Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50351387
Substrate
n/a
Meas. Tech.
ChEMBL_764454 (CHEMBL1821006)
EC50
40±n/a nM
Citation
 Saito, TObitsu, TKondo, TMatsui, TNagao, YKusumi, KMatsumura, NUeno, SKishi, AKatsumata, SKagamiishi, YNakai, HToda, M 6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists. Bioorg Med Chem 19:5432-45 (2011) [PubMed]  Article 
Target
Name:
Corticotropin-releasing factor receptor 1
Synonyms:
CRF-R | CRF-R2 Alpha | CRF1 | CRFR | CRFR1 | CRFR1_HUMAN | CRH-R 1 | CRHR | 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:
BDBM50351387
Synonyms:
CHEMBL1819077
Type:
Small organic molecule
Emp. Form.:
C22H27ClN4O
Mol. Mass.:
398.929
SMILES:
CCC(CC)Nc1c2CCCc2nc2c(c(C)nn12)-c1ccc(OC)cc1Cl |(23.48,-13.44,;22.13,-14.18,;22.1,-15.72,;23.42,-16.52,;24.77,-15.77,;20.75,-16.47,;20.72,-18.01,;19.37,-18.75,;17.91,-18.25,;16.98,-19.48,;17.87,-20.74,;19.34,-20.29,;20.67,-21.09,;22.02,-20.33,;23.48,-20.82,;24.4,-19.59,;25.94,-19.61,;23.51,-18.34,;22.04,-18.8,;23.94,-22.29,;22.89,-23.42,;23.35,-24.89,;24.85,-25.23,;25.31,-26.7,;24.27,-27.83,;25.9,-24.09,;25.44,-22.62,;26.47,-21.49,)|
Structure:
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