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TargetCorticotropin-releasing factor receptor 1
LigandBDBM50293967
Substrate/Competitorn/a
Meas. Tech.ChEMBL_572726 (CHEMBL1030150)
IC50 1.7±n/a nM
Citation Hartz, RAAhuja, VTArvanitis, AGRafalski, MYue, EWDenhart, DJSchmitz, WDDitta, JLDeskus, JABrenner, ABHobbs, FWPayne, JLelas, SLi, YWMolski, TFMattson, GKPeng, YWong, HGrace, JELentz, KAQian-Cutrone, JZhuo, XShu, YZLodge, NJZaczek, RCombs, APOlson, REBronson, JJMattson, RJMacor, 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
More Info.:Get all data from this article,  Assay Method
 
Corticotropin-releasing factor receptor 1
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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  Blast E-value cutoff:
BDBM50293967
n/a
NameBDBM50293967
Synonyms:(R)-5-Chloro-3-(4-methoxy-2,5-dimethylphenylamino)-1-(2-methoxy-1-methylethyl)pyrazin-2(1H)-one | CHEMBL550685
TypeSmall organic molecule
Emp. Form.C17H22ClN3O3
Mol. Mass.351.828
SMILESCOC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O |r|
Structure
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