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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50293912
Substrate
n/a
Meas. Tech.
ChEMBL_572729
IC50
1.9±n/a nM
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 Chem 52:4173-91 (2009) [PubMed]  Article  BDB Entry
Target
Name:
Corticotropin-releasing factor receptor 1
Synonyms:
CRF-R | CRF-R2 Alpha | CRF1 | CRH-R 1 | CRHR1 | Corticotropin releasing factor receptor 1 | Corticotropin-releasing factor receptor 1 (CRF-1) | Corticotropin-releasing factor receptor 1 (CRF1) | Corticotropin-releasing hormone receptor 1
Type:
Enzyme
Mol. Mass.:
50744.31
Organism:
Homo sapiens (Human)
Description:
P34998
Residue:
444
Sequence:
MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRPGCTHWGDQADGALEVGAPWSGAPFQVRRSIRCLRNIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
Inhibitor
Name:
BDBM50293912
Synonyms:
(R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-methoxy-2,5-dimethylphenylamino)pyrazin-2(1H)-one | CHEMBL559437
Type:
Small organic molecule
Emp. Form.:
C19H24ClN3O3
Mol. Mass.:
377.865
SMILES:
COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O |r|
Structure:
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