Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT60Q8D)

DTT Name Orexin receptor type 1 (HCRTR1)
Synonyms Ox1r; Ox1-R; Ox-1-R; Orexin-1 receptor; Hypocretin receptor type 1; HFGAN72 receptor; 7-transmembrane G-protein coupledneuropeptide receptor
Gene Name HCRTR1
DTT Type
Clinical trial target
 [1]
BioChemical Class
GPCR rhodopsin
UniProt ID
OX1R_HUMAN
TTD ID
T73482
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEPSATPGAQMGVPPGSREPSPVPPDYEDEFLRYLWRDYLYPKQYEWVLIAAYVAVFVVA
LVGNTLVCLAVWRNHHMRTVTNYFIVNLSLADVLVTAICLPASLLVDITESWLFGHALCK
VIPYLQAVSVSVAVLTLSFIALDRWYAICHPLLFKSTARRARGSILGIWAVSLAIMVPQA
AVMECSSVLPELANRTRLFSVCDERWADDLYPKIYHSCFFIVTYLAPLGLMAMAYFQIFR
KLWGRQIPGTTSALVRNWKRPSDQLGDLEQGLSGEPQPRARAFLAEVKQMRARRKTAKML
MVVLLVFALCYLPISVLNVLKRVFGMFRQASDREAVYACFTFSHWLVYANSAANPIIYNF
LSGKFREQFKAAFSCCLPGLGPCGSLKAPSPRSSASHKSLSLQSRCSISKISEHVVLTSV
TTVLP
Function Triggers an increase in cytoplasmic Ca(2+) levels in response to orexin-A binding. Moderately selective excitatory receptor for orexin-A and, with a lower affinity, for orexin-B neuropeptide.
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
Reactome Pathway
G alpha (q) signalling events (R-HSA-416476 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
3 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
JNJ-61393215 DME2S4D Major depressive disorder 6A70.3 Phase 2 [2]
SB-649868 DMYLBOU Insomnia 7A00-7A0Z Phase 2 [1]
AZD4041 DMEPQI4 Opioid use disorder 6C43.2Z Phase 1 [3]
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33 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
1,2-diamino cyclopentane-based derivative 1 DMNH8GW N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 10 DM3ZF95 N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 11 DMPZECW N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 12 DMWV53X N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 13 DM10UX4 N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 14 DMTZDUV N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 15 DMBY65W N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 16 DMHEX1Q N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 17 DMBC9UK N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 18 DMCNQAF N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 19 DMCBPI4 N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 2 DM7RG5I N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 20 DM9PHIK N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 21 DM5Y1DC N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 22 DMXRLI6 N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 23 DM0HIQU N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 24 DMC26MT N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 25 DMEW0AT N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 26 DMTFG4J N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 27 DM5LQJW N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 29 DM5FVH0 N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 3 DM143OK N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 30 DMZ4NJQ N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 31 DMVZ5EP N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 32 DMQX8SD N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 33 DMBOLSU N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 34 DMVHL3W N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 4 DMFBPSX N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 5 DMCP15K N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 6 DMJ4ACP N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 7 DMHIV24 N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 8 DM7JX8U N. A. N. A. Patented [4]
1,2-diamino cyclopentane-based derivative 9 DM7I8ZV N. A. N. A. Patented [4]
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⏷ Show the Full List of 33 Patented Agent(s)
1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Almorexant DMQALR5 Insomnia 7A00-7A0Z Terminated [5]
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6 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
orexin-B DM0XT69 Discovery agent N.A. Investigative [6]
PMID15261275C1 DMFI4J6 Discovery agent N.A. Investigative [7]
SB-334867 DMDZKWJ Discovery agent N.A. Investigative [5]
SB-408124 DMB8XZP Discovery agent N.A. Investigative [5]
SB-410220 DMQLHE8 Discovery agent N.A. Investigative [8]
[3H]SB-674042 DMO9L38 Discovery agent N.A. Investigative [9]
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⏷ Show the Full List of 6 Investigative Drug(s)

References

1 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
2 Translational evaluation of novel selective orexin-1 receptor antagonist JNJ-61393215 in an experimental model for panic in rodents and humans. Transl Psychiatry. 2020 Sep 7;10(1):308.
3 Clinical pipeline report, company report or official report of AstraZeneca
4 Substituted cyclopentanes, tetrahydrofurans and pyrrolidines as orexin-1-receptor antagonists for treatment of various CNS disorders (WO2015/055994; WO2015/124932; WO2015/124934).Expert Opin Ther Pat. 2016;26(3):409-15.
5 Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison ... Mol Pharmacol. 2009 Sep;76(3):618-31.
6 Agonist ligand discrimination by the two orexin receptors depends on the expression system. Neurosci Lett. 2011 Apr 20;494(1):57-60.
7 Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4225-9.
8 Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141(2):340-6.
9 Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA). Mol Pharmacol. 2010 Jul;78(1):81-93.