Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T77548 | Target Info | |||
| Target Name | Metabotropic glutamate receptor 8 (mGluR8) | ||||
| Synonyms |
MGluR8a; MGLUR8; Glutamate receptor mGLU8; GRM8
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| Target Type | Literature-reported Target | ||||
| Gene Name | GRM8 | ||||
| Biochemical Class | GPCR glutamate | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 14 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
PMID25435285-Compound-15
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Patented | Compound Info | ||
| Activity |
EC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
CPCCOEt
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL327783; 179067-99-3; AC1O3E8H; 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester; SCHEMBL12648369; MolPort-003-940-874; CPCCOEt, > AKOS024456339; LP00300; NCGC00024948-02; KB-49121; AS-16761; L000202; SR-01000597466; SR-01000597466-1; BRD-A05729358-001-01-2; ethyl (7E)-7-hydroxyimino-1,7a-dihydrocyclopropa[b]chromene-1a-carboxylate
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| Activity |
Ki ~ 100000 nM
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[2] | |||
| Compound Name |
SIB-1757
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Investigative | Compound Info | ||
| Activity |
Ki ~ 100000 nM
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[2] | |||
| Compound Name |
(2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate
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Investigative | Compound Info | ||
| Synonyms |
(2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid; (2R,4R)-APDC; (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid; 169209-63-6; 2R,4R-APDC; CHEMBL40086; CHEBI:40139; EN300-88063; 2R, 4R-APDC monohydrate; 52A; 4-amino-2,4-pyrrolidinedicarboxylic acid; AC1NSJRT; AC1Q4UAD; SCHEMBL158843; 2R, 4R-APDC; (2R,3R)-APDC; GTPL1392; CTK0E5090; DTXSID10415500; MolPort-003-982-102; BDBM50052398; ZINC32628523; SBB067830; MFCD16875409; AKOS015916056; AKOS015854214; RTC-065564; FCH3884669; NCGC00025040-02; LY314593; AJ-85443; SC-48823; TC-065564; B6634
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| Activity |
Ki ~ 100000 nM
|
[2] | |||
| Compound Name |
2-methyl-6-(phenylethynyl)pyridine
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Investigative | Compound Info | ||
| Synonyms |
2-Methyl-6-(phenylethynyl)pyridine; MPEP; 96206-92-7; 6-Methyl-2-(phenylethynyl)pyridine; 2-methyl-6-(2-phenylethynyl)pyridine; UNII-7VC0YVI27Y; 7VC0YVI27Y; CHEMBL66654; CHEBI:64159; Pyridine, 2-methyl-6-(phenylethynyl)-; Tocris-1212; AC1MHGB1; Lopac-M-5435; Lopac0_000738; MLS006011229; SCHEMBL103061; 2-Picoline, 6-phenylethynyl-; GTPL1426; DTXSID9043982; MolPort-003-958-770; HMS3651F13; 2-Methyl-6-phenylethynyl-pyridine; ZINC2581406; BCP05962; ZX-AN014840; 2-methyl-6-(phenylethynyl)-pyridine; s2809; HY-14609A; 2151AH
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| Activity |
Ki ~ 100000 nM
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[2] | |||
| Compound Name |
SIB-1893
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Investigative | Compound Info | ||
| Synonyms |
SIB 1893; SIB-1893; 2-methyl-6-(2-phenylethenyl)pyridine; 6266-99-5; SIB1893; 2-methyl-6-[(E)-2-phenylethenyl]pyridine; 7370-21-0; CHEMBL88612; MLS002607995; (E)-2-methyl-6-styrylpyridine; [E]-2-Methyl-6-[2-phenylethenyl]pyridine; (E)-2-Methyl-6-[2-phenylethenyl]pyridine; SR-01000076143; Lopac0_001171; Pyridine,2-methyl-6-(2-phenylethenyl)-; AC1NSKMI; AC1Q4VO3; GTPL1432; CHEBI:93178; BDBM86715; MolPort-003-959-634; HMS3263L03; ZINC3941522; 2-[(E)-Styryl]-6-methylpyridine; NSC36665; SIB 1893, >99%, solid; Tox21_501171
