Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMX80BL)

Drug Name

R214127 Drug Info

Synonyms

HXUSRWUBSYSWII-UHFFFAOYSA-N; CHEMBL369459; 409345-76-2; R 214127; Ethanone, 1-(3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-2-phenyl-; 1-(3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-2-phenylethanone; [3H]R214127; [3H]-R214127; SCHEMBL662314; R-214127; GTPL1391; GTPL6336; CTK1D4173; DTXSID20440505; ZINC3817902; PDSP2_000348; PDSP1_000350; BDBM50163606; AKOS028110267; L022369; 1-(3,4-Dihydro-2H-1-oxa-9-aza-anthracen-6-yl)-2-phenyl-ethanone; R 214127

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

Cross-matching ID

PubChem CID: 10470232
CAS Number: CAS 409345-76-2
TTD Drug ID: DMX80BL

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Discontinued Drug(s)

Preclinical Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Metabotropic glutamate receptor 1 (mGluR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PF-1913539	DMXEU14	Alzheimer disease	8A20	Discontinued in Phase 3	[3]
AZD8529	DMEQ2N1	Schizophrenia	6A20	Discontinued in Phase 2	[4]
AZD-9272	DMYSBN3	Neuropathic pain	8E43.0	Discontinued in Phase 1	[5]
NPS-2390	DMMRY0Z	Cerebrovascular ischaemia	8B1Z	Preclinical	[6]
A-841720	DMSO8IE	Pain	MG30-MG3Z	Preclinical	[7]
LY-367385	DM98POQ	Neurological disorder	6B60	Terminated	[8]
[3H]quisqualate	DMDQBTX	Discovery agent	N.A.	Investigative	[9]
L-CCG-I	DMPZ8XH	Discovery agent	N.A.	Investigative	[10]
(1S,3R)-ACPD	DM5DOAF	Discovery agent	N.A.	Investigative	[10]
(+)-MCPG	DMG5QJB	Discovery agent	N.A.	Investigative	[2]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Metabotropic glutamate receptor 1 (mGluR1)	TTVBPDM	GRM1_HUMAN	Modulator (allosteric modulator)	[2]

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References

1	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. (Ligand id: 1391).
2	[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.
3	Pfizer. Product Development Pipeline. March 31 2009.
4	Clinical pipeline report, company report or official report of AstraZeneca (2009).
5	Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
6	Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem. 2008 Feb 14;51(3):634-47.
7	Comparison of the mGluR1 antagonist A-841720 in rat models of pain and cognition. Behav Pharmacol. 2007 Jul;18(4):273-81.
8	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.
9	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.
10	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.