Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T58178 | Target Info | |||
| Target Name | Glutamate receptor ionotropic kainate 2 (GRIK2) | ||||
| Synonyms |
Glutamate receptor ionotropic, kainate 2; Glutamate receptor 6; GluR6; GluR-6; GluK2; Excitatory amino acid receptor 4; EAA4
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| Target Type | Literature-reported Target | ||||
| Gene Name | GRIK2 | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 37 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 |
Ki ~ 100000 nM
|
[1] | |||
| Compound Name |
NBQX
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Phase 1 | Compound Info | ||
| Synonyms |
nbqx; 118876-58-7; FG 9202; 2,3-Dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline; 2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline; 6-Nitro-7-sulfamoylbenzo(f)quinoxaline-2,3-dione; CHEMBL222519; CHEBI:31073; SBB066176; 6-nitro-2,3-dioxo-1,4-dihydrobenzo[f]quinoxaline-7-sulfonamide; 1,2,3,4-Tetrahydro-6-nitro-2,3-dioxobenzo(f)quinoxaline-8-sulfonamide; 6-Nitro-7-sulphamoylbenzo[f]quinoxaline-2,3-dione; 6-Nitro-7-sulfamoylbenzo[f]quinoxaline-2,3-Dione; 2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(f)quinoxaline
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| Activity |
Ki ~ 100000 nM
|
[2] | |||
| Compound Name |
LY525327
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Terminated | Compound Info | ||
| Synonyms |
CHEMBL187941; BDBM86753; BDBM50168966; LY-525327; LY 525327; LS-193664; (3S,4aR,6S,8aR)-6-[2-(1H-Tetrazol-5-yl)-phenylamino]-decahydro-isoquinoline-3-carboxylic acid 2-ethyl-butyl ester
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
ACET
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL373429; 3-({3-[(2s)-2-Amino-2-Carboxyethyl]-5-Methyl-2,6-Dioxo-3,6-Dihydropyrimidin-1(2h)-Yl}methyl)-5-Phenylthiophene-2-Carboxylic Acid; (S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxy-5-phenylthiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione; GTPL4123; MolPort-023-276-559; ZINC35324127; BDBM50207591; AKOS024457262; NCGC00378702-01; UBE; 3-({3-[(2S)-2-amino-2-carboxyethyl]-5-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-1-yl}methyl)-5-phenylthiophene-2-carboxylic acid
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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
UBP310
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Investigative | Compound Info | ||
| Synonyms |
(S)-1-(2-Amino-2-carboxyethyl)-3(2-carboxythiophene-3-YL-methyl)-5-methylpyrimidine-2,4-dione; UBP 310; UBP-310; CHEMBL373428; (S)-1-(2-AMINO-2-CARBOXYETHYL)-3(2-CARBOXYTHIOPHENE-3-YL-METHYL)-5-METHYLPYRIMIDINE-2,4-DIONE; UBA; 3-[[3-[(2S)-2-amino-3-hydroxy-3-oxopropyl]-5-methyl-2,6-dioxopyrimidin-1-yl]methyl]thiophene-2-carboxylic acid; [3H]UBP310; AC1O4WKX; GTPL4334; GTPL4092; SCHEMBL15959446; ZTAZUCRXCRXNSU-VIFPVBQESA-N; MolPort-006-069-045; 2f34; ZINC16052001; BDBM50207593; AKOS024457719; NCGC00370889-01; UBP-310
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
LY382884
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Investigative | Compound Info | ||
| Synonyms |
LY-382884; LY 382884
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
{2-[3-(3-Bromophenyl)ureido]-4-chlorophenyl}acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL224688; SCHEMBL3965634; BDBM50158554; {2-[3-(3-Bromo-phenyl)-ureido]-4-chloro-phenyl}-acetic acid; 2-[2-[(3-bromophenyl)carbamoylamino]-4-chlorophenyl]acetic acid
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| Activity |
IC50 ~ 50000 nM
|
[5] | |||
| Compound Name |
(S)-2-Amino-4-butylidene-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL50041; SCHEMBL8404045; SCHEMBL8404046; BDBM50091485
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| Activity |
Ki = 57200 nM
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[6] | |||
| Compound Name |
2-Amino-4-but-2-enyl-pentanedioic acid(LY339180)
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL294139; BDBM50088212; LY-339180
