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Target
Orexin/Hypocretin receptor type 1
Ligand
BDBM373175
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:
BDBM373175
Synonyms:
US9896452, Example 35 | rac-N-((5-fluoro-1-(2-methyl-4-phenylthiazole-5-carbonyl)piperidin-2-yl)methyl)quinoline-8-carboxamide
Type:
Small organic molecule
Emp. Form.:
C27H25FN4O2S
Mol. Mass.:
488.576
SMILES:
Cc1nc(c(s1)C(=O)N1CC(F)CCC1CNC(=O)c1cccc2cccnc12)-c1ccccc1
Structure:
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