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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50152040
Substrate
n/a
Meas. Tech.
ChEMBL_306747 (CHEMBL830892)
IC50
113±n/a nM
Citation
 Hartz, RA; Nanda, KK; Ingalls, CL; Ahuja, VT; Molski, TF; Zhang, G; Wong, H; Peng, Y; Kelley, M; Lodge, NJ; Zaczek, R; Gilligan, PJ; Trainor, GL Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists. J Med Chem 47:4741-54 (2004) [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:
BDBM50152040
Synonyms:
3-(2-Chloro-4-methoxy-phenyl)-7-(1-cyclopropyl-propyl)-8-ethyl-1-methyl-1,2,3,7-tetrahydro-purin-6-one | CHEMBL181259
Type:
Small organic molecule
Emp. Form.:
C21H27ClN4O2
Mol. Mass.:
402.918
SMILES:
CCC(C1CC1)n1c(CC)nc2N(CN(C)C(=O)c12)c1ccc(OC)cc1Cl
Structure:
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