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| Activity |
EC50 = 58300 nM
|
[7] | |||
| 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 = 62000 nM
|
[5] | |||
| Compound Name |
2-Amino-4-hex-2-ynyl-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL302402; SCHEMBL7780779; ZINC1903205; BDBM50088210; (2S,4R)-2-amino-4-hex-2-ynylpentanedioic acid
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| Activity |
Ki = 68547 nM
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[7] | |||
| Compound Name |
(2S,4R)-2-Amino-4-[(E)-3-(4-chlorophenyl)prop-2-enyl]pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL58590; LY-339295; BDBM50088197; ZINC13808423; E-2-Amino-4-[3-(4-chloro-phenyl)-allyl]-pentanedioic acid(LY339295)
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| Activity |
EC50 = 70800 nM
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[7] | |||
| Compound Name |
(2S,4E)-2-Amino-4-(2-methylpropylidene)pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
LY-339637; CHEMBL299180; SCHEMBL8401765; BDBM50091474
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| Activity |
Ki = 82500 nM
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[6] | |||
| Compound Name |
4-[(E)-Cyclopentylmethylene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL299291; SCHEMBL8403440; BDBM50091488; (2S,4E)-2-amino-4-(cyclopentylmethylidene)pentanedioic acid; (S)-2-Amino-4-[1-cyclopentyl-meth-(E)-ylidene]-pentanedioic acid
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| Activity |
Ki = 87600 nM
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[6] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-[2-(1H-Tetrazol-5-yl)-phenoxy]-decahydro-isoquinoline-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL189985; SCHEMBL13390159; BDBM86755; BDBM50168965; LY 458545; LY-458545
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| Activity |
Ki ~ 100000 nM
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[3] | |||
| Compound Name |
4-[(E)-2,2-Dimethylcyclopentylidene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL51395; BDBM50091494; (S)-2-Amino-4-[2,2-dimethyl-cyclopent-(E)-ylidene]-pentanedioic acid
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| Activity |
Ki ~ 100000 nM
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[6] | |||
| 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 |
Ki ~ 100000 nM
|
[8] | |||
| Compound Name |
(S)-2-Amino-4-cyclopentylidene-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL51660; LY-339624; SCHEMBL8403414; BDBM50091477; (2S)-2-amino-4-cyclopentylidenepentanedioic acid
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| Activity |
Ki ~ 100000 nM
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[6] | |||
| Compound Name |
4-[(E)-2,2-Dimethylpropylidene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL52742; BDBM50091479; (S)-2-Amino-4-(2,2-dimethyl-propylidene)-pentanedioic acid
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| Activity |
Ki ~ 100000 nM
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[6] | |||
| Compound Name |
4-Cyclobutylidene-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL51054; SCHEMBL8403565; BDBM50091486; (2S)-2-amino-4-cyclobutylidenepentanedioic acid; (S)-2-Amino-4-cyclobutylidene-pentanedioic acid
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| Activity |
Ki ~ 100000 nM
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[6] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-[2-(1H-Tetrazol-5-yl)-phenoxy]-decahydro-isoquinoline-3-carboxylic acid isobutyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL189721; BDBM50168963
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| Activity |
Ki ~ 100000 nM
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[3] | |||
| Compound Name |
(2s)-2-Amino-3-(4-Hydroxy-1,2,5-Thiadiazol-3-Yl)propanoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL429594; BDBM50373890; 3-(4-hydroxy-1,2,5-thiadiazol-3-yl)-L-alanine; 3-(4-Hydroxy-1,2,5-thiadiazole-3-yl)-L-alanine; Q27465224
