Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T87588 | Target Info | |||
| Target Name | Glutamate receptor ionotropic kainate 4 (GluK4) | ||||
| Synonyms |
KA1; Glutamate receptor ionotropic, kainate 4; Glutamate receptor KA-1; GluK4; GRIK; Excitatory amino acid receptor 1; EAA1
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| Target Type | Literature-reported Target | ||||
| Gene Name | GRIK4 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 12 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-oxo-5-(1H-1,2,4-triazol-5-yl)-1,2-oxazol-4-yl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL318467
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| Activity |
IC50 = 58000 nM
|
[2] | |||
| 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 = 74000 nM
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[2] | |||
| 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 ~ 100000 nM
|
[2] | |||
| 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-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 ~ 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-[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 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-Amino-3-[5-(1-methyl-1,2,4-triazol-3-yl)-3-oxo-1,2-oxazol-4-yl]propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL441460
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-Amino-3-[5-(1H-imidazol-2-yl)-3-oxo-1,2-oxazol-4-yl]propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL97742
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
6,7-Dichloro-N-methylsulfonyl-3-oxo-4H-quinoxaline-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL167548; SCHEMBL9704360
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| Activity |
IC50 = 103000 nM
|
[1] | |||
| Compound Name |
Click to Show/Hide
|
Compound Info | |||
| Activity |
IC50 = 68000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
LY293558
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|
Phase 2 | Compound Info | ||
| Synonyms |
Tezampanel; 154652-83-2; LY-293558; LY293558; Ted-isoquinoline-3-cooh; LY 293558; UNII-GA36S2O9C2; CHEMBL14935; GA36S2O9C2; 150131-78-5; Decahydro-6-(2-(1H-tetrazol-5-yl)ethyl)-3-isoquinolinecarboxylic acid; 6-(2-(1H-Tetrazol-5-yl)ethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid; 3-Isoquinolinecarboxylic acid, decahydro-6-(2-(1H-tetrazol-5-yl)ethyl)-, (3S,4aR,6R,8aR)-; 3-Isoquinolinecarboxylic acid, decahydro-6-(2-(1H-tetrazol-5-yl)ethyl)-, (3S-(3alpha,4aalpha,6beta,8aalpha))-; Tezampanel [INN]
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| Activity |
IC50 = 247000 nM
|
[3] | |||
| Compound Name |
(3S,4Ar,6R,8aR)-6-[2-(4H-triazol-5-yl)ethyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL62809
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| Activity |
IC50 = 247000 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 | (3SR,4aRS,6RS,8aRS)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3 - carboxylic acid: a structurally novel, systemically active, competitive AMPA receptor antagonist. J Med Chem. 1993 Jul 9;36(14):2046-8. | ||||
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