| Reaction Details |
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 | Report a problem with these data |
| Target | Corticotropin-releasing factor receptor 1 |
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| Ligand | BDBM50155965 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_306679 (CHEMBL830013) |
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| IC50 | 2.6±n/a nM |
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| Citation |  Dzierba, CD; Takvorian, AG; Rafalski, M; Kasireddy-Polam, P; Wong, H; Molski, TF; Zhang, G; Li, YW; Lelas, S; Peng, Y; McElroy, JF; Zaczek, RC; Taub, RA; Combs, AP; Gilligan, PJ; Trainor, GL Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists. J Med Chem47:5783-90 (2004) [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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| BDBM50155965 |
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| n/a |
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| Name | BDBM50155965 |
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| Synonyms: | 4-(2-Chloro-4-isopropyl-phenyl)-8-[(2-methoxy-ethyl)-propyl-amino]-6-methyl-3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-one; TFA | CHEMBL186517 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H31ClN4O2 |
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| Mol. Mass. | 430.971 |
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| SMILES | CCCN(CCOC)c1cc(C)nc2N(CC(=O)Nc12)c1ccc(cc1Cl)C(C)C |
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| Structure | 
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