Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T42392 | Target Info | |||
| Target Name | Glutamate receptor AMPA 2 (GRIA2) | ||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 2; Glutamate receptor 2; GluRK2; GluRB; GluR2; GluR-K2; GluR-B; GluR-2; GluA2; AMPAselective glutamate receptor 2; AMPA-selective glutamate receptor 2
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| Target Type | Successful Target | ||||
| Gene Name | GRIA2 | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 45 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Cyclothiazide
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Approved | Compound Info | ||
| Synonyms |
Anhydron; Aquirel; Ciclotiazida; Ciclotiazide; Cyclothiazidum; Doburil; Fluidil; Renazide; Valmiran; Ciclotiazide [DCIT]; C 9847; MDi 193; Anhydron (TN); Ciclotiazida [INN-Spanish]; Cyclothiazidum [INN-Latin]; Lilly 35,483; Cyclothiazide [USAN:INN:BAN]; Cyclothiazide (JAN/USAN/INN); 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 3,4-dihydro-6-chloro-3-(5-norbornen-2-yl)-, 1,1-dioxide; 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 3,4-dihydro-6-chloro-3-(5-norbornen-2-yl)-,1,1-dioxide; 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 3-bicyclo(2.2.1)hept-5-en-2-yl-6-chloro-3,4-dihydro-, 1,1-dioxide; 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 3-bicyclo[2.2.1]hept-5-en-2-yl-6-chloro-3,4-dihydro-, 1,1-dioxide; 2H-1,2,4-Benzothiadiazine-7-sulfonamide, 6-chloro-3,4-dihydro-3-(5-norbornen-2-yl)-, 1,1-dioxide; 3-(bicyclo[2.2.1]hept-5-en-2-yl)-6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 3-Bicyclo(2.2.1)hept-5-en-2-yl-6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 3-Bicyclo[2.2.1]hept-5-en-2-yl-6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-Chloro-3,4-dihydro-3-(2-norbornen-5-yl)-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-Chloro-3,4-dihydro-3-(2-norbornen-5-yl)-2H-1,2-4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-Chloro-3,4-dihydro-3-(2-norbornen-5-yl)-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide; 6-Chloro-3,4-dihydro-3-(5-norbornen-2-yl)-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-Chloro-3,4-dihydro-3-(norbornen-2-yl)-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-Chloro-3-(2-norbornen-5-yl)-7-sulfamyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide; 6-chloro-3,4-dihydro-3-(norbornen-2-yl)-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| 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 = 140000 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 |
GYKI-53655
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Terminated | Compound Info | ||
| Synonyms |
GYKI-53655; Gyki 53655; GYKI53655; 1-(4-AMINOPHENYL)-3-METHYLCARBAMOYL-4-METHYL-7,8-METHYLENEDIOXY-3,4-DIHYDRO-5H-2,3-BENZODIAZEPINE; 143692-18-6; CHEMBL267450; LY 300168; SMGACXZFVXKEAX-UHFFFAOYSA-N; AC1L2QV0; GYKI-53655 free base; MLS006010331; SCHEMBL351325; GTPL4209; DTXSID30276296; MolPort-006-418-196; BCP27661; BDBM50048386; ABP000447; NCGC00263113-03; NCGC00263113-01; SMR004701394; LY300168; LY-300168; FT-0765288; LY 300168(GYKI 53655); LY-300168, (+/-)-; 7H-1,3-Dioxolo(4,5-H)(2,3)benzodiazepine-7-carboxamide, 5-(4-aminopheny
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| Activity |
EC50 = 100000 nM
|
[1] | |||
| 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
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[4] | |||
| 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
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[5] | |||
| Compound Name |
LY382884
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Investigative | Compound Info | ||
| Synonyms |
LY-382884; LY 382884
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| Activity |
Ki ~ 100000 nM
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[3] | |||
| Compound Name |
6-(4-Amino-3-methylphenyl)-8-[(3-bromo-4,5-dihydro-1,2-oxazol-5-yl)methyl]-3,10-dihydro-2H-[1,4]dioxino[2,3-h][2,3]benzodiazepin-9-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4088629; BDBM50267947
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| Activity |
Ki = 50000 nM
|
[6] | |||
| Compound Name |
2-Methyl-N-[3-[2-(propan-2-ylsulfonylamino)-2,3-dihydro-1H-inden-5-yl]phenyl]propanamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2930356; CHEMBL1214261
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| Activity |
EC50 ~ 50118.72 nM
|
[7] | |||
| Compound Name |
N-[5-(3-Acetylphenyl)-2,3-dihydro-1H-inden-2-yl]propane-2-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2930371; CHEMBL1214205; N-[5-(3-acetylphenyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide
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| Activity |
EC50 ~ 50118.72 nM
|
[7] | |||
| Compound Name |
N-[5-(3-Cyanophenyl)-2,3-dihydro-1H-inden-2-yl]propane-2-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL2930332; CHEMBL1214204; N-[5-(3-cyanophenyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide
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| Activity |
EC50 ~ 50118.72 nM
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[7] | |||
| Compound Name |
4-Ethyl-3,4-Dihydro-2h-Pyrido[3,2-E][1,2,4]thiadiazine 1,1-Dioxide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL103741; SCHEMBL8559034; BDBM50032248; Q27453694; 4-ethyl-2,3-dihydropyrido[3,2-e][1,2,4]thiadiazine 1,1-dioxide
