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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50293912
Substrate
n/a
Meas. Tech.
ChEMBL_572700
IC50
0.26±n/a nM
Citation
 Hartz, RA; Ahuja, VT; Rafalski, M; Schmitz, WD; Brenner, AB; Denhart, DJ; Ditta, JL; Deskus, JA; Yue, EW; Arvanitis, AG; Lelas, S; Li, YW; Molski, TF; Wong, H; Grace, JE; Lentz, KA; Li, J; Lodge, NJ; Zaczek, R; Combs, AP; Olson, RE; Mattson, RJ; Bronson, JJ; Macor, JE In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. J Med Chem 52:4161-72 (2009) [PubMed]  Article  BDB Entry
Target
Name:
Corticotropin-releasing factor receptor 1
Synonyms:
CRF-R | CRF1 | CRH-R 1 | CRHR1 | Corticotropin releasing factor receptor | Corticotropin releasing factor receptor 1 | Corticotropin-releasing Factor Receptor 1 | Corticotropin-releasing hormone receptor 1
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:
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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