General Information of Drug (ID: DM01HLX)

Drug Name
GR-127935 Drug Info
Synonyms
148672-13-3; GR 127935; GR-127935; N-(4-Methoxy-3-(4-methylpiperazin-1-yl)phenyl)-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide; GR127935; UNII-2LLH6CEB40; 2'-Methyl-4'-(5-methyl-(1,2,4)-oxadiazol-3-yl)biphenyl-4-carboxylic acid (4-methoxy-3-(4-methylpiperazin-1-yl)phenyl)amide; 2LLH6CEB40; CHEMBL15928; GR 127935 hydrochloride hydrate; N-[4-METHOXY-3-(4-METHYLPIPERAZIN-1-YL)-PHENYL]-4-[2-METHYL-4-(5-METHYL-1,2,4-OXADIAZOL-3-YL)PHENYL]BENZAMIDE; CHEBI:64114; GR 127935 HCl; C29H31N5O3
Indication
Disease Entry ICD 11 Status REF
Major depressive disorder 6A70.3 Terminated [1] , [2]
Cross-matching ID
PubChem CID
107780
ChEBI ID
CHEBI:64114
CAS Number
CAS 148672-13-3
TTD Drug ID
DM01HLX

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting 5-HT 1B receptor (HTR1B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [4]
Eletriptan DMW649X Migraine 8A80 Approved [5]
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [5]
Frovatriptan DM7RE8P Migraine 8A80 Approved [5]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [5]
Naratriptan DMO50U2 Migraine 8A80 Approved [6]
Prolixin decanoate DMMJ1IS Schizophrenia 6A20 Approved [5]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [7]
NXN-188 DMMBAIH Migraine 8A80 Phase 2 [8]
[N-methyl-3H(3)]AZ-10419369 DMSCV02 Mood disorder 6A60-6E23 Phase 1 [9]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 1D receptor (HTR1D)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [10]
Eletriptan DMW649X Migraine 8A80 Approved [5]
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [5]
Frovatriptan DM7RE8P Migraine 8A80 Approved [5]
Sumatriptan DMVYXR8 Migraine 8A80 Approved [11]
Rizatriptan DMDJMA3 Migraine 8A80 Approved [12]
Almogran DM7I64Z Migraine 8A80 Approved [13]
Neu-P11 DMIQDFW Alzheimer disease 8A20 Phase 2 [14]
FKB01MD DM2O7NM N. A. N. A. Phase 2 [15]
NXN-188 DMMBAIH Migraine 8A80 Phase 2 [8]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1B receptor (HTR1B) TTK8CXU 5HT1B_HUMAN Modulator [3]
5-HT 1D receptor (HTR1D) TT6MSOK 5HT1D_HUMAN Modulator [3]

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: 14).
2 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002743)
3 GR127935: a potent and selective 5-HT1D receptor antagonist.Behav Brain Res.1996;73(1-2):157-61.
4 Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem. 1996 Nov;67(5):2096-103.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9.
7 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
8 Company report (NeurAxon)
9 5-HT1B and other related serotonergic proteins are altered in APPswe mutation. Neurosci Lett. 2015 May 6;594:137-43.
10 Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8.
11 Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
12 An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.
13 Efficacy and tolerability of subcutaneous almotriptan for the treatment of acute migraine: a randomized, double-blind, parallel-group, dose-finding study. Clin Ther. 2001 Nov;23(11):1867-75.
14 Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
15 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)