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| Activity |
EC50 = 50582.47 nM
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[8] | |||
| 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 = 52000 nM
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[2] | |||
| Compound Name |
CCNC(=O)c1c(C)sc2nc(Cc3cccc(c3)C#N)cc(=O)n12
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3799162; SCHEMBL16645606; BDBM50164391
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| Activity |
EC50 = 53700 nM
|
[9] | |||
| Compound Name |
CCN(Cc1cc(=O)n2c(N3CCOCC3)c(C)sc2n1)c1ccc(F)cc1
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3798907; SCHEMBL16636599; BDBM50164397
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| Activity |
EC50 = 60200 nM
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[9] | |||
| Compound Name |
N-Cyclopentyl-2-{4-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]phenyl}acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1649665; SCHEMBL3127061; BDBM50334936; N-cyclopentyl-2-[4-[3-(trifluoromethyl)-4,5,6,7-tetrahydroindazol-1-yl]phenyl]acetamide
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| Activity |
EC50 = 63095.73 nM
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[10] | |||
| Compound Name |
N-[5-(5-Cyanopyridin-3-yl)-2,3-dihydro-1H-inden-2-yl]propane-2-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1214395; SCHEMBL3248303; BDBM50323795; n-[5-(5-cyano-3-pyridinyl)-2,3-dihydro-1h-inden-2-yl]-2-propanesulfonamide
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| Activity |
EC50 = 63095.73 nM
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[7] | |||
| Compound Name |
N-Ethyl-2-methyl-5-oxo-7-[[3-(trifluoromethyl)phenyl]methyl]-[1,3]thiazolo[3,2-a]pyrimidine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3799419; SCHEMBL16645791; BDBM50164390
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| Activity |
EC50 = 66200 nM
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[9] | |||
| Compound Name |
CCN(Cc1cc(=O)n2c(CO)c(C)sc2n1)c1ccc(F)cc1
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3797994; SCHEMBL16636601; BDBM50164383
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| Activity |
EC50 = 66300 nM
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[9] | |||
| Compound Name |
CCN(Cc1cc(=O)n2c(C#N)c(C)sc2n1)c1ccc(F)cc1
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3799103; SCHEMBL16636800; BDBM50164396
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| Activity |
EC50 = 66600 nM
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[9] | |||
| Compound Name |
(1r,2r)-2-(2-{[5-Chloro-3-(Trifluoromethyl)-1h-Pyrazol-1-Yl]methyl}-7-Methyl-4-Oxo-4h-Pyrido[1,2-A]pyrimidin-6-Yl)cyclopropane-1-Carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3983039; BDBM50206009
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| Activity |
EC50 = 67000 nM
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[11] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxyphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440687; BDBM50494060
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| Activity |
Ki = 70000 nM
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[12] | |||
| Compound Name |
7-[[5-Chloro-3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]-N-ethyl-2-methyl-5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidine-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3799694; SCHEMBL16645609; BDBM50164400
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| Activity |
EC50 = 73000 nM
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[11] | |||
| Compound Name |
CID 60023874
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440689; BDBM50494061; (3S,4aR,6S,8aR)-6-(2-carboxyanilino)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
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| Activity |
Ki = 77000 nM
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[12] | |||
| Compound Name |
N-((3R,4R)-1-Methyl-4-(3''-(trifluoromethyl)biphenyl-4-yl)pyrrolidin-3-yl)propane-2-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1290612; SCHEMBL5185436; BDBM50331377
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| Activity |
EC50 = 79400 nM
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[13] | |||
| Compound Name |
(R)-2-Amino-3-(3'-Hydroxybiphenyl-3-Yl)propanoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3759959; BDBM50142618; Q27459844; (2R)-2-amino-3-(3'-hydroxybiphenyl-3-yl)propanoic acid (non-preferred name); E42
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| Activity |
Ki = 84000 nM
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[14] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-4-methoxyphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440515; BDBM50494065
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| Activity |
Ki = 87000 nM
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[12] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-5-methylphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440701; BDBM50494064
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| Activity |
Ki = 89000 nM
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[12] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-3-fluorophenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440686; BDBM50494072
