Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T54128 | Target Info | |||
| Target Name | Glutamate receptor AMPA (GRIA) | ||||
| Synonyms |
Glutamate receptor ionotropic, AMPA; Glutamate receptor; AMPA selective glutamate receptor; AMPA receptor
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| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| Biochemical Class | Chloride channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 10 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
5,7-Dichlorokynurenic Acid
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Investigative | Compound Info | ||
| Synonyms |
Dcka
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
2-Amino-3-[3-hydroxy-5-(1-methyl-1H-tetrazol-5-yl)-isoxazol-4-yl]-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL317790; SCHEMBL13319946; BDBM50059674; (RS)-2-amino-3-[3-hydroxy-5-(1-methyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid
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| Activity |
IC50 = 54000 nM
|
[2] | |||
| Compound Name |
2-Amino-3-[3-oxo-5-(2H-tetrazol-5-yl)-1,2-oxazol-4-yl]propanoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL94860; SCHEMBL7412093
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| Activity |
IC50 = 72000 nM
|
[2] | |||
| Compound Name |
(3s,4Ar,6s,8ar)-6-(2h-tetrazol-5-ylmethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL72123; SCHEMBL3690618; SCHEMBL8867563; LY-202157
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| Activity |
IC50 = 84500 nM
|
[3] | |||
| Compound Name |
alpha-Amino-3-carboxymethoxy-5-methyl-4-isoxazolepropionic acid
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Investigative | Compound Info | ||
| Synonyms |
2-amino-3-[3-(carboxymethoxy)-5-methyl-1,2-oxazol-4-yl]propanoic acid; 2-Amino-3-[3-(carboxymethoxy)-5-methylisoxazol-4-yl]propanoic acid; 2-Amoa; CHEMBL291274; SCHEMBL2036596; 3-[3-(carboxymethoxy)-5-methyl-1,2-oxazol-4-yl]alanine; DTXSID80926613; AMOA NON-NMDA GLUTAMATE RE; alpha-Amino-3-(carboxymethoxy)-5-methyl-4-isoxazolepropanoic acid; 2-Amino-3-(3-(carboxymethoxy)-5-methylisoxazol-4-yl)propionic acid; PDSP1_001840; PDSP2_001823; 2-Amino-3-[3-(carboxymethoxy)-5-methyl-4-isoxazolyl]propionic acid; 4-Isoxazolepropanoic acid, alpha-amino-3-(carboxymethoxy)-5-methyl-; (rs)-2-amino-3-[3-(carboxymethoxy)-5-methylisoxazol-4-yl]propionic acid; 4-Isoxazolepropanoic acid, alpha-amino-3-(carboxymethoxy)-5-methyl-, (+-)-
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| Activity |
IC50 = 88000 nM
|
[4] | |||
| Compound Name |
7,8-Dichlorotetrazolo[1,5-a]quinoxalin-4(5H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL112014; SCHEMBL9036984; BDBM50002695; 7,8-dichloro-5H-tetrazolo[1,5-a]quinoxalin-4-one; 7,8-Dichloro-5H-1,2,3,5,9b-pentaaza-cyclopenta[a]naphthalen-4-one
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| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3,6-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL144462
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
(3s,4Ar,6r,8ar)-6-(2h-tetrazol-5-yl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL423201; SCHEMBL3689036
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
(3s,4Ar,6s,8ar)-6-(2h-tetrazol-5-yl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL308941; SCHEMBL3687071; (?)-LY-246492
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
2-Amino-3-[5-(1-methylimidazol-2-yl)-3-oxo-1,2-oxazol-4-yl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL98723
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
alpha-Amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)methyl-5-methyl-3-oxo-4-isoxazoline-4-propionic acid
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Investigative | Compound Info | ||
| Synonyms |
2-Amnh; CHEMBL1159826; DTXSID40926614
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| Activity |
IC50 = 335000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | N-sulfonyl derivatives of 6,7-dichloro 3,4-dihydro-3-oxo-quinoxalinecarboxylate as glycine-site NMDA and AMPA antagonists. Bioorg Med Chem Lett. 1993 Jan;3(1):77-80. | ||||
| REF 2 | Heteroaryl analogues of AMPA. Synthesis and quantitative structure-activity relationships. J Med Chem. 1997 Aug 29;40(18):2831-42. | ||||
| REF 3 | (3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist. J Med Chem. 1995 Dec 8;38(25):4885-90. | ||||
| REF 4 | Novel class of amino acid antagonists at non-N-methyl-D-aspartic acid excitatory amino acid receptors. Synthesis, in vitro and in vivo pharmacology, and neuroprotection. J Med Chem. 1991 Jan;34(1):123-30. | ||||
| REF 5 | Tricyclic quinoxalines as ligands for the strychnine-insensitive glycine site. Bioorg Med Chem Lett. 1991;1(12):751-6. | ||||
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