Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50395828
Substrate
n/a
Meas. Tech.
ChEMBL_860640 (CHEMBL2167614)
IC50
7.8±n/a nM
Citation
 Deskus, JADischino, DDMattson, RJDitta, JLParker, MFDenhart, DJZuev, DHuang, HHartz, RAAhuja, VTWong, HMattson, GKMolski, TFGrace, JEZueva, LNielsen, JMDulac, HLi, YWGuaraldi, MAzure, MOnthank, DHayes, MWexler, EMcDonald, JLodge, NJBronson, JJMacor, JE [18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents. Bioorg Med Chem Lett 22:6651-5 (2012) [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:
BDBM50395828
Synonyms:
CHEMBL2165200
Type:
Small organic molecule
Emp. Form.:
C18H24BrN3O4
Mol. Mass.:
426.305
SMILES:
COCC(COC)n1cc(Br)nc(Nc2c(C)cc(OC)cc2C)c1=O
Structure:
Search PDB for entries with ligand similarity: