| Reaction Details |
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 | Report a problem with these data |
| Target | Corticotropin-releasing factor receptor 1 |
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| Ligand | BDBM50300137 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_593894 (CHEMBL1037787) |
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| IC50 | 1.5±n/a nM |
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| Citation |  Hartz, RA; Ahuja, VT; Zhuo, X; Mattson, RJ; Denhart, DJ; Deskus, JA; Vrudhula, VM; Pan, S; Ditta, JL; Shu, YZ; Grace, JE; Lentz, KA; Lelas, S; Li, YW; Molski, TF; Krishnananthan, S; Wong, H; Qian-Cutrone, J; Schartman, R; Denton, R; Lodge, NJ; Zaczek, R; Macor, JE; Bronson, JJ A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist. J Med Chem52:7653-68 (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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| BDBM50300137 |
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| n/a |
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| Name | BDBM50300137 |
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| Synonyms: | (R)-5-Chloro-1-(1-cyclopropylethyl)-3-(6-methoxy-2,5-dimethylpyridin-3-ylamino)pyrazin-2(1H)-one | CHEMBL573748 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H21ClN4O2 |
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| Mol. Mass. | 348.827 |
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| SMILES | COc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C |r| |
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| Structure | 
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