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

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]

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 Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting 5-HT 1B receptor (HTR1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[3]
Eletriptan	DMW649X	Migraine	8A80	Approved	[4]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[4]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[4]
Fluphenazine	DMIT8LX	Psychotic disorder	6A20-6A25	Approved	[4]
Naratriptan	DMO50U2	Headache	8A80-8A84	Approved	[5]
Prolixin decanoate	DMMJ1IS	Schizophrenia	6A20	Approved	[4]
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[6]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[7]
[N-methyl-3H(3)]AZ-10419369	DMSCV02	Mood disorder	6A60-6E23	Phase 1	[8]
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Drug(s) Targeting 5-HT 1D receptor (HTR1D)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[9]
Eletriptan	DMW649X	Migraine	8A80	Approved	[4]
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[4]
Frovatriptan	DM7RE8P	Migraine	8A80	Approved	[4]
Sumatriptan	DMVYXR8	Cluster headache	8A81.0	Approved	[10]
Rizatriptan	DMDJMA3	Migraine	8A80	Approved	[11]
Almogran	DM7I64Z	Migraine	8A80	Approved	[12]
Neu-P11	DMIQDFW	Alzheimer disease	8A20	Phase 2	[13]
FKB01MD	DM2O7NM	N. A.	N. A.	Phase 2	[14]
NXN-188	DMMBAIH	Migraine	8A80	Phase 2	[7]
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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
5-HT 1B receptor (HTR1B)	TTK8CXU	5HT1B_HUMAN	Modulator	[2]
5-HT 1D receptor (HTR1D)	TT6MSOK	5HT1D_HUMAN	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: 14).
2	GR127935: a potent and selective 5-HT1D receptor antagonist.Behav Brain Res.1996;73(1-2):157-61.
3	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.
4	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5	Triptans in pregnancy. Ther Drug Monit. 2008 Feb;30(1):5-9.
6	Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
7	Company report (NeurAxon)
8	5-HT1B and other related serotonergic proteins are altered in APPswe mutation. Neurosci Lett. 2015 May 6;594:137-43.
9	Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol. 1991 Aug;40(2):143-8.
10	Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
11	An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210.
12	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.
13	Clinical pipeline report, company report or official report of Neurim Pharmaceuticals.
14	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)