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| Activity |
Ki ~ 100000 nM
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[2] | |||
| Compound Name |
(2S)-2-Amino-4-[hydroxy-[hydroxy-(4-methoxyphenyl)methyl]phosphoryl]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4086929; BDBM50255387
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| Activity |
EC50 = 61000 nM
|
[3] | |||
| Compound Name |
(2S)-2-Amino-4-[hydroxy-[hydroxy-(4-hydroxy-3-nitrophenyl)methyl]phosphoryl]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4060360; SCHEMBL4091107; SCHEMBL10027439; BDBM50255339
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| Activity |
EC50 = 73000 nM
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[3] | |||
| Compound Name |
(2S)-2-Amino-4-[hydroxy-[hydroxy-(2-oxo-1H-pyridin-4-yl)methyl]phosphoryl]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4076857; BDBM50255448
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| Activity |
EC50 = 81000 nM
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[3] | |||
| Compound Name |
(2S)-2-Amino-4-[hydroxy-[hydroxy-(4-methylsulfonylphenyl)methyl]phosphoryl]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4094636; SCHEMBL8232961; BDBM50255293
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| Activity |
EC50 ~ 100000 nM
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[3] | |||
| Compound Name |
(2S)-2-Amino-4-[hydroxy-[hydroxy-(4-morpholin-4-yl-3-nitrophenyl)methyl]phosphoryl]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4082270; SCHEMBL4103522; BDBM50255333
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| Activity |
EC50 ~ 100000 nM
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[3] | |||
| Compound Name |
(+)-(1R,2R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2-oxide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL218710; BDBM50202406; LY-404040; (-)-(1R,2R,4S,5S,6S)-4-amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2-oxide; (-)-(1R,2S,4S,5S,6S)-4-amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2-oxide; (1R,4S,5S,6S)-4-amino-2-oxo-2lambda4-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid; [(1beta,5beta)-4-Amino-2-thiabicyclo[3.1.0]hexane-4beta,6beta-dicarboxylic acid]2-oxide
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
3-[[[(3S)-3-Amino-3-carboxypropyl]-hydroxyphosphoryl]-hydroxymethyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4061539; SCHEMBL4101257; BDBM50255400
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| Activity |
EC50 = 125000 nM
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[3] | |||
| Compound Name |
4-[[[(3S)-3-Amino-3-carboxypropyl]-hydroxyphosphoryl]-hydroxymethyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4095462; SCHEMBL4085528; BDBM50255416
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| Activity |
EC50 = 141000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 18 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-benzyl-APDC
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL60238; 171336-76-8; (2R,4R)-1-BENZYL-4-AMINO-PYRROLIDINE-2,4-DIcarboxylic acid; GTPL1436; SCHEMBL8061968; CTK0A8043; DTXSID60573467; ZINC39952128; BDBM50071161; DB-064818; AJ-101168; FT-0772028; 4-amino-1-(phenylmethyl)pyrrolidine-2,4-dicarboxylic acid; (2R,4R)-4-amino-1-benzylpyrrolidine-2,4-dicarboxylic acid; (2R,4R)-4-Amino-1-benzyl-pyrrolidine-2,4-dicarboxylic acid; (2R)-1-Benzyl-4-aminopyrrolidine-2beta,4alpha-dicarboxylic acid; 4-Amino-1-benzyl-pyrrolidine-2,4-dicarboxylic acid(1-benzyl-APDC)
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
