Target
Orexin/Hypocretin receptor type 1
Ligand
BDBM373137
Substrate
n/a
Meas. Tech.
Cell-based Functional Assay
IC50
1.000±n/a nM
Citation
 Kamenecka, TMHe, YNguyen, WJiang, RSong, XHerr, RJJiang, Q Substituted prolines/piperidines as orexin receptor antagonists US Patent  US9896452 Publication Date 2/20/2018 
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:
BDBM373137
Synonyms:
US9896452, Example 2 | rac-N-((5-fluoro-1-(2-methyl-5-phenylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide
Type:
Small organic molecule
Emp. Form.:
C26H24FN3O3S
Mol. Mass.:
477.55
SMILES:
Cc1nc(C(=O)N2CC(F)CCC2CNC(=O)c2cccc3occc23)c(s1)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: