Target
Orexin/Hypocretin receptor type 1
Ligand
BDBM205087
Substrate
n/a
Meas. Tech.
FLIPR Ca2+ Flux Assay
IC50
1473±0 nM
Citation
 Kuduk, SDSkudlarek, JW 2-pyridyloxy-4-ester orexin receptor antagonists US Patent  US9556145 Publication Date 1/31/2017 
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:
BDBM205087
Synonyms:
US9556145, example 7 | methyl 2-methyl-6-{[(3r,6r)-6- methyl-1-{[2-(2h-1,2,3-triazol- 2-yl)phenyl]carbonyl}piperidin- 3-yl]oxy}pyridine-4-carboxylate
Type:
Small organic molecule
Emp. Form.:
C23H25N5O4
Mol. Mass.:
435.4757
SMILES:
COC(=O)c1cc(C)nc(O[C@@H]2CC[C@@H](C)N(C2)C(=O)c2ccccc2-n2nccn2)c1
Structure:
Search PDB for entries with ligand similarity: