Target
Orexin/Hypocretin receptor type 1
Ligand
BDBM274920
Substrate
n/a
Meas. Tech.
Intracellular Calcium Assay
IC50
10000±n/a nM
Citation
 Kuduk, SDSkudlarek, JW Piperidinyloxy lactone orexin receptor antagonists US Patent  US9556190 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:
BDBM274920
Synonyms:
4-{[(3R,6R)-1-{[4-fluoro-2-(2H-1,2,3- triazol-2-yl)phenyl]carbonyl}-6- methylpiperidin-3-yl]oxy}-1,1- dimethylfuro[3,4-c]pyridin-3(1H)-one | US9556190, Example 10
Type:
Small organic molecule
Emp. Form.:
C24H24FN5O4
Mol. Mass.:
465.4769
SMILES:
C[C@@H]1CC[C@H](CN1C(=O)c1ccc(F)cc1-n1nccn1)Oc1nccc2c1C(=O)OC2(C)C |r|
Structure:
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