Target Poor or Non Binder(s) Information

Target General Information

Target ID

T33584

Target Info

Target Name

Glutamate receptor AMPA 1 (GRIA1)

Synonyms

Glutamate receptor ionotropic, AMPA 1; Glutamate receptor 1; GluR-K1; GluR-A; GluR-1; GluA1; GLUR1; GLUH1; AMPA-selective glutamate receptor 1

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Target Type

Successful Target

Gene Name

GRIA1

Biochemical Class

Glutamate-gated ion channel

UniProt ID

P42261

Poor Binders of This Target (in total, 19 binders)

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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 = 71000 nM

[1]

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

[2]

Compound Name

Kainic acid

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Investigative

Compound Info

Synonyms

Digenin; Digenic acid; Helminal; Kainate; L-alpha-Kainic acid; alpha-Kainic acid; Digensaeure; Kainsaeure; Acidum kainicum; Acide kainique; Acido kainico; C10H15NO4; UNII-SIV03811UC; alpha- Kainic acid; CHEMBL275040; SIV03811UC; NSC136038; NCGC00024504-05; NSC 136038; DSSTox_CID_20526; DSSTox_RID_79503; DSSTox_GSID_40526; Kainic acid [INN:JAN]; 3-(Carboxymethyl)-4-isopropenylproline; Acide kainique [INN-French]; Acido kainico [INN-Spanish]; Acidum kainicum [INN-Latin]; 2-Carboxy-4-isopropenyl-3-pyrrolidineacetic acid; SR-01000075454; BRN 0086660; Kainic acid (synthetic); Biomol-NT_000217; UPCMLD-DP146; Lopac0_000656; SCHEMBL15777; 4-22-00-01523 (Beilstein Handbook Reference); MLS001074661; BPBio1_001306; (-)-(.alpha.)-Kainic Acid; DTXSID7040526; UPCMLD-DP146:001; UPCMLD-DP146:002; CTK1D6000; HMS2233K05; HMS3262C13; HMS3266C11; HMS3411A21; HMS3675A21; HY-N2309; ZINC3995575; Tox21_110905; Tox21_500656; BDBM50002369; Kainic Acid - CAS 487-79-6; AKOS024456995; Tox21_110905_1; CCG-204742; LP00656; MB00564; NSC-136038; SDCCGSBI-0050635.P002; NCGC00024504-02; NCGC00024504-03; NCGC00024504-04; NCGC00024504-06; NCGC00024504-07; NCGC00024504-08; NCGC00024504-09; NCGC00024504-15; NCGC00261341-01; SC-19815; SMR000471885; B6226; CS-0020451; EU-0100656; C12819; K 0250; Q390239; SR-01000597728; SR-01000075454-1; SR-01000075454-5; SR-01000075454-6; SR-01000075454-7; SR-01000597728-1

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Activity

EC50 = 60000 nM

[3]

Compound Name

6-((1S)-1-(1-(5-(2-Hydroxyethoxy)-2-pyridinyl)-1H-pyrazol-3-yl)ethyl)-2(3H)-benzothiazolone

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Investigative

Compound Info

Synonyms

LY3130481; YIQTLNB50N; UNII-YIQTLNB50N; CHEMBL3823394; LY-3130481; SCHEMBL15733246; BDBM50184444; SB18769; HY-108707; CS-0030138; J3.566.399A

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Activity

IC50 = 68500 nM

[4]

Compound Name

N-(1H-Indazol-5-yl)-N-[(1-methylpyrazol-3-yl)methyl]-4-pyridin-2-yl-1,3-thiazol-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL3822572; BDBM50184418

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Activity

IC50 = 83300 nM

[4]

Compound Name

N-Methyl-N-(1-pyridin-2-ylpyrazol-3-yl)-1H-indazol-5-amine

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Investigative

Compound Info

Synonyms

CHEMBL3823956; BDBM50184413

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Activity

IC50 ~ 83300 nM

[4]

Compound Name

6-[(1S)-1-(1-Pyridin-2-ylpyrazol-3-yl)ethyl]-3H-1,3-benzothiazol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3822825; BDBM50184416

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Activity

IC50 = 83300 nM

[4]

Compound Name

6-[(1S)-1-[1-(5-Fluoropyridin-2-yl)pyrazol-3-yl]ethyl]-3H-1,3-benzothiazol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3823445; BDBM50184419

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Activity

IC50 = 83300 nM

[4]

Compound Name

6-[(1R)-1-(1-Pyridin-2-ylpyrazol-3-yl)ethyl]-3H-1,3-benzothiazol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3823247; BDBM50184417

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Activity

IC50 = 83300 nM

[4]

Compound Name

6-[Methyl-(4-pyridin-2-yl-1,3-thiazol-2-yl)amino]-3H-1,3-benzothiazol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3823131; BDBM50184414

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Activity

IC50 ~ 83300 nM

[4]

Compound Name

4-[Methyl[4-(2-pyridinyl)thiazole-2-yl]amino]phenol

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Investigative

Compound Info

Synonyms

CHEMBL3823441; BAS 08770278; ZINC613583; BDBM50184411; AKOS000563515; MCULE-3919220524; J3.614.875F

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Activity

IC50 ~ 83300 nM

[4]

Compound Name

N-(1H-Indazol-5-yl)-N-methyl-4-pyridin-2-yl-1,3-thiazol-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL3823274; BDBM50184412

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Activity

IC50 ~ 83300 nM

[4]

Compound Name

6-[1-(1-Pyridin-2-ylpyrazol-3-yl)ethyl]-3H-1,3-benzothiazol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3823222; BDBM50184415

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Activity

IC50 = 83300 nM

[4]

Compound Name

6-[(1S)-1-[1-[5-(2-Hydroxyethyl)pyridin-2-yl]pyrazol-3-yl]ethyl]-3H-1,3-benzothiazol-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3823351; SCHEMBL17288289; BDBM50184442; 6-[(S)-1-[1-[5-(2-hydroxyethyl)-2-pyridyl]pyrazol-3-yl]ethyl]-3H-1,3-benzothiazol-2-one

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Activity

IC50 = 83300 nM

[4]

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 ~ 100000 nM

[5]

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

[2]

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 = 113400 nM

[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 = 134000 nM

[6]

Compound Name

N-[1-{3-[4-(3-Amino-propylamino)-butylamino]-propylcarbamoyl}-2-(4-hydroxy-phenyl)-ethyl]-butyramide

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Investigative

Compound Info

Synonyms

CHEMBL55975; SCHEMBL13759824; BDBM50122088

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Activity

Ki = 170000 nM

[7]

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Non Binders of This Target (in total, 6 non binders)

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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 > 300000 nM

[8]

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 = 480000 nM

[1]

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 = 550000 nM

[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

EC50 > 3000000 nM

[1]

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 = 3000000 nM

[1]

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+13 nM

[1]

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References

Top

REF 1

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.

REF 2

2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5. J Med Chem. 2003 Dec 18;46(26):5834-43.

REF 3

Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands. Bioorg Med Chem. 2010 Feb 15;18(4):1381-7.

REF 4

Discovery of the First alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) -8. J Med Chem. 2016 May 26;59(10):4753-68.

REF 5

4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists. Bioorg Med Chem Lett. 2000 Aug 21;10(16):1807-10.

REF 6

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 7

Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors. J Med Chem. 2002 Dec 19;45(26):5745-54.

REF 8

Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624.

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