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TargetOrexin/Hypocretin receptor type 1
LigandBDBM50447810
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1290419 (CHEMBL3119328)
IC50 3.0±n/a nM
Citation Sifferlen, TBoller, AChardonneau, ACottreel, EHoecker, JAissaoui, HWilliams, JTBrotschi, CHeidmann, BSiegrist, RGatfield, JTreiber, ABrisbare-Roch, CJenck, FBoss, C Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1. Bioorg Med Chem Lett24:1201-8 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Orexin/Hypocretin receptor type 1
Name:Orexin/Hypocretin receptor type 1
Synonyms:HCRTR1 | Hypocretin receptor type 1 | OX1R_HUMAN | Orexin receptor type 1 | Orexin receptor type 1 (OR 1) | Orexin receptor type 1 (OR-1) | Orexin receptor type 1 (OX1) | Orexin receptor type 1 (OX1R) | Orexin receptor type 1 (OxR1) | Ox1r
Type:Protein
Mol. Mass.:47554.50
Organism:Homo sapiens (Human)
Description:O43613
Residue:425
Sequence:
MEPSATPGAQMGVPPGSREPSPVPPDYEDEFLRYLWRDYLYPKQYEWVLIAAYVAVFVVA
LVGNTLVCLAVWRNHHMRTVTNYFIVNLSLADVLVTAICLPASLLVDITESWLFGHALCK
VIPYLQAVSVSVAVLTLSFIALDRWYAICHPLLFKSTARRARGSILGIWAVSLAIMVPQA
AVMECSSVLPELANRTRLFSVCDERWADDLYPKIYHSCFFIVTYLAPLGLMAMAYFQIFR
KLWGRQIPGTTSALVRNWKRPSDQLGDLEQGLSGEPQPRARAFLAEVKQMRARRKTAKML
MVVLLVFALCYLPISVLNVLKRVFGMFRQASDREAVYACFTFSHWLVYANSAANPIIYNF
LSGKFREQFKAAFSCCLPGLGPCGSLKAPSPRSSASHKSLSLQSRCSISKISEHVVLTSV
TTVLP
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  Blast E-value cutoff:
BDBM50447810
n/a
NameBDBM50447810
Synonyms:CHEMBL3113746 | US9242970, 16
TypeSmall organic molecule
Emp. Form.C24H26N2O3S
Mol. Mass.422.54
SMILESCOc1cccc(OC)c1C1CCCC(=O)N1Cc1cccc(c1)-c1csc(C)n1
Structure
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