Reaction Details |
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Target | Corticotropin-releasing factor receptor 1 |
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Ligand | BDBM50293941 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_572726 (CHEMBL1030150) |
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IC50 | 0.42±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 |
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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BDBM50293941 |
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n/a |
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Name | BDBM50293941 |
Synonyms: | (R)-5-Chloro-1-(1-cyclopropylethyl)-3-(4-methoxy-2,5-dimethylphenylamino)pyrazin-2(1H)-one | CHEMBL539670 |
Type | Small organic molecule |
Emp. Form. | C18H22ClN3O2 |
Mol. Mass. | 347.839 |
SMILES | COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C |r| |
Structure |
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