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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50394517
Substrate
n/a
Meas. Tech.
ChEMBL_855116 (CHEMBL2160874)
IC50
65±n/a nM
Citation
 Takeda, K; Terauchi, T; Hashizume, M; Shikata, K; Taguchi, R; Murata-Tai, K; Fujisawa, M; Takahashi, Y; Shin, K; Ino, M; Shibata, H; Yonaga, 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:
Homo sapiens (Human)
Description:
P34998
Residue:
444
Sequence:
MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRPGCTHWGDQADGALEVGAPWSGAPFQVRRSIRCLRNIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
Inhibitor
Name:
BDBM50394517
Synonyms:
CHEMBL2160173
Type:
Small organic molecule
Emp. Form.:
C28H38N2O5
Mol. Mass.:
482.6117
SMILES:
COCCN(CC(C)C)c1ccc(OC)c2nc(c(C)cc12)-c1c(OC)cc(COC)cc1OC |(1.41,9.22,;.07,8.47,;.05,6.93,;1.37,6.14,;1.35,4.6,;2.68,3.82,;4.02,4.57,;5.34,3.78,;4.04,6.11,;.01,3.85,;-1.31,4.64,;-2.66,3.88,;-2.68,2.34,;-4.02,1.59,;-5.34,2.38,;-1.35,1.56,;-1.37,.02,;-.05,-.77,;1.29,-.02,;2.62,-.8,;1.31,1.52,;-.01,2.31,;-.07,-2.31,;-1.41,-3.06,;-2.74,-2.28,;-4.08,-3.03,;-1.43,-4.6,;-.11,-5.39,;-.13,-6.93,;-1.47,-7.68,;-1.49,-9.22,;1.24,-4.64,;1.25,-3.1,;2.6,-2.34,;3.92,-3.13,)|
Structure:
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