Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T02719 | Target Info | |||
| Target Name | Metabotropic glutamate receptor 3 (mGluR3) | ||||
| Synonyms |
mGLUR3; Group III metabotropic glutamate receptor; GPRC1C
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| Target Type | Clinical trial Target | ||||
| Gene Name | GRM3 | ||||
| Biochemical Class | GPCR glutamate | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 10 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
SIB-1757
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Investigative | Compound Info | ||
| Activity |
Ki ~ 100000 nM
|
[1] | |||
| Compound Name |
Ro64-5229
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Investigative | Compound Info | ||
| Synonyms |
Ro 64-5229
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| Activity |
Ki ~ 100000 nM
|
[1] | |||
| 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
|
[1] | |||
| 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
|
[1] | |||
| Compound Name |
2-[[2,4-Dicarboxybutyl(hydroxy)phosphoryl]methyl]pentanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL134749; SCHEMBL4135913; 2-[(2,4-Dicarboxy-butyl)-hydroxy-phosphinoylmethyl]-pentanedioic acid; CTK7I4539; DTXSID70274433; PBDA, >95% (NMR), liquid; BDBM50085699; 4,4'-phosphinicobis(butane-1,3-dicarboxylic acid); J-014911; Pentanedioic acid, 2,2'-[phosphinicobis(methylene)]bis-; 4-Carboxy-5-[(2,4-dicarboxy-butyl)-hydroxy-phosphinoyl]-pentanoic acid; (meso)4-Carboxy-5-[(2,4-dicarboxy-butyl)-hydroxy-phosphinoyl]-pentanoic acid
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| Activity |
EC50 = 51000 nM
|
[2] | |||
| Compound Name |
(2R,4R)-1,4-Diamino-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL297150; BDBM50078596; 4-Amino-2,4-dicarboxy-pyrrolidin-1-yl-ammonium(1-Amino-APDC)
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| Activity |
Ki = 52000 nM
|
[1] | |||
| 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 = 63600 nM
|
[3] | |||
| Compound Name |
(1R,2R,4S,5S,6R)-2-Amino-4-methyl-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL195500; BDBM50167031
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
(2R,4R)-4-Amino-1-phenethyl-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL292553; SCHEMBL8972917; BDBM50071152; (2R,4R)-4-amino-1-(2-phenylethyl)pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 = 166000 nM
|
[3] | |||
| Compound Name |
(1R,2S)-2-Amino-2-carboxycyclopropane-1-acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3347670; ZINC39058088
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| Activity |
Ki = 199526.23 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 15 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(R,S)-4-phosphonophenylglycine
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Investigative | Compound Info | ||
| Synonyms |
(RS)-PPG; 120667-15-4; 2-amino-2-(4-phosphonophenyl)acetic acid; CHEMBL277475; AC1ND7MS; (RS)PPG; (RS) PPG; C8H10NO5P; (RS)-4-Phosphonophenylglycine; GTPL1406; SCHEMBL9150881; CTK8F0597; (R,S)-4-PPG; MolPort-003-983-668; BN0429; BDBM50004881; AKOS015911887; Amino-(4-phosphono-phenyl)-acetic acid; NCGC00025051-02; RT-015313; V2034; Amino-(4-phosphono-phenyl)-acetic acid(RS-PPG); SR-01000597406; 667P154; L000025; SR-01000597406-1; J-004376
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| Activity |
Ki > 200000 nM
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[1] | |||
| 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
|
[3] | |||
| Compound Name |
L-AP4
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Investigative | Compound Info | ||
| Synonyms |
(2S)-2-Amino-4-phosphonobutanoic acid; 23052-81-5; (2S)-2-amino-4-phosphonobutanoic acid; L-(+)-2-Amino-4-phosphonobutyric acid; L-APB; (S)-2-amino-4-phosphonobutanoic acid; CHEMBL33567; L-AP-4; S-2-amino-4-phosphonobutyrate; [3H]AP4; L-2-amino-4-phosphonobutiric acid; L-1-amino-4-phosphonobutanoic acid; Tocris-0103; NCIStruc2_000128; NCIStruc1_000162; SCHEMBL1969235; GTPL1410; GTPL1412; AC1L456H; MolPort-002-514-399; NCI30079; ZINC2033983; BN0084; CCG-37553; NCGC00013365
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| Activity |
Ki > 1000000 nM
|
[1] | |||
| 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
|
[3] | |||
| Compound Name |
4,8-Dicarboxy-6-oxo-undecanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL164896; SCHEMBL14102824; BDBM50085701
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| Activity |
EC50 > 300000 nM
|
[2] | |||
| 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
|
[3] | |||
| 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
|
[3] | |||
| Compound Name |
(2R,4R)-4-Amino-1-(4-chloro-benzyl)-pyrrolidine-2,4-dicarboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL61964; SCHEMBL8973457; BDBM50071157; (2R,4R)-4-amino-1-[(4-chlorophenyl)methyl]pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
|
[3] | |||
| Compound Name |
(2R,4R)-4-Amino-1-cyclohexylmethyl-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL418650; SCHEMBL8973301; BDBM50071160; (2R,4R)-4-amino-1-(cyclohexylmethyl)pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
|
[3] | |||
| Compound Name |
(2R,4R)-4-Amino-1-benzhydrylpyrrolidine-2,4-dicarboxylic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1169414; SCHEMBL8973161; BDBM50366533
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| Activity |
IC50 > 300000 nM
|
[3] | |||
| Compound Name |
(2R,4R)-4-Amino-1-biphenyl-4-ylmethyl-pyrrolidine-2,4-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL304034; SCHEMBL8973013; BDBM50071158; (2R,4R)-4-amino-1-[(4-phenylphenyl)methyl]pyrrolidine-2,4-dicarboxylic acid
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| Activity |
IC50 > 300000 nM
|
[3] | |||
| 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
|
[3] | |||
| Compound Name |
(2S,4R)-4-(2,2-Diphenylethylamino-3-oxopropyl)glutamic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL480169; BDBM50251894
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| Activity |
IC50 > 1000000 nM
|
[6] | |||
| Compound Name |
(1S,2S)-1-Amino-2-(carboxymethyl)cyclopropane-1-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CTK0H1302; CHEMBL3347671; DTXSID20472068; ZINC32629480; AKOS026740805; Cyclopropaneaceticacid, 2-amino-2-carboxy-, (1S,2S)-
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| Activity |
EC50 > 1000000 nM
|
[5] | |||
| Compound Name |
2-Amino-4-(3-hydroxy-5-methyl-isoxazol-4-yl)-butyric acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL315268; (S)-Homo-AMPA; NCGC00024946-01; Tocris-1026; SCHEMBL12506417; BDBM50060719; (s)-2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid; (S)-2-Amino-4-(3-hydroxy-5-methyl-isoxazol-4-yl)-butyric acid; 2-Amino-4-(3-hydroxy-5-methyl-isoxazol-4-yl)-butyric acid(S-homo-AMPA)
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| Activity |
Ki > 1000000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Ligands for glutamate receptors: design and therapeutic prospects. J Med Chem. 2000 Jul 13;43(14):2609-45. | ||||
| REF 2 | Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity. J Med Chem. 2000 Mar 9;43(5):772-4. | ||||
| REF 3 | 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 4 | Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist. J Med Chem. 2005 May 19;48(10):3605-12. | ||||
| REF 5 | A highly selective agonist for the metabotropic glutamate receptor mGluR2. Medchemcomm. 2011;2:1120-4. | ||||
| REF 6 | Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human exci... J Med Chem. 2008 Jul 24;51(14):4085-92. | ||||
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