Reaction Details |
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Target | Orexin/Hypocretin receptor type 1 |
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Ligand | BDBM50447810 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1290419 (CHEMBL3119328) |
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IC50 | 3.0±n/a nM |
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Citation | Sifferlen, T; Boller, A; Chardonneau, A; Cottreel, E; Hoecker, J; Aissaoui, H; Williams, JT; Brotschi, C; Heidmann, B; Siegrist, R; Gatfield, J; Treiber, A; Brisbare-Roch, C; Jenck, F; Boss, C Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1. Bioorg Med Chem Lett24:1201-8 (2014) [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_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: | MEPSATPGAQMGVPPGSREPSPVPPDYEDEFLRYLWRDYLYPKQYEWVLIAAYVAVFVVA
LVGNTLVCLAVWRNHHMRTVTNYFIVNLSLADVLVTAICLPASLLVDITESWLFGHALCK
VIPYLQAVSVSVAVLTLSFIALDRWYAICHPLLFKSTARRARGSILGIWAVSLAIMVPQA
AVMECSSVLPELANRTRLFSVCDERWADDLYPKIYHSCFFIVTYLAPLGLMAMAYFQIFR
KLWGRQIPGTTSALVRNWKRPSDQLGDLEQGLSGEPQPRARAFLAEVKQMRARRKTAKML
MVVLLVFALCYLPISVLNVLKRVFGMFRQASDREAVYACFTFSHWLVYANSAANPIIYNF
LSGKFREQFKAAFSCCLPGLGPCGSLKAPSPRSSASHKSLSLQSRCSISKISEHVVLTSV
TTVLP
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BDBM50447810 |
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n/a |
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Name | BDBM50447810 |
Synonyms: | CHEMBL3113746 | US9242970, 16 |
Type | Small organic molecule |
Emp. Form. | C24H26N2O3S |
Mol. Mass. | 422.54 |
SMILES | COc1cccc(OC)c1C1CCCC(=O)N1Cc1cccc(c1)-c1csc(C)n1 |
Structure |
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