Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50394530
Substrate
n/a
Meas. Tech.
ChEMBL_855115 (CHEMBL2160873)
IC50
414±n/a nM
Citation
 Takeda, KTerauchi, THashizume, MShikata, KTaguchi, RMurata-Tai, KFujisawa, MTakahashi, YShin, KIno, MShibata, HYonaga, M Synthesis and structure-activity relationships of 8-substituted-2-aryl-5-alkylaminoquinolines: Potent, orally active corticotropin-releasing factor-1 receptor antagonists. Bioorg Med Chem 20:6559-78 (2012) [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:
Human
Description:
P34998
Residue:
415
Sequence:
MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
Inhibitor
Name:
BDBM50394530
Synonyms:
CHEMBL2160162
Type:
Small organic molecule
Emp. Form.:
C25H30F2N2O3
Mol. Mass.:
444.5141
SMILES:
CCN(CC)c1ccc(C(F)F)c2nc(c(C)cc12)-c1c(OC)cc(COC)cc1OC |(4.63,5.81,;3.3,5.02,;1.97,5.78,;1.95,7.32,;3.28,8.1,;.64,5,;-.7,5.76,;-2.03,4.98,;-2.02,3.44,;-3.35,2.66,;-4.69,3.42,;-3.34,1.12,;-.68,2.68,;-.67,1.14,;.67,.38,;2,1.16,;3.34,.4,;1.99,2.7,;.65,3.46,;.68,-1.16,;-.65,-1.94,;-1.99,-1.18,;-3.32,-1.96,;-.64,-3.48,;.7,-4.24,;.71,-5.78,;-.61,-6.56,;-.6,-8.1,;2.03,-3.46,;2.02,-1.92,;3.35,-1.14,;4.69,-1.9,)|
Structure:
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