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| Activity |
Ki ~ 100000 nM
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[9] | |||
| Compound Name |
4-[(1E,2E)-3-Phenyl-2-propene-1-ylidene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL53194; SCHEMBL8403451; BDBM50091476; (2S,4E)-2-amino-4-[(E)-3-phenylprop-2-enylidene]pentanedioic acid; (S)-2-Amino-4-[(E)-3-phenyl-prop-2-en-(E)-ylidene]-pentanedioic acid
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| Activity |
Ki ~ 100000 nM
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[6] | |||
| 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 |
Ki ~ 100000 nM
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[8] | |||
| Compound Name |
(2S,4R)-2-Amino-4-[(E)-3-naphthalen-2-ylprop-2-enyl]pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
LY-339434; CHEMBL301536; SCHEMBL5958122; ZINC1545895; BDBM50088222; (2S,4R,6E)-2-amino-4-carboxy-7-(2-naphthyl)hept-6-enoic acid; (2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pentanedioic acid; E-2-Amino-4-(3-naphthalen-2-yl-allyl)-pentanedioic acid(LY339434)
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| Activity |
EC50 ~ 100000 nM
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[10] | |||
| 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 |
Ki ~ 100000 nM
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[8] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-[2-(1H-Tetrazol-5-yl)-phenylamino]-decahydro-isoquinoline-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL191249; BDBM86749; BDBM50168964; LY 457691
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| Activity |
Ki ~ 100000 nM
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[3] | |||
| Compound Name |
2-Amino-3-(4-bromo-3-hydroxyisoxazol-5-YL)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL73698; (RS)-4-Bromo-homo-ibotenic acid; (S)-2-AMINO-3-(4-BROMO-3-HYDROXY-ISOXAZOL-5-YL)PROPIONIC ACID; Bromohomoibotenic acid; 2-amino-3-(4-bromo-3-oxo-1,2-oxazol-5-yl)propanoic acid; SCHEMBL5280594; SCHEMBL13957643; CTK5E3726; DTXSID30991699; (+/-)-4-Bromohomoibotenic acid; BDBM50017244; AB44069; (+/-)-4-Bromohomoibotenic acid, solid; ST50405217; 3-(4-Bromo-3-hydroxy-1,2-oxazol-5-yl)alanine; Q27458524; 2-azaniumyl-3-(4-bromo-3-oxo-1,2-oxazol-5-yl)propanoate; 2-Amino-3-(4-bromo-3-hydroxy-isoxazol-5-yl)-propionic acid; 5-Isoxazolepropanoicacid, a-amino-4-bromo-2,3-dihydro-3-oxo-; (R,S)-2-amino-3-(4-bromo-3-hydroxy-5-isoxazolyl)propionic acid; 2-AMINO-3-(4-BROMO-3-HYDROXYISOXAZOL-5-YL)PROPANOICACID; 2-amino-3-(4-bromo-3-oxo-2,3-dihydroisoxazol-5-yl)propanoic acid; 2-AMINO-3-(4-BROMO-3-HYDROXY-1,2-OXAZOL-5-YL)PROPANOIC ACID
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| Activity |
Ki ~ 100000 nM
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[11] | |||
| Compound Name |
(2R,3S)-1-(9-Iodophenanthrene-3-carbonyl)piperazine-2,3-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1950805; BDBM50364074
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| Activity |
IC50 ~ 100000 nM
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[12] | |||
| Compound Name |
4-[(E)-4,4-Diphenylbutylidene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL53655; BDBM50091487; (2S,4E)-2-amino-4-(4,4-diphenylbutylidene)pentanedioic acid; (S)-2-Amino-4-[4,4-diphenyl-but-(E)-ylidene]-pentanedioic acid
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| Activity |
Ki ~ 100000 nM
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[6] | |||
| Compound Name |
(S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxythiophene-3-ylmethyl)pyrimidine-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL379442; BDBM50185318; ZINC13686112
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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
Cl-HIBO
