Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T96235 | Target Info | |||
| Target Name | Glutamate receptor AMPA 4 (GRIA4) | ||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 4; GluRD; GluR4; GluA4; GRIA4; AMPAselective glutamate receptor 4
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| Target Type | Successful Target | ||||
| Gene Name | GRIA4 | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 13 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
CX-516
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Phase 2/3 | Compound Info | ||
| Synonyms |
Ampalex; BDP 12; CX 516; CX516; BDP-12; SPD-420; Piperidin-1-yl(quinoxalin-6-yl)methanone; 1-(6-Quinoxalinylcarbonyl)piperidine; 1-(6-quinoxalinylcarbonyl)-Piperidine; 1-(quinoxalin-6-ylcarbonyl)piperidine; 6-(piperidin-1-ylcarbonyl)quinoxaline
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| Activity |
EC50 = 156000 nM
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[1] | |||
| 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 |
Ki = 50000 nM
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[2] | |||
| Compound Name |
2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL154700; 2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid; SCHEMBL6431740; ZINC1491954; BDBM50137125; AKOS012857302; 2-[3-(3-Bromo-phenyl)-ureido]-4-chloro-benzoic acid
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
N-[2-[4-(2-Fluorophenyl)phenyl]propyl]benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL137798; SCHEMBL5878210; BDBM50094012; N-[2-(2'-Fluoro-4-biphenylyl)propyl]benzenesulfonamide; N-[2-(2''-Fluoro-biphenyl-4-yl)-propyl]-benzenesulfonamide
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| Activity |
EC50 = 62500 nM
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[4] | |||
| Compound Name |
(RS)-2-amino-3-[3-hydroxy-5-(2-benzyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL388746; BDBM50211399
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| Activity |
EC50 = 75000 nM
|
[5] | |||
| Compound Name |
(RS)-2-amino-3-[3-hydroxy-5-(2-propyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL372643; BDBM50166285; 2-amino-3-(3-hydroxy-5-(2-propyl-2H-tetrazol-5-yl)isoxazol-4-yl)propanoic acid; 2-Amino-3-[3-hydroxy-5-(2-propyl-2H-tetrazol-5-yl)-isoxazol-4-yl]-propionic acid
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| Activity |
EC50 = 79000 nM
|
[5] | |||
| Compound Name |
2-[4-(2-Fluorophenyl)phenyl]propan-1-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL337103; SCHEMBL5878471; BDBM50094015; 2-(2''-Fluoro-biphenyl-4-yl)-propylamine
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| Activity |
EC50 ~ 100000 nM
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[4] | |||
| Compound Name |
N-[2-(2'-Fluoro-4-biphenylyl)propyl]-1-butanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL136750; BDBM50094025; Butane-1-sulfonic acid [2-(2''-fluoro-biphenyl-4-yl)-propyl]-amide
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| Activity |
EC50 ~ 100000 nM
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[4] | |||
| Compound Name |
N-(beta-Phenethyl-4-tert-butylphenethyl)-2-propanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL136888; BDBM50094027; Propane-2-sulfonic acid [2-(4-tert-butyl-phenyl)-4-phenyl-butyl]-amide
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| Activity |
EC50 ~ 100000 nM
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[4] | |||
| Compound Name |
4-Chloro-2-(naphthalen-2-ylcarbamoylamino)benzoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL346524; SCHEMBL3959804; CTK2A8003; DTXSID90436076; BDBM50137124; ZINC13531921; 4-chloro-2-(3-(naphthalen-2-yl)ureido)benzoic acid; 4-Chloro-2-(3-naphthalen-2-yl-ureido)-benzoic acid; Benzoic acid, 4-chloro-2-[[(2-naphthalenylamino)carbonyl]amino]-
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
