Reaction Details |
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Target | Corticotropin-releasing factor receptor 1 |
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Ligand | BDBM50387616 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_830642 (CHEMBL2061535) |
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IC50 | 3±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 |
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 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 47870.75 |
Organism: | Rattus norvegicus (rat) |
Description: | Receptor binding assays were performed using rat cortex homogenate. |
Residue: | 415 |
Sequence: | MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEV
HQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPF
PIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRA
STTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVS
VFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
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BDBM50387616 |
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n/a |
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Name | BDBM50387616 |
Synonyms: | CHEMBL2057477 |
Type | Small organic molecule |
Emp. Form. | C23H25N3O2 |
Mol. Mass. | 375.4635 |
SMILES | COc1ccc(c(C)c1)-c1ccnc2n(C(C3CC3)C3CC3)c(=O)c(C)nc12 |
Structure |
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