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| Activity |
Ki = 93000 nM
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[12] | |||
| Compound Name |
1-(3,5-Dimethyl-4-aminophenyl)-7,8-(ethylenedioxy)-3H-2,3-benzodiazepine-4(5H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL406937; BDBM50267952; J3.569.206A
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| Activity |
Ki = 94000 nM
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[6] | |||
| Compound Name |
1-[4-(1-Pyrrolidinylcarbonyl)phenyl]-3-(trifluoromethyl)-1,4,5,7-tetrahydropyrano[3,4-c]pyrazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1649683; SCHEMBL1423867; BDBM50334927; pyrrolidin-1-yl-[4-[3-(trifluoromethyl)-5,7-dihydro-4H-pyrano[3,4-c]pyrazol-1-yl]phenyl]methanone
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| Activity |
EC50 = 100000 nM
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[10] | |||
| 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 |
Piperidin-1-yl-[4-[3-(trifluoromethyl)-4,5,6,7-tetrahydroindazol-1-yl]phenyl]methanone
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL3139195; CHEMBL1649653; STL231235; AKOS002138873; MCULE-1417099689; piperidin-1-yl{4-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]phenyl}methanone
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| Activity |
EC50 ~ 100000 nM
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[10] | |||
| 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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[5] | |||
| 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 |
(3S,4As,6S,8aR)-6-(2-carboxy-4-methylphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440516; BDBM50494066
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| Activity |
Ki = 107000 nM
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[12] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-5-methoxyphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440700; BDBM50494056
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| Activity |
Ki = 111000 nM
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[12] | |||
| 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 = 117000 nM
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[15] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-[3-methyl-2-(2H-tetrazol-5-yl)anilino]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3088056; BDBM50494354
Click to Show/Hide
|
||||
| Activity |
Ki = 128000 nM
|
[16] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-[(3-carboxyphenyl)methyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440124; BDBM50494070
Click to Show/Hide
|
||||
| Activity |
Ki = 149000 nM
|
[12] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-5-chlorophenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440703; SCHEMBL3304074; BDBM50494057
Click to Show/Hide
|
||||
| Activity |
Ki = 151000 nM
|
[12] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(2-carboxy-4-phenylphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440704; BDBM50494069
Click to Show/Hide
|
||||
| Activity |
Ki = 172000 nM
|
[12] | |||
| Compound Name |
4-Methyl-2,3-dihydro-1lambda6,2,4-benzothiadiazine 1,1-dioxide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL226584; BDBM50457615
Click to Show/Hide
|
||||
| Activity |
EC50 = 176300 nM
|
[17] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-[3-methoxy-2-(2H-tetrazol-5-yl)anilino]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3088057; BDBM50494353
Click to Show/Hide
|
||||
| Activity |
Ki = 181000 nM
|
[16] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 22 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
UBP-302
Click to Show/Hide
|
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
Click to Show/Hide
|
||||
| Activity |
IC50 > 300000 nM
|
[4] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-(3-carboxyanilino)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440693; BDBM50494052
Click to Show/Hide
|
||||
| Activity |
Ki = 238000 nM
|
[12] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-[3-methoxy-2-(2H-tetrazol-5-yl)phenoxy]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3088055; BDBM50494359
Click to Show/Hide
|
||||
| Activity |
Ki = 252000 nM
|
[16] | |||
| Compound Name |
(S)-2-Amino-4-(1-ethyl-propylidene)-pentanedioic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL51008; LY-339687; SCHEMBL8404009; BDBM50091473; (2S)-2-amino-4-pentan-3-ylidenepentanedioic acid
Click to Show/Hide
|
||||
| Activity |
Ki = 280900 nM
|
[18] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-[5-phenoxy-2-(2H-tetrazol-5-yl)phenoxy]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3085835; BDBM50494345
Click to Show/Hide
|
||||
| Activity |
Ki = 335000 nM
|
[16] | |||
| Compound Name |
Chembl4206883
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50457618
Click to Show/Hide
|
||||
| Activity |
EC50 = 403300 nM
|
[17] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(4-carboxyphenyl)sulfanyl-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440695; BDBM50494053
Click to Show/Hide
|
||||
| Activity |
Ki = 418000 nM
|
[12] | |||
| 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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3088067; BDBM50494357
Click to Show/Hide
|
||||
| Activity |
Ki = 450000 nM
|
[16] | |||
| Compound Name |
