)
BDBM50207594
PNG
(2,3-Dihydroxy-6-nitro-benzo[f]quinoxaline-7-sulfon...)
Show SMILES NS(=O)(=O)c1cccc2c1c(cc1[nH]c(=O)c(=O)[nH]c21)[N+]([O-])=O
Show InChI InChI=1S/C12H8N4O6S/c13-23(21,22)8-3-1-2-5-9(8)7(16(19)20)4-6-10(5)15-12(18)11(17)14-6/h1-4H,(H,14,17)(H,15,18)(H2,13,21,22)
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n/an/a 1.10E+3n/an/an/an/an/an/a



University Walk

Curated by ChEMBL


Assay Description
Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA4


J Med Chem 49: 2579-92 (2006)


Article DOI: 10.1021/jm051086f
BindingDB Entry DOI: 10.7270/Q2FQ9W76
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50137125
PNG
(2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid |...)
Show SMILES OC(=O)c1ccc(Cl)cc1NC(=O)Nc1cccc(Br)c1
Show InChI InChI=1S/C14H10BrClN2O3/c15-8-2-1-3-10(6-8)17-14(21)18-12-7-9(16)4-5-11(12)13(19)20/h1-7H,(H,19,20)(H2,17,18,21)
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n/an/a>1.00E+5n/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
In vitro inhibitory activity of the compound against Ionotropic glutamate receptor AMPA 4 of HEK293 cells in FLIPR assay


J Med Chem 46: 5834-43 (2003)


Article DOI: 10.1021/jm030428j
BindingDB Entry DOI: 10.7270/Q2KK9B60
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50137124
PNG
(4-Chloro-2-(3-naphthalen-2-yl-ureido)-benzoic acid...)
Show SMILES OC(=O)c1ccc(Cl)cc1NC(=O)Nc1ccc2ccccc2c1
Show InChI InChI=1S/C18H13ClN2O3/c19-13-6-8-15(17(22)23)16(10-13)21-18(24)20-14-7-5-11-3-1-2-4-12(11)9-14/h1-10H,(H,22,23)(H2,20,21,24)
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n/an/a>1.00E+5n/an/an/an/an/an/a



The Danish University of Pharmaceutical Sciences

Curated by ChEMBL


Assay Description
In vitro inhibitory activity of the compound against Ionotropic glutamate receptor AMPA 4 of HEK293 cells in FLIPR assay


J Med Chem 46: 5834-43 (2003)


Article DOI: 10.1021/jm030428j
BindingDB Entry DOI: 10.7270/Q2KK9B60
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50094012
PNG
(CHEMBL137798 | N-[2-(2'-Fluoro-biphenyl-4-yl)-prop...)
Show SMILES CC(CNS(=O)(=O)c1ccccc1)c1ccc(cc1)-c1ccccc1F
Show InChI InChI=1S/C21H20FNO2S/c1-16(15-23-26(24,25)19-7-3-2-4-8-19)17-11-13-18(14-12-17)20-9-5-6-10-21(20)22/h2-14,16,23H,15H2,1H3
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n/an/an/an/a 6.25E+4n/an/an/an/a



NPS Allelix Corporation

Curated by ChEMBL


Assay Description
Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells


J Med Chem 43: 4354-8 (2000)


Article DOI: 10.1021/jm0002836
BindingDB Entry DOI: 10.7270/Q2R2123P
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50094013
PNG
(CHEMBL137359 | Propane-2-sulfonic acid [2-(2'-fluo...)
Show SMILES CC(C)S(=O)(=O)NCCc1ccc(cc1)-c1ccccc1F
Show InChI InChI=1S/C17H20FNO2S/c1-13(2)22(20,21)19-12-11-14-7-9-15(10-8-14)16-5-3-4-6-17(16)18/h3-10,13,19H,11-12H2,1-2H3
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n/an/an/an/a 7.20E+3n/an/an/an/a



NPS Allelix Corporation

Curated by ChEMBL


Assay Description
Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells


J Med Chem 43: 4354-8 (2000)


Article DOI: 10.1021/jm0002836
BindingDB Entry DOI: 10.7270/Q2R2123P
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50094014
PNG
(CHEMBL334464 | Propane-2-sulfonic acid [2-(4'-trif...)
Show SMILES CC(C)S(=O)(=O)NCC(C)c1ccc(cc1)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C19H22F3NO2S/c1-13(2)26(24,25)23-12-14(3)15-4-6-16(7-5-15)17-8-10-18(11-9-17)19(20,21)22/h4-11,13-14,23H,12H2,1-3H3
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n/an/an/an/a>3.00E+3n/an/an/an/a



NPS Allelix Corporation

Curated by ChEMBL


Assay Description
Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells


J Med Chem 43: 4354-8 (2000)


Article DOI: 10.1021/jm0002836
BindingDB Entry DOI: 10.7270/Q2R2123P
More data for this
Ligand-Target Pair
Glutamate receptor ionotropic AMPA


(Homo sapiens)
BDBM50094016
PNG
(CHEMBL343571 | Propane-2-sulfonic acid [2-(4'-meth...)
Show SMILES CC(C)S(=O)(=O)NCC(C)c1ccc(cc1)-c1ccc(C)cc1
Show InChI InChI=1S/C19H25NO2S/c1-14(2)23(21,22)20-13-16(4)17-9-11-19(12-10-17)18-7-5-15(3)6-8-18/h5-12,14,16,20H,13H2,1-4H3
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n/an/an/an/a 270n/an/an/an/a



NPS Allelix Corporation

Curated by ChEMBL


Assay Description
Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells


J Med Chem 43: 4354-8 (2000)


Article DOI: 10.1021/jm0002836
BindingDB Entry DOI: 10.7270/Q2R2123P
More data for this
Ligand-Target Pair
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