Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50351398
Substrate
n/a
Meas. Tech.
ChEMBL_764454 (CHEMBL1821006)
EC50
8±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:
BDBM50351398
Synonyms:
CHEMBL1819088
Type:
Small organic molecule
Emp. Form.:
C21H25ClN4O2
Mol. Mass.:
400.902
SMILES:
CCC(CC)Nc1c2CCOc2nc2c(c(C)nn12)-c1ccc(OC)cc1Cl |(15.19,-12.03,;13.84,-12.77,;13.81,-14.31,;15.13,-15.11,;16.48,-14.36,;12.46,-15.06,;12.43,-16.6,;11.08,-17.34,;9.62,-16.84,;8.69,-18.07,;9.58,-19.33,;11.05,-18.89,;12.38,-19.74,;13.73,-18.92,;15.19,-19.42,;16.11,-18.18,;17.65,-18.2,;15.22,-16.93,;13.75,-17.39,;15.65,-20.89,;14.6,-22.02,;15.06,-23.48,;16.56,-23.82,;17.02,-25.29,;15.98,-26.43,;17.61,-22.68,;17.15,-21.22,;18.19,-20.08,)|
Structure:
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