Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50293953
Substrate
n/a
Meas. Tech.
ChEMBL_572726 (CHEMBL1030150)
IC50
0.59±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 Chem 52:4173-91 (2009) [PubMed]  Article 
Target
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:
MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEVHQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPFPIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
Inhibitor
Name:
BDBM50293953
Synonyms:
(R)-5-Chloro-3-(4-methoxy-2,5-dimethylphenylamino)-1-[1-(methoxymethyl)propyl]pyrazin-2(1H)-one | CHEMBL552504
Type:
Small organic molecule
Emp. Form.:
C18H24ClN3O3
Mol. Mass.:
365.854
SMILES:
CC[C@H](COC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O |r|
Structure:
Search PDB for entries with ligand similarity: