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] , [2]
Cross-matching ID
PubChem CID
10470232
CAS Number
CAS 409345-76-2
TTD Drug ID
DMX80BL

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Metabotropic glutamate receptor 1 (mGluR1) TTVBPDM GRM1_HUMAN Modulator (allosteric modulator) [3]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Metabotropic glutamate receptor 1 (mGluR1) DTT GRM1 3.888 3.848 3.711 3.678
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Discovery agent
ICD Disease Classification N.A.
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Metabotropic glutamate receptor 1 (mGluR1) DTT GRM1 2.31E-01 -0.05 -0.2
Metabotropic glutamate receptor 1 (mGluR1) DTT GRM1 2.46E-02 0.11 0.74
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

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 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: 6336).
3 [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.