| Reaction Details |
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 | Report a problem with these data |
| Target | Corticotropin-releasing factor receptor 1 |
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| Ligand | BDBM50293982 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_572726 (CHEMBL1030150) |
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| IC50 | 0.94±n/a nM |
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| Citation |  Hartz, RA; Ahuja, VT; Arvanitis, AG; Rafalski, M; Yue, EW; Denhart, DJ; Schmitz, WD; Ditta, JL; Deskus, JA; Brenner, AB; Hobbs, FW; Payne, J; Lelas, S; Li, YW; Molski, TF; Mattson, GK; Peng, Y; Wong, H; Grace, JE; Lentz, KA; Qian-Cutrone, J; Zhuo, X; Shu, YZ; Lodge, NJ; Zaczek, R; Combs, AP; Olson, RE; Bronson, JJ; Mattson, RJ; Macor, JE Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists. J Med Chem52:4173-91 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Corticotropin-releasing factor receptor 1 |
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| Name: | Corticotropin-releasing factor receptor 1 |
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| Synonyms: | CRF-R | CRF1 | CRFR1_RAT | CRH-R 1 | Corticotropin releasing factor receptor | Corticotropin releasing factor receptor 1 | Corticotropin-releasing Factor Receptor 1 | Corticotropin-releasing hormone receptor 1 | Crhr | Crhr1 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 47870.75 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Receptor binding assays were performed using rat cortex homogenate. |
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| Residue: | 415 |
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| Sequence: | MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEV
HQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPF
PIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRA
STTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVS
VFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
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| BDBM50293982 |
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| n/a |
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| Name | BDBM50293982 |
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| Synonyms: | (R)-3-(7-Bromo-5-methoxyindolin-1-yl)-5-chloro-1-(1-cyclopropylethyl)pyrazin-2(1H)-one | CHEMBL562161 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H19BrClN3O2 |
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| Mol. Mass. | 424.719 |
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| SMILES | COc1cc2CCN(c2c(Br)c1)c1nc(Cl)cn([C@H](C)C2CC2)c1=O |r| |
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| Structure | 
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