General Information of DTT (ID: TTVBPDM)

DTT Name Metabotropic glutamate receptor 1 (mGluR1) DTT Info
Gene Name GRM1

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
4 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
PF-1913539 DMXEU14 Alzheimer disease 8A20 Discontinued in Phase 3 [1]
AZD8529 DMEQ2N1 Schizophrenia 6A20 Discontinued in Phase 2 [2]
AZD-9272 DMYSBN3 Neuropathic pain 8E43.0 Discontinued in Phase 1 [3]
LY-367385 DM98POQ Neurological disorder 6B60 Terminated [6]
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2 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
A-841720 DMSO8IE Pain MG30-MG3Z Preclinical [4]
NPS-2390 DMMRY0Z Cerebrovascular ischaemia 8B1Z Preclinical [5]
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84 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(+)-MCPG DMG5QJB Discovery agent N.A. Investigative [7]
(1S,3R)-ACPD DM5DOAF Discovery agent N.A. Investigative [8]
(3,4-dimethylphenyl)(4-phenoxyphenyl)methanone DMAF43E Discovery agent N.A. Investigative [9]
(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone DMQ9TWD Discovery agent N.A. Investigative [9]
(E)-4,4-Dimethyl-1-quinolin-3-yl-pent-1-en-3-one DMJGAFV Discovery agent N.A. Investigative [9]
(S)-(+)-CBPG DMPDOY8 Discovery agent N.A. Investigative [10]
(S)-3HPG DMQ0FVJ Discovery agent N.A. Investigative [8]
(S)-4C3HPG DMQK4I2 Discovery agent N.A. Investigative [8]
(S)-4CPG DMZ9UIL Discovery agent N.A. Investigative [7]
(S)-TBPG DM68XFZ Discovery agent N.A. Investigative [11]
2-methyl-6-(phenylethynyl)pyridine DMVQK4Y Discovery agent N.A. Investigative [12]
3,5-DHPG DMFEQ6S Discovery agent N.A. Investigative [7]
3,5-dimethyl PPP DM3E98I Discovery agent N.A. Investigative [13]
3-MATIDA DMRMF13 Discovery agent N.A. Investigative [14]
4-(cyclohexyloxy)quinazoline DMCDZ7E Discovery agent N.A. Investigative [15]
6-bromo-N-(3-chlorophenyl)quinazolin-4-amine DM0A3DB Discovery agent N.A. Investigative [16]
A-794278 DM6BRTF Discovery agent N.A. Investigative [17]
A-794282 DMU965M Discovery agent N.A. Investigative [17]
A-850002 DMJCPSD Discovery agent N.A. Investigative [17]
AIDA DM3LCDK Discovery agent N.A. Investigative [7]
BAY 367620 DMVP74I Discovery agent N.A. Investigative [18]
CFMMC DMN8B1S Discovery agent N.A. Investigative [19]
CFMTI DM9HMP4 Discovery agent N.A. Investigative [20]
CPCCOEt DMI4WVE Discovery agent N.A. Investigative [7]
DM-PPP DMUGPD1 Discovery agent N.A. Investigative [13]
FPTQ DMR2NBK Discovery agent N.A. Investigative [21]
FTIDC DM65VLB Discovery agent N.A. Investigative [22]
ibotenate DM8RZE0 Discovery agent N.A. Investigative [8]
JNJ-16567083 DMXNFU5 Discovery agent N.A. Investigative [23]
L-CCG-I DMPZ8XH Discovery agent N.A. Investigative [8]
LY-3390334 DMUXFZQ Discovery agent N.A. Investigative [24]
LY456066 DM86Y1V Discovery agent N.A. Investigative [19]
LY456236 DMROFX8 Discovery agent N.A. Investigative [25]
MK-5435 DMU8VRB Discovery agent N.A. Investigative [26]
N-(2,3-dihydro-1H-inden-2-yl)isoquinolin-1-amine DMTLPDZ Discovery agent N.A. Investigative [15]
N-(2,3-dihydro-1H-inden-2-yl)quinazolin-4-amine DMJ6LI8 Discovery agent N.A. Investigative [15]
N-(2-methyl-2-phenylpropyl)pyrazine-2-carboxamide DMXRSM1 Discovery agent N.A. Investigative [27]
