Reaction Details |
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Target | Orexin/Hypocretin receptor type 1 |
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Ligand | BDBM50417257 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_768077 (CHEMBL1833033) |
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Ki | 0.117±n/a nM |
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Citation | Di Fabio, R; Pellacani, A; Faedo, S; Roth, A; Piccoli, L; Gerrard, P; Porter, RA; Johnson, CN; Thewlis, K; Donati, D; Stasi, L; Spada, S; Stemp, G; Nash, D; Branch, C; Kindon, L; Massagrande, M; Poffe, A; Braggio, S; Chiarparin, E; Marchioro, C; Ratti, E; Corsi, M Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett21:5562-7 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Orexin/Hypocretin receptor type 1 |
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Name: | Orexin/Hypocretin receptor type 1 |
Synonyms: | Hcrtr1 | Hypocretin receptor type 1 | OX1R_RAT | Orexin receptor type 1 (OX1) | Orexin receptor type 1 (OX1R) | Ox-1-R | Ox1-R | Ox1R |
Type: | Protein |
Mol. Mass.: | 46817.55 |
Organism: | Rattus norvegicus (Rat) |
Description: | P56718 |
Residue: | 416 |
Sequence: | MEPSATPGAQPGVPTSSGEPFHLPPDYEDEFLRYLWRDYLYPKQYEWVLIAAYVAVFLIA
LVGNTLVCLAVWRNHHMRTVTNYFIVNLSLADVLVTAICLPASLLVDITESWLFGHALCK
VIPYLQAVSVSVAVLTLSFIALDRWYAICHPLLFKSTARRARGSILGIWAVSLAVMVPQA
AVMECSSVLPELANRTRLFSVCDERWADELYPKIYHSCFFFVTYLAPLGLMGMAYFQIFR
KLWGPQIPGTTSALVRNWKRPSEQLEAQHQGLCTEPQPRARAFLAEVKQMRARRKTAKML
MVVLLVFALCYLPISVLNVLKRVFGMFRQASDREAVYACFTFSHWLVYANSAANPIIYNF
LSGKFREQFKAAFSCCLPGLGPSSSARHKSLSLQSRCSVSKVSEHVVLTTVTTVLS
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BDBM50417257 |
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n/a |
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Name | BDBM50417257 |
Synonyms: | SB-649868 |
Type | Small organic molecule |
Emp. Form. | C26H24FN3O3S |
Mol. Mass. | 477.55 |
SMILES | Cc1nc(C(=O)N2CCCC[C@H]2CNC(=O)c2cccc3occc23)c(s1)-c1ccc(F)cc1 |r| |
Structure |
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