LY307452
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Investigative | Compound Info | ||
| Synonyms |
LY-307452; LY-307,452; LY 307452
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| Activity |
Ki > 300000 nM
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[2] | |||
| Compound Name |
(2S)-2-Amino-4-[[(3-cyanophenyl)-hydroxymethyl]-hydroxyphosphoryl]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4090699; BDBM50255395
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| Activity |
EC50 = 219000 nM
|
[3] | |||
| Compound Name |
(2S)-2-Amino-4-[hydroxy-[(4-hydroxy-3-nitrophenyl)methyl]phosphoryl]butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4082813; BDBM50255391
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| Activity |
EC50 = 277000 nM
|
[3] | |||
| Compound Name |
(2R,4R)-4-Amino-1-methylpyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL300330; SCHEMBL14278713; CTK1A0056; DTXSID10658238; BDBM50071164; ZINC29571185; (2R,4R)-4-Amino-1-methyl-pyrrolidine-2,4-dicarboxylic acid; 2,4-Pyrrolidinedicarboxylicacid, 4-amino-1-methyl-, (2R,4R)-
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
(2R,4R)-4-Amino-1-biphenyl-2-ylmethyl-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL293434; SCHEMBL8973026; BDBM50071150; (2R,4R)-4-amino-1-[(2-phenylphenyl)methyl]pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
(2R,4R)-4-Amino-1-(3-chloro-benzyl)-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL60008; SCHEMBL8973090; BDBM50071168; (2R,4R)-4-amino-1-[(3-chlorophenyl)methyl]pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
(2R,4R)-4-Amino-1-naphthalen-2-ylmethyl-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL61281; SCHEMBL8973223; BDBM50071155; (2R,4R)-4-amino-1-(naphthalen-2-ylmethyl)pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
(2S,4S)-2-Amino-4-(2,2-diphenylethyl)pentanedioic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL40123; SCHEMBL187449; BDBM50069111; ZINC13797034; 2-Amino-4-(2,2-diphenyl-ethyl)-pentanedioic acid; (2S,4S)-2-Amino-4-(2,2-diphenyl-ethyl)-pentanedioic acid
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| Activity |
Ki > 300000 nM
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[2] | |||
| Compound Name |
(2R,4R)-4-Amino-1-(naphthalen-1-ylmethyl)pyrrolidine-2,4-dicarboxylic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL302411; SCHEMBL8973459; BDBM50071159; (2R,4R)-4-Amino-1-naphthalen-1-ylmethyl-pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
(2R,4R)-4-Amino-1-ethylpyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL59830; CTK1A0057; DTXSID80658240; BDBM50071156; ZINC26157741; (2R,4R)-4-Amino-1-ethyl-pyrrolidine-2,4-dicarboxylic acid; 2,4-Pyrrolidinedicarboxylicacid, 4-amino-1-ethyl-, (2R,4R)-
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
2-Amino-2,3-methano-4-phosphonobutanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL287703; (1R,2R)-1-amino-2-(phosphonomethyl)cyclopropane-1-carboxylic acid; (1R,2R)-1-amino-2-(phosphonomethyl)cyclopropanecarboxylic acid; 2-Ampba; DTXSID80928258; BDBM50089518; 1-amino-2-(phosphonomethyl)cyclopropane-1-carboxylic acid; (1R,2R)-1-amino-2-phosphonomethylcyclopropane-carboxylic acid; Cyclopropanecarboxylic acid, 1-amino-2-(phosphonomethyl)-, trans-(+-)-
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| Activity |
EC50 > 300000 nM
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[6] | |||
| Compound Name |
(2R,4R)-4-Amino-1-(2,2-diphenyl-ethyl)-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL304919; SCHEMBL8972526; BDBM50071151; (2R,4R)-4-amino-1-(2,2-diphenylethyl)pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