(+)-2-Amino-4-(4-hydroxy-1,2,5-oxadiazol-3-yl)butanoicAcid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1098101; BDBM50318265; 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX)
Click to Show/Hide
|
||||
| Activity |
EC50 = 489000 nM
|
[19] | |||
| Compound Name |
(+)-2-Amino-5-(4-hydroxy-1,2,5-oxadiazol-3-yl)pentanoicAcid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1098104; BDBM50318266; 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX)
Click to Show/Hide
|
||||
| Activity |
EC50 = 489778.82 nM
|
[19] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-[(4-carboxyphenyl)methyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL7056068; CHEMBL2440697
Click to Show/Hide
|
||||
| Activity |
Ki = 553000 nM
|
[16] | |||
| Compound Name |
(1S,2S,6R,8S)-6-(Carboxymethyl)-3-oxo-7-oxa-4,12-diazatricyclo[6.4.0.02,6]dodec-9-ene-5-carboxylic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2323527; BDBM50427677
Click to Show/Hide
|
||||
| Activity |
Ki = 560000 nM
|
[20] | |||
| 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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440514; BDBM50494071
Click to Show/Hide
|
||||
| Activity |
Ki = 818000 nM
|
[12] | |||
| Compound Name |
(RS)-2-amino-3-[3-hydroxy-5-(2-propyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid
Click to Show/Hide
|
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
Click to Show/Hide
|
||||
| Activity |
EC50 = 830000 nM
|
[2] | |||
| Compound Name |
(3S,4As,6S,8aR)-6-(4-carboxyphenoxy)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid;hydrochloride
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440694; BDBM50494049
Click to Show/Hide
|
||||
| Activity |
Ki = 913000 nM
|
[12] | |||
| Compound Name |
2-Amino-3-(3-hydroxy-5-(2-isopropyl-2H-tetrazol-5-yl)isoxazol-4-yl)propanoic acid
Click to Show/Hide
|
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
Click to Show/Hide
|
||||
| Activity |
EC50 = 1000000 nM
|
[2] | |||
| Compound Name |
(3S,4Ar,6S,8aR)-6-(4-carboxyanilino)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440696; BDBM50494063
Click to Show/Hide
|
||||
| Activity |
Ki = 1420000 nM
|
[12] | |||
| 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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440698; BDBM50494054
Click to Show/Hide
|
||||
| Activity |
Ki = 1470000 nM
|
[12] | |||
| Compound Name |
(R)-N-(2-Phenylpropyl)methanesulfonamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1276216; BDBM50330413; ZINC48903376
Click to Show/Hide
|
||||
| Activity |
EC50 = 1980000 nM
|
[21] | |||
| Compound Name |
2-Amino-3-[3-hydroxy-5-(1-methyl-1H-tetrazol-5-yl)-isoxazol-4-yl]-propionic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL317790; SCHEMBL13319946; BDBM50059674; (RS)-2-amino-3-[3-hydroxy-5-(1-methyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid
Click to Show/Hide
|
||||
| Activity |
EC50 > 3000000 nM
|
[2] | |||
| Compound Name |
(RS)-2-amino-3-[3-hydroxy-5-(2-benzyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL388746; BDBM50211399
Click to Show/Hide
|
||||
| Activity |
EC50 > 3000000 nM
|
[2] | |||
| 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
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2440690; BDBM50494048
Click to Show/Hide
|
||||
| Activity |
Ki = 29600000 nM
|
[12] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands. Bioorg Med Chem. 2010 Feb 15;18(4):1381-7. | ||||
| REF 2 | 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 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 | 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5. J Med Chem. 2003 Dec 18;46(26):5834-43. | ||||
| REF 6 | Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists. Bioorg Med Chem. 2017 Jul 15;25(14):3631-3637. | ||||
| REF 7 | Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator. J Med Chem. 2010 Aug 12;53(15):5801-12. | ||||
| REF 8 | 7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency. J Med Chem. 2018 Jan 11;61(1):251-264. | ||||
| REF 9 | Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design. J Med Chem. 2016 Mar 24;59(6):2760-79. | ||||
| REF 10 | Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators. J Med Chem. 2011 Jan 13;54(1):78-94. | ||||
| REF 11 | GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile. ACS Med Chem Lett. 2016 Oct 31;8(1):84-89. | ||||
| REF 12 | 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 13 | N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7116-9. | ||||
| REF 14 | Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors. J Med Chem. 2016 Jan 14;59(1):448-61. | ||||
| REF 15 | 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 16 | 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. | ||||
| REF 17 | Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds. J Med Chem. 2018 Jun 28;61(12):5279-5291. | ||||
| REF 18 | 4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists. Bioorg Med Chem Lett. 2000 Aug 21;10(16):1807-10. | ||||
| REF 19 | 4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological charact... J Med Chem. 2010 May 27;53(10):4110-8. | ||||
| REF 20 | Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159: asymmetric synthesis, neuroactivity, and structural characterization. J Med Chem. 2013 Mar 28;56(6):2283-93. | ||||
| REF 21 | 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. | ||||
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