| Reaction Details |
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 | Report a problem with these data |
| Target | Corticotropin-releasing factor receptor 1 |
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| Ligand | BDBM50387603 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_830642 (CHEMBL2061535) |
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| IC50 | 1.1±n/a nM |
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| Citation |  Dzierba, CD; Sielecki, TM; Arvanitis, AG; Galka, A; Johnson, TL; Takvorian, AG; Rafalski, M; Kasireddy-Polam, P; Vig, S; Dasgupta, B; Zhang, G; Molski, TF; Wong, H; Zaczek, RC; Lodge, NJ; Combs, AP; Gilligan, PJ; Trainor, GL; Bronson, JJ; Macor, JE Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists. Bioorg Med Chem Lett22:4986-9 (2012) [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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| BDBM50387603 |
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| n/a |
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| Name | BDBM50387603 |
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| Synonyms: | CHEMBL2058598 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H24ClN3O2 |
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| Mol. Mass. | 397.898 |
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| SMILES | CCC(C1CC1)n1c2nccc(-c3cc(C)c(Cl)cc3OC)c2nc(C)c1=O |
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| Structure | 
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