(2R,4R)-4-Amino-1-(2,6-dichloro-benzyl)-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL60164; BDBM50071167; (2R,4R)-4-amino-1-[(2,6-dichlorophenyl)methyl]pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
(2R,4R)-4-Amino-1-(2-chloro-benzyl)-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL418462; SCHEMBL8973329; BDBM50071165; (2R,4R)-4-amino-1-[(2-chlorophenyl)methyl]pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
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[5] | |||
| Compound Name |
3-[[[(3S)-3-Amino-3-carboxypropyl]-hydroxyphosphoryl]methyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4103332; SCHEMBL4084499; BDBM50255405
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| Activity |
EC50 = 511000 nM
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[3] | |||
| Compound Name |
(S)-4-((1-Carboxyethyl)amino)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL58247; 4-[[(1S)-1-carboxyethyl]amino]benzoic acid; 4-{[(1S)-1-carboxyethyl]amino}benzoic acid; SCHEMBL350279; KS-00001CM5; BDBM50071162; ZINC52969665; 4-((S)-1-Carboxy-ethylamino)-benzoic acid; (2S)-2-[(4-Carboxyphenyl)amino]propanoic acid
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| Activity |
IC50 > 1000000 nM
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[5] | |||
| Compound Name |
(S)-3,5-Dihydroxyphenylglycine
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Investigative | Compound Info | ||
| Synonyms |
(S)-3,5-DHPG; S-DHPG; L-3,5-Dihydroxyphenylglycine; C8H9NO4; UNII-CF5G2G268A; CHEMBL39221; 3,5-Dihydroxy-L-phenylglycine; CF5G2G268A; (S)-3,5 DHPG; (S)-3,5-Dihydroxyphenylglycine hydrate; Benzeneacetic acid, alpha-amino-3,5-dihydroxy-, (alphaS)-; (2r)-Amino(3,5-Dihydroxyphenyl)Acetic Acid; (2S)-amino(3,5-dihydroxyphenyl)ethanoic acid; (S)-2-amino-2-(3,5-dihydroxyphenyl)acetic acid; (S)-3,5-dihydroxyphenylglycine zwitterion; Tocris-0342; Tocris-0805; Lopac-D-3689; C12026; 3,5-Dihydroxy-phenylglycine; Lopac0_000328; (2S)-2-amino-2-(3,5-dihydroxyphenyl)acetic acid; SCHEMBL12648471; (s)-3,5-dihydroxylphenylglycine; CTK8F0556; DTXSID20904031; HMS3261A17; HMS3266F22; HMS3411L21; HMS3675L21; ZINC968043; Dihydroxyphenylglycine, (S)-3,5-; Tox21_500328; BDBM50079183; MFCD11044457; AKOS006239507; amino(3,5-dihydroxyphenyl)acetic acid; CCG-204423; DB04228; LP00328; SDCCGSBI-0050316.P002; NCGC00015338-01; NCGC00015338-02; NCGC00024545-01; NCGC00024800-01; NCGC00024800-02; NCGC00024800-03; NCGC00024800-04; NCGC00024800-05; NCGC00024800-10; NCGC00261013-01; HY-12598; Amino-(3,5-dihydroxy-phenyl)-acetic acid; J516.528H; (2S)-amino(3,5-dihydroxyphenyl)acetic acid; B6459; CS-0012064; EU-0100328; (S)-Amino-(3,5-dihydroxy-phenyl)-acetic acid; D 3689; SR-01000075813; SR-01000597444; Amino-(3,5-dihydroxy-phenyl)-acetic acid(S-DHPG); J-009981; SR-01000075813-1; SR-01000597444-1; Q27095051; UNII-5YR2N37E6D component HOOWCUZPEFNHDT-ZETCQYMHSA-N
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| Activity |
Ki > 1000000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5663-5668. | ||||
| REF 2 | Ligands for glutamate receptors: design and therapeutic prospects. J Med Chem. 2000 Jul 13;43(14):2609-45. | ||||
| REF 3 | Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989. | ||||
| REF 4 | Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identif... J Med Chem. 2007 Jan 25;50(2):233-40. | ||||
| REF 5 | Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid. Bioorg Med Chem Lett. 1998 Aug 4;8(15):1985-90. | ||||
| REF 6 | Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists. J Med Chem. 2007 Jul 26;50(15):3585-95. | ||||
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