N-(2-phenylpropyl)quinoxaline-2-carboxamide DMA1LRF Discovery agent N.A. Investigative [27]
N-(3-bromophenyl)-6-chloroquinazolin-4-amine DMEWQCN Discovery agent N.A. Investigative [16]
N-(3-bromophenyl)-6-fluoroquinazolin-4-amine DMRIK7P Discovery agent N.A. Investigative [16]
N-cyclohexylquinazolin-4-amine DMJ0T3W Discovery agent N.A. Investigative [15]
N-cyclohexylquinolin-4-amine DMJY2PA Discovery agent N.A. Investigative [15]
N-phenethylquinoxaline-2-carboxamide DM1ZPGY Discovery agent N.A. Investigative [27]
PHCCC DMNJY79 Discovery agent N.A. Investigative [25]
PMID12470711C3 DM1ISJU Discovery agent N.A. Investigative [13]
PMID16099654C3a DMIRSWL Discovery agent N.A. Investigative [28]
PMID16099654C4b DMV8UK1 Discovery agent N.A. Investigative [28]
PMID17064898C29 DMITDEB Discovery agent N.A. Investigative [27]
PMID17276684C22 DMWNYBV Discovery agent N.A. Investigative [29]
PMID17532216C2f DMX3CYG Discovery agent N.A. Investigative [30]
PMID17929793C11c DMDVW4K Discovery agent N.A. Investigative [31]
PMID17929793C23c DMIG308 Discovery agent N.A. Investigative [31]
PMID17929793C23e DMOB07W Discovery agent N.A. Investigative [31]
PMID17929793C23h DM83Z6M Discovery agent N.A. Investigative [31]
PMID17929793C23i DM07TVS Discovery agent N.A. Investigative [31]
PMID19289283C22 DMJRLB5 Discovery agent N.A. Investigative [15]
PMID19289283C32 DMSKGEJ Discovery agent N.A. Investigative [15]
PMID19433355C11q DMPXEIQ Discovery agent N.A. Investigative [32]
PMID19433355C11s DMBU0XJ Discovery agent N.A. Investigative [32]
PMID20346665C24 DMLKFTE Discovery agent N.A. Investigative [33]
PMID20346665C27 DMDKW6G Discovery agent N.A. Investigative [33]
PMID22266036C12e DM4NRG5 Discovery agent N.A. Investigative [34]
PMID22266036C9a DMFQHVL Discovery agent N.A. Investigative [34]
PMID23084894C10i DMURP5Y Discovery agent N.A. Investigative [35]
PMID23084894C9n DM4ATLM Discovery agent N.A. Investigative [35]
Pyrazine-2-carboxylic acid adamantan-1-ylamide DMIZB81 Discovery agent N.A. Investigative [5]
Quinoline-2-carboxylic acid adamantan-1-ylamide DMDY3I2 Discovery agent N.A. Investigative [5]
Quinoline-3-carboxylic acid adamantan-1-ylamide DM9BIVL Discovery agent N.A. Investigative [5]
R214127 DMX80BL Discovery agent N.A. Investigative [7]
Ro01-6128 DM0AC84 Discovery agent N.A. Investigative [36]
Ro0711401 DMZLUAK Discovery agent N.A. Investigative [37]
Ro67-4853 DMD93NP Discovery agent N.A. Investigative [36]
Ro67-7476 DMI95DP Discovery agent N.A. Investigative [36]
VU-71 DMHX1KJ Discovery agent N.A. Investigative [28]
VU0080241 DMUMOV1 Discovery agent N.A. Investigative [38]
VU0469650 DM1H5DL Discovery agent N.A. Investigative [39]
YM-202074 DM3IOLR Discovery agent N.A. Investigative [40]
YM298198 DMUYDXT Discovery agent N.A. Investigative [41]
[11C]MMTP DMQRSP7 Discovery agent N.A. Investigative [42]
[18F]FITM DM4VQNE Discovery agent N.A. Investigative [43]
[18F]FPIT DMRQ6XD Discovery agent N.A. Investigative [44]
[18F]MK-1312 DMQ6AR5 Discovery agent N.A. Investigative [26]
[3H]EM-TBPC DMM1KBW Discovery agent N.A. Investigative [45]
[3H]quisqualate DMDQBTX Discovery agent N.A. Investigative [45]
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⏷ Show the Full List of 84 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Pfizer. Product Development Pipeline. March 31 2009.
