Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50148887
Substrate
n/a
Meas. Tech.
ChEBML_51104
Ki
2.4±n/a nM
Citation
 Chen, CWilcoxen, KMHuang, CQMcCarthy, JRChen, TGrigoriadis, DE Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility. Bioorg Med Chem Lett 14:3669-73 (2004) [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:
BDBM50148887
Synonyms:
CHEMBL120823 | Cyclopropylmethyl-[3-(2,4-dimethoxy-phenyl)-2,5-dimethyl-3H-pyrazolo[1,5-a]pyrimidin-7-yl]-propyl-amine
Type:
Small organic molecule
Emp. Form.:
C23H30N4O2
Mol. Mass.:
394.5099
SMILES:
CCCN(CC1CC1)c1cc(C)nc2c(c(C)nn12)-c1ccc(OC)cc1OC |(14.58,-6.56,;14.55,-8.11,;15.86,-8.9,;15.82,-10.44,;17.14,-11.26,;17.09,-12.79,;18.4,-13.59,;15.74,-13.52,;14.47,-11.19,;14.42,-12.73,;13.05,-13.48,;13.01,-15,;11.73,-12.65,;11.78,-11.11,;10.69,-10.04,;11.35,-8.64,;10.61,-7.28,;12.88,-8.86,;13.15,-10.37,;9.17,-10.3,;8.65,-11.75,;7.14,-12.03,;6.13,-10.83,;4.63,-11.12,;4.1,-12.56,;6.66,-9.39,;8.18,-9.12,;8.7,-7.66,;7.72,-6.5,)|
Structure:
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