N-[2-(2'-Fluoro-4-biphenylyl)propyl]phenylmethanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL136761; BDBM50094021; N-[2-(2''-Fluoro-biphenyl-4-yl)-propyl]-C-phenyl-methanesulfonamide
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| Activity |
EC50 ~ 100000 nM
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[4] | |||
| Compound Name |
N-(beta-Benzyl-4-tert-butylphenethyl)-2-propanesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL342853; BDBM50094035; Propane-2-sulfonic acid [2-(4-tert-butyl-phenyl)-3-phenyl-propyl]-amide
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-Amino-3-(3-hydroxy-5-(2-isopropyl-2H-tetrazol-5-yl)isoxazol-4-yl)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL193087; BDBM50166287; (RS)-2-amino-3-[3-hydroxy-5-(2-isopropyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid; 2-Amino-3-[3-hydroxy-5-(2-isopropyl-2H-tetrazol-5-yl)-isoxazol-4-yl]-propionic acid
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| Activity |
EC50 = 160000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
L-Glutamic Acid
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Approved | Compound Info | ||
| Synonyms |
Aciglut; Glu; Glusate; Glut; Glutacid; Glutamicol; Glutamidex; Glutaminol; Glutaton; Gulutamine; Acide glutamique; Acido glutamico; Acidum glutamicum; Acidum glutaminicum; Glutamic acid polymer; Glutaminic acid; E 620; A-Aminoglutaric acid; A-Glutamic acid; Acide glutamique [INN-French]; Acido glutamico [INN-Spanish]; Acidum glutamicum [INN-Latin]; D-Glutamiensuur; Glutamic Acid [USAN:INN]; Glutamic acid (VAN); Glutaminic acid (VAN); Gulutamine (USP); L-Glutamic acid hydrochloride; L-Glutaminic acid; L-Glutaminsaeure; L-glu; L-glutamate; Alpha-Aminoglutaric acid (VAN); Alpha-L-Glutamic acid polymer; Glutamic Acid (L-glutamic acid); Glutamic acid (H-3); H-Glu-OH; L-2-Aminoglutaric acid; L-Glutamic acid (9CI); L-Glutamic acid (JAN); L-Glutamic acid, homopolymer; L-a-Aminoglutaric acid; L-alpha-Aminoglutaric acid; Poly-L-glutamate; Sodium Glutamate (L-glutamic Acid); Glutamic acid, L-, peptides; L-Glutamic acid, homopolymer (9CI); Poly(alpha-L-glutamic acid); Glutamic acid, L-(7CI,8CI); L-(+)-glutamic acid; (S)-(+)-Glutamic acid; (S)-2-Aminopentanedioic acid; (S)-Glutamic acid; 1-Aminopropane-1,3-dicarboxylic acid
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| Activity |
EC50 = 3.98E+13 nM
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[5] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-[(4-carboxyimidazol-1-yl)methyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;dihydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL542242
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| Activity |
Ki = 262000 nM
|
[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 |
EC50 = 3000000 nM
|
[5] | |||
| Compound Name |
2-Amino-3-(5-(2-ethyl-2H-tetrazol-5-yl)-3-hydroxyisoxazol-4-yl)propanoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL370941; BDBM50166286; (RS)-2-amino-3-[3-hydroxy-5-(2-ethyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid; 2-Amino-3-[5-(2-ethyl-2H-tetrazol-5-yl)-3-hydroxy-isoxazol-4-yl]-propionic acid
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| Activity |
EC50 = 2.51E+14 nM
|
[5] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Positive allosteric modulators of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. J Med Chem. 2010 Oct 28;53(20):7271-9. | ||||
| REF 2 | Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine. J Med Chem. 2002 Sep 26;45(20):4383-6. | ||||
| REF 3 | 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5. J Med Chem. 2003 Dec 18;46(26):5834-43. | ||||
| REF 4 | Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors. J Med Chem. 2000 Nov 16;43(23):4354-8. | ||||
| REF 5 | Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA. J Med Chem. 2007 Aug 23;50(17):4177-85. | ||||
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