2 Clinical pipeline report, company report or official report of AstraZeneca (2009).
3 Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
4 Comparison of the mGluR1 antagonist A-841720 in rat models of pain and cognition. Behav Pharmacol. 2007 Jul;18(4):273-81.
5 Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem. 2008 Feb 14;51(3):634-47.
6 Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur J Pharmacol. 1999 Feb 26;368(1):17-24.
7 [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. Mol Pharmacol. 2003 May;63(5):1082-93.
8 Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J Neurochem. 2000 Dec;75(6):2590-601.
9 Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate recepto... Bioorg Med Chem. 2009 Aug 1;17(15):5708-15.
10 Biochemical and electrophysiological studies on (S)-(+)-2-(3'-carboxybicyclo(1.1.1)pentyl)-glycine (CBPG), a novel mGlu5 receptor agonist endowed with mGlu1 receptor antagonist activity. Neuropharmacology. 1999 Jul;38(7):917-26.
11 Synthesis and biological evaluation of 2-(3'-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist. Bioorg Med Chem. 2001 Feb;9(2):221-7.
12 Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4371-5.
13 Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists. Bioorg Med Chem. 2003 Jan 17;11(2):171-83.
14 The novel and systemically active metabotropic glutamate 1 (mGlu1) receptor antagonist 3-MATIDA reduces post-ischemic neuronal death. Neuropharmacology. 2002 May;42(6):741-51.
15 In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2190-4.
16 Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6.
17 Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. J Med Chem. 2005 Nov 17;48(23):7374-88.
18 BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. Mol Pharmacol. 2001 May;59(5):965-73.
19 Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one. Neuropharmacology. 2009 Sep;57(4):438-45.
20 Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one. J Pharmacol Exp Ther. 2009 Jul;330(1):179-90.
21 Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain. Bioorg Med Chem. 2011 Jan 1;19(1):102-10.
22 Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-... J Pharmacol Exp Ther. 2007 Jun;321(3):1144-53.
23 A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone. J Med Chem. 2005 Aug11;48(16):5096-9.
24 Inhibition of group I metabotropic glutamate receptor responses in vivo in rats by a new generation of carboxyphenylglycine-like amino acid antagon... Neurosci Lett. 2002 Sep 20;330(2):127-30.
25 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 289).
26 Synthesis, characterization, and monkey PET studies of [ ]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435. Synapse. 2011 Feb;65(2):125-35.
27 Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain. Bioorg Med Chem Lett. 2007 Jan 15;17(2):486-90.
28 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4628-31.
29 From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2254-9.
30 Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4303-7.
31 Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain. J Med Chem. 2007 Nov 15;50(23):5550-3.
32 Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3199-203.
33 A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2474-7.
34 Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1575-8.
35 Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7223-6.
36 Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7.
37 Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1666-9.
38 Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel ... Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30.
39 N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8.
40 Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models. Brain Res. 2008 Jan 29;1191:168-79.
41 Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide ... J Pharmacol Exp Ther. 2005 Oct;315(1):163-9.
42 Synthesis, in vitro and in vivo evaluation of [11C]MMTP: a potential PET ligand for mGluR1 receptors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3499-501.
43 Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1. Bioorg Med Chem Lett. 2011 May 15;21(10):2998-3001.
44 Characterization of 1-(2-[18F] fluoro-3-pyridyl)-4-(2-isopropyl-1-oxo- isoindoline-5-yl)-5-methyl-1H-1,2,3-triazole, a PET ligand for imaging the metabotropic glutamate receptor type 1 in rat and monkey brains. J Neurochem. 2012 Apr;121(1):115-24.
45 Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glut... J Biol Chem. 2003 Mar 7;278(10):8340-7.