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL72366; 2-amino-3-(4-chloro-3-oxo-1,2-oxazol-5-yl)propanoic acid; (RS)-2-AMINO-3-(4-CHLORO-3-HYDROXY-5-ISOXAZOLYL)PROPIONIC ACID; SCHEMBL1055865; 4-CHLOROHOMOIBOTENIC ACID; CTK8F8718; (2S)-2-amino-3-(4-chloro-3-oxo-1,2-oxazol-5-yl)propanoic acid; BDBM50128264; AKOS024456741; AB17833; C-355; SR-01000597512; SR-01000597512-1; (R,S)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionate; 2-Amino-3-(4-chloro-3-hydroxy-isoxazol-5-yl)-propionic acid; 2-amino-3-(4-chloro-3-oxo-1,2-oxazol-5-yl)propanoic acid.; 2-AMINO-3-(4-CHLORO-3-HYDROXY-1,2-OXAZOL-5-YL)PROPANOIC ACID
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| Activity |
Ki ~ 100000 nM
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[11] | |||
| Compound Name |
4-[(E)-Cyclohexylmethylene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL53702; SCHEMBL8399683; SCHEMBL8399687; BDBM50091489; (2S,4E)-2-amino-4-(cyclohexylmethylidene)pentanedioic acid; (S)-2-Amino-4-[1-cyclohexyl-meth-(E)-ylidene]-pentanedioic acid
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| Activity |
Ki ~ 100010 nM
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[6] | |||
| Compound Name |
(S)-2-Amino-4-pentylidene-pentanedioicacid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL297919; SCHEMBL8399796; SCHEMBL8399799; BDBM50091478
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| Activity |
Ki = 125000 nM
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[6] | |||
| Compound Name |
(2R,4S)-2-(3-((Phenylcarbamoyl)methylcarbamoyl)propyl)-4-aminopentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1222147; BDBM50482549
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| Activity |
EC50 = 180000 nM
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[13] | |||
| Compound Name |
4-[(E)-4-Chlorobenzylidene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL297283; SCHEMBL8403177; BDBM50091492; (2S,4E)-2-amino-4-[(4-chlorophenyl)methylidene]pentanedioic acid; (S)-2-Amino-4-[1-(4-chloro-phenyl)-meth-(E)-ylidene]-pentanedioic acid
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| Activity |
Ki = 193000 nM
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[6] | |||
| Compound Name |
Click to Show/Hide
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Compound Info | |||
| Activity |
Ki ~ 100000 nM
|
[11] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 11 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
UBP-302
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Investigative | Compound Info | ||
| Synonyms |
UBP 302; (S)-1-(2-AMINO-2-CARBOXYETHYL)-3-(2-CARBOXYBENZYL)PYRIMIDINE-2,4-DIONE; UBP302; CHEMBL372797; 745055-91-8; UBC; Tocris-2079; AC1O4WKY; SCHEMBL2265710; GTPL4333; DTXSID80423571; MolPort-003-983-705; 2f35; ZINC3996041; BDBM50178136; BN0533; AKOS024456932; NCGC00025352-01; UBP302, > B6942; SR-01000597533; SR-01000597533-1; (S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl)-pyrimidine-2,4-dione; 2-[[3-[(2S)-2-amino-3-hydroxy-3-oxopropyl]-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid
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| Activity |
IC50 > 300000 nM
|
[4] | |||
| Compound Name |
(S)-AMPA
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Investigative | Compound Info | ||
| Synonyms |
(S)-AMPA; 83643-88-3; (S)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; UNII-9280SC28GD; CHEMBL276815; 9280SC28GD; (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)-propionic acid; AMPA, L-; AMQ; glutamate-AMPA; 1ftm; Tocris-0254; Tocris-0169; Tocris-1074; S-AMPA; 1p1q; L-AMPA; Lopac-G-017; AC1L4JUQ; Biomol-NT_000216; (S)-a-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; SCHEMBL667915; BPBio1_001304; CTK7I3476; BDBM17662; BDBM85214; UUDAMDVQRQNNHZ-YFKPBYRVSA-N; MolPort-003-940-001; MolPort-003-983-512; HMS3266E09
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| Activity |
Ki > 1000000 nM
|
[8] | |||
| Compound Name |
4-[(E)-3-Phenylpropylidene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL53775; SCHEMBL8404626; BDBM50091484; (2S,4E)-2-amino-4-(3-phenylpropylidene)pentanedioic acid; (S)-2-Amino-4-[3-phenyl-prop-(E)-ylidene]-pentanedioic acid
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| Activity |
