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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50387617
Substrate
n/a
Meas. Tech.
ChEMBL_830642 (CHEMBL2061535)
IC50
2.1±n/a nM
Citation
 Dzierba, CD; Sielecki, TM; Arvanitis, AG; Galka, A; Johnson, TL; Takvorian, AG; Rafalski, M; Kasireddy-Polam, P; Vig, S; Dasgupta, B; Zhang, G; Molski, TF; Wong, H; Zaczek, RC; Lodge, NJ; Combs, AP; Gilligan, PJ; Trainor, GL; Bronson, JJ; Macor, JE Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists. Bioorg Med Chem Lett 22:4986-9 (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:
BDBM50387617
Synonyms:
CHEMBL2057478
Type:
Small organic molecule
Emp. Form.:
C20H21ClFN3O3
Mol. Mass.:
405.85
SMILES:
CCC(COC)n1c2nccc(-c3cc(F)c(OC)cc3Cl)c2nc(C)c1=O
Structure:
Search PDB for entries with ligand similarity: