Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT9N02I)

DTT Name Orexin receptor type 2 (HCRTR2)
Synonyms Ox2r; Ox2-R; Ox-2-R; Orexin-2 receptor; Hypocretin receptor type 2; HFGANP
Gene Name HCRTR2
DTT Type
Successful target
 [1]
BioChemical Class
GPCR rhodopsin
UniProt ID
OX2R_HUMAN
TTD ID
T69485
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MSGTKLEDSPPCRNWSSASELNETQEPFLNPTDYDDEEFLRYLWREYLHPKEYEWVLIAG
YIIVFVVALIGNVLVCVAVWKNHHMRTVTNYFIVNLSLADVLVTITCLPATLVVDITETW
FFGQSLCKVIPYLQTVSVSVSVLTLSCIALDRWYAICHPLMFKSTAKRARNSIVIIWIVS
CIIMIPQAIVMECSTVFPGLANKTTLFTVCDERWGGEIYPKMYHICFFLVTYMAPLCLMV
LAYLQIFRKLWCRQIPGTSSVVQRKWKPLQPVSQPRGPGQPTKSRMSAVAAEIKQIRARR
KTARMLMIVLLVFAICYLPISILNVLKRVFGMFAHTEDRETVYAWFTFSHWLVYANSAAN
PIIYNFLSGKFREEFKAAFSCCCLGVHHRQEDRLTRGRTSTESRKSLTTQISNFDNISKL
SEQVVLTSISTLPAANGAGPLQNW
Function Triggers an increase in cytoplasmic Ca(2+) levels in response to orexin-A binding. Nonselective, high-affinity receptor for both orexin-A and orexin-B neuropeptides.
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
1 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Suvorexant DM0E6S3 Insomnia 7A00-7A0Z Approved [1]
------------------------------------------------------------------------------------
4 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
MIN-202 DMZFW8V Major depressive disorder 6A70.3 Phase 2 [2]
MK-3697 DM347TQ Insomnia 7A00-7A0Z Phase 2 [3]
TAK-861 DMLGEQ7 Narcolepsy type 1 7A20.0 Phase 2 [4]
TAK-925 DM7N4H9 Narcolepsy 7A20 Phase 1 [5]
------------------------------------------------------------------------------------
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 [6]
1,2-diamino cyclopentane-based derivative 10 DM3ZF95 N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 11 DMPZECW N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 12 DMWV53X N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 13 DM10UX4 N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 14 DMTZDUV N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 15 DMBY65W N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 16 DMHEX1Q N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 17 DMBC9UK N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 18 DMCNQAF N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 19 DMCBPI4 N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 2 DM7RG5I N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 20 DM9PHIK N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 21 DM5Y1DC N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 22 DMXRLI6 N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 23 DM0HIQU N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 24 DMC26MT N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 25 DMEW0AT N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 26 DMTFG4J N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 27 DM5LQJW N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 29 DM5FVH0 N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 3 DM143OK N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 30 DMZ4NJQ N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 31 DMVZ5EP N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 32 DMQX8SD N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 33 DMBOLSU N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 34 DMVHL3W N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 4 DMFBPSX N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 5 DMCP15K N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 6 DMJ4ACP N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 7 DMHIV24 N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 8 DM7JX8U N. A. N. A. Patented [6]
1,2-diamino cyclopentane-based derivative 9 DM7I8ZV N. A. N. A. Patented [6]
------------------------------------------------------------------------------------
⏷ Show the Full List of 33 Patented Agent(s)
8 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
EMPA DM6O2BR Discovery agent N.A. Investigative [7]
JNJ-10397049 DMZ8M0K Insomnia 7A00-7A0Z Investigative [8]
orexin-B DM0XT69 Discovery agent N.A. Investigative [9]
PMID15261275C1 DMFI4J6 Discovery agent N.A. Investigative [10]
SB-334867 DMDZKWJ Discovery agent N.A. Investigative [11]
SB-408124 DMB8XZP Discovery agent N.A. Investigative [11]
TCS-OX2-29 DML8RTO Discovery agent N.A. Investigative [12]
[3H]SB-674042 DMO9L38 Discovery agent N.A. Investigative [11]
------------------------------------------------------------------------------------
⏷ Show the Full List of 8 Investigative Drug(s)

References

1 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90.
4 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
5 Molecular mechanism of the wake-promoting agent TAK-925. Nat Commun. 2022 May 25;13(1):2902.
6 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.
7 Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor. Br J Pharmacol. 2009 Apr;156(8):1326-41.
8 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. (Target id: 322).
9 The signalling profile of recombinant human orexin-2 receptor. Cell Signal. 2008 Sep;20(9):1651-61.
10 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.
11 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.
12 N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4497-9.