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Target
Orexin/Hypocretin receptor type 1
Ligand
BDBM373356
Substrate
n/a
Meas. Tech.
Cell-based Functional Assay
IC50
2.00±n/a nM
Citation
 Kamenecka, TM; He, Y; Nguyen, W; Jiang, R; Song, X; Herr, RJ; Jiang, 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:
BDBM373356
Synonyms:
((2S,3R)-3-Methyl-2-(((5-(trifluoromethyl)pyridin-2-yl)amino)methyl)piperidin-1-yl)(5-methyl-2-(4-methyl-2H-1,2,3-triazol-2-yl)phenyl)methanone | US9896452, Ex. A112
Type:
Small organic molecule
Emp. Form.:
C24H27F3N6O
Mol. Mass.:
472.506
SMILES:
C[C@@H]1CCCN([C@@H]1CNc1ccc(cn1)C(F)(F)F)C(=O)c1cc(C)ccc1-n1ncc(C)n1 |r|
Structure:
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