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Target
Orexin/Hypocretin receptor type 1
Ligand
BDBM50596486
Substrate
n/a
Meas. Tech.
ChEMBL_2220531 (CHEMBL5133865)
EC50
14±n/a nM
Citation
 Iio, K; Saitoh, T; Ohshita, R; Hino, T; Amezawa, M; Takayama, Y; Nagumo, Y; Yamamoto, N; Kutsumura, N; Irukayama-Tomobe, Y; Ishikawa, Y; Tanimura, R; Yanagisawa, M; Nagase, H Discovery of orexin 2 receptor selective and dual orexin receptor agonists based on the tetralin structure: Switching of receptor selectivity by chirality on the tetralin ring. Bioorg Med Chem Lett 60:0 (2022) [PubMed] 
Target
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:
MEPSATPGAQMGVPPGSREPSPVPPDYEDEFLRYLWRDYLYPKQYEWVLIAAYVAVFVVALVGNTLVCLAVWRNHHMRTVTNYFIVNLSLADVLVTAICLPASLLVDITESWLFGHALCKVIPYLQAVSVSVAVLTLSFIALDRWYAICHPLLFKSTARRARGSILGIWAVSLAIMVPQAAVMECSSVLPELANRTRLFSVCDERWADDLYPKIYHSCFFIVTYLAPLGLMAMAYFQIFRKLWGRQIPGTTSALVRNWKRPSDQLGDLEQGLSGEPQPRARAFLAEVKQMRARRKTAKMLMVVLLVFALCYLPISVLNVLKRVFGMFRQASDREAVYACFTFSHWLVYANSAANPIIYNFLSGKFREQFKAAFSCCLPGLGPCGSLKAPSPRSSASHKSLSLQSRCSISKISEHVVLTSVTTVLP
  
Inhibitor
Name:
BDBM50596486
Synonyms:
CHEMBL5203887
Type:
Small organic molecule
Emp. Form.:
C36H39N3O6S
Mol. Mass.:
641.776
SMILES:
COc1cccc(CC(=O)N(C)[C@@H]2CCCc3ccc(NS(=O)(=O)c4cc(ccc4OC)-c4cccc(c4)C(=O)N(C)C)cc23)c1 |r|
Structure:
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