Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T73495 | Target Info | |||
| Target Name | Glutamate receptor ionotropic kainate 1 (GRIK1) | ||||
| Synonyms |
Glutamate receptor 5; GluR5 kainate receptor; GluR5; GluR-5; GRIK1; Excitatory amino acid receptor 3; EAA3
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| Target Type | Successful Target | ||||
| Gene Name | GRIK1 | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 14 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 = 75000 nM
|
[1] | |||
| Compound Name |
N-(3-Bromophenyl)-6-chloro-3-hydroxy-1H-indazole-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL224831; BDBM50158559
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
4-Chloro-2-(3-thiophen-3-yl-ureido)-benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL156768; BDBM50137135; AKOS015699753
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| Activity |
IC50 = 51000 nM
|
[3] | |||
| Compound Name |
3-[3-(3-Trifluoromethyl-phenyl)-ureido]-naphthalene-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL347828; SCHEMBL6448240; BDBM50137132
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| Activity |
IC50 = 60000 nM
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[3] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-[(2-carboxyphenyl)methyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440690; BDBM50494048
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| Activity |
Ki = 67000 nM
|
[4] | |||
| Compound Name |
4-Chloro-2-(3-pyridin-3-yl-ureido)-benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL154960; BDBM50137146; AKOS010436749
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| Activity |
IC50 = 69000 nM
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[3] | |||
| 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 = 69000 nM
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[3] | |||
| Compound Name |
Anthranilic acid, N-((alpha,alpha,alpha-trifluoro-m-tolyl)carbamoyl)-
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Investigative | Compound Info | ||
| Synonyms |
NS1652; NS-1652; UNII-9B8X1YC8U2; 9B8X1YC8U2; CHEMBL156519; NS 1652; SCHEMBL1463217; ZINC7038; 2-[[3-(trifluoromethyl)phenyl]carbamoylamino]benzoic Acid; BDBM50137154; Benzoic acid, 2-((((3-(trifluoromethyl)phenyl)amino)carbonyl)amino)-; MCULE-1660808733; HY-100244; CS-0018395; 2-[3-(3-Trifluoromethyl-phenyl)-ureido]-benzoic acid; Q27272309
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| Activity |
IC50 = 72000 nM
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[3] | |||
| Compound Name |
4-Chloro-2-(pyridin-4-ylcarbamoylamino)benzoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL154290; SCHEMBL5950252; BDBM50137161; ZINC13531910; 4-Chloro-2-(3-pyridin-4-yl-ureido)-benzoic acid
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| Activity |
IC50 = 88000 nM
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[3] | |||
| Compound Name |
2-Methyl-6-[[3-(trifluoromethyl)phenyl]carbamoylamino]benzoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL154022; SCHEMBL1463302; BDBM50137148; 2-Methyl-6-[3-(3-trifluoromethyl-phenyl)-ureido]-benzoic acid
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
2-[(Anilinocarbonyl)amino]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
2-(phenylcarbamoylamino)benzoic acid; CHEMBL157063; Maybridge1_005476; CBMicro_028578; Cambridge id 5579848; Oprea1_642948; DivK1c_001764; SCHEMBL1462332; o-(3-Phenylureido)benzoic acid; 2-(3-Phenylureido)benzoic acid; CTK1A7438; HMS557A20; ZINC68783; DTXSID10277488; NSC2540; 2-(3-Phenyl-ureido)-benzoic acid; NSC-2540; BDBM50137155; SBB041935; AKOS000126663; MCULE-5777098590; CDS1_000724; 2-[(Anilinocarbonyl)amino]benzoic acid #; 2-[(phenylamino)carbonylamino]benzoic acid; BIM-0028562.P001; N-(2-CARBOXYPHENYL)-N'-PHENYLUREA
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
5-Methyl-2-[[3-(trifluoromethyl)phenyl]carbamoylamino]benzoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL154878; SCHEMBL1464103; BDBM50137123; 5-Methyl-2-[3-(3-trifluoromethyl-phenyl)-ureido]-benzoic acid
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
4-Chloro-2-(cyclohexylcarbamoylamino)benzoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL153891; SCHEMBL1463554; BDBM50137139; ZINC13531901; AKOS002435283; 4-Chloro-2-(3-cyclohexyl-ureido)-benzoic acid
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
3-Methyl-2-[[3-(trifluoromethyl)phenyl]carbamoylamino]benzoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL156464; SCHEMBL1463385; BDBM50137163; 3-Methyl-2-[3-(3-trifluoromethyl-phenyl)-ureido]-benzoic acid
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 5 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-6-methylphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440514; BDBM50494071
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| Activity |
Ki = 228000 nM
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[4] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(4-carboxyphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440694; BDBM50494049
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| Activity |
Ki = 267000 nM
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[4] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-6-chlorophenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440698; BDBM50494054
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| Activity |
Ki = 316000 nM
|
[4] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-[2-fluoro-6-(2H-tetrazol-5-yl)phenoxy]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3088067; BDBM50494357
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| Activity |
Ki = 422000 nM
|
[5] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-(4-carboxyanilino)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440696; BDBM50494063
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| Activity |
Ki = 528000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists. Bioorg Med Chem Lett. 2000 Aug 21;10(16):1807-10. | ||||
| REF 2 | 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 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 | GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6459-62. | ||||
| REF 5 | GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6463-6. | ||||
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