Ki = 205000 nM
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[6] | |||
| Compound Name |
(S)-2-Amino-4-(1-ethyl-propylidene)-pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL51008; LY-339687; SCHEMBL8404009; BDBM50091473; (2S)-2-amino-4-pentan-3-ylidenepentanedioic acid
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| Activity |
Ki = 207000 nM
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[6] | |||
| 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 = 236000 nM
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[2] | |||
| Compound Name |
4-Cyclohexylidene-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL54238; SCHEMBL8399846; BDBM50091493; (2S)-2-amino-4-cyclohexylidenepentanedioic acid; (S)-2-Amino-4-cyclohexylidene-pentanedioic acid
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| Activity |
Ki = 255000 nM
|
[6] | |||
| Compound Name |
4-Propylidene-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL52295; LY-310683; SCHEMBL8520058; BDBM50091481; (S)-2-Amino-4-propylidene-pentanedioicacid
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| Activity |
EC50 > 300000 nM
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[6] | |||
| Compound Name |
4-Isopropylidene-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL298779; SCHEMBL8404622; BDBM50091483; (S)-2-Amino-4-isopropylidene-pentanedioic acid; (2S)-2-amino-4-propan-2-ylidenepentanedioic acid
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| Activity |
Ki > 400000 nM
|
[6] | |||
| Compound Name |
(2S,4Z)-2-Amino-4-(2-methylpropylidene)pentanedioic Acid
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Investigative | Compound Info | ||
| Synonyms |
LY-339675; CHEMBL298800; SCHEMBL8401766; SCHEMBL8401769; BDBM50091475
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| Activity |
Ki > 500000 nM
|
[6] | |||
| Compound Name |
4-[(E)-3-Methylbutylidene]-L-glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL299365; SCHEMBL8403439; BDBM50091490; (S)-2-Amino-4-(3-methyl-butylidene)-pentanedioic acid; (2S,4E)-2-amino-4-(3-methylbutylidene)pentanedioic acid
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| Activity |
Ki = 634000 nM
|
[6] | |||
| Compound Name |
(2r)-2-Amino-3-(4-Hydroxy-1,2,5-Thiadiazol-3-Yl)propanoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL402444; BDBM50373889; 3-(4-hydroxy-1,2,5-thiadiazol-3-yl)-D-alanine; 3-(4-Hydroxy-1,2,5-thiadiazole-3-yl)-D-alanine; Q27464829
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| Activity |
Ki > 1000000 nM
|
[9] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. J Med Chem. 2010 Aug 12;53(15):5367-82. | ||||
| 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 | Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. J Med Chem. 2005 Jun 30;48(13):4200-3. | ||||
| REF 4 | Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil r... J Med Chem. 2007 Apr 5;50(7):1558-70. | ||||
| REF 5 | Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5. J Med Chem. 2004 Dec 30;47(27):6948-57. | ||||
| REF 6 | 4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists. Bioorg Med Chem Lett. 2000 Aug 21;10(16):1807-10. | ||||
| REF 7 | 4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists. J Med Chem. 2000 May 18;43(10):1958-68. | ||||
| REF 8 | Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues. J Med Chem. 2005 May 5;48(9):3438-42. | ||||
| REF 9 | Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency. J Med Chem. 2008 Mar 13;51(5):1459-63. | ||||
| REF 10 | Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624. | ||||
| REF 11 | Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO). J Med Chem. 2003 May 22;46(11):2246-9. | ||||
| REF 12 | Piperazine-2,3-dicarboxylic acid derivatives as dual antagonists of NMDA and GluK1-containing kainate receptors. J Med Chem. 2012 Jan 12;55(1):327-41. | ||||
| REF 13 | Allosteric control of an ionotropic glutamate receptor with an optical switch. Nat Chem Biol. 2006 Jan;2(1):47-52. | ||||
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