Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50314012
Substrate
n/a
Meas. Tech.
ChEMBL_615933 (CHEMBL1099779)
Ki
27±n/a nM
Citation
 Vrudhula, VMDasgupta, BPin, SSBurris, KDBalanda, LAFung, LKFiedler, TBrowman, KETaber, MTZhang, JMacor, JEDubowchik, GM Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF1R). Bioorg Med Chem Lett 20:1905-9 (2010) [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:
BDBM50314012
Synonyms:
CHEMBL1088624 | N-(cyclobutylmethyl)-2,2,2-trifluoro-N-((8-mesityl-2-(trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidin-3-yl)methyl)ethanamine
Type:
Small organic molecule
Emp. Form.:
C24H30F6N4
Mol. Mass.:
488.5122
SMILES:
Cc1cc(C)c(N2CCCn3c(CN(CC4CCC4)CC(F)(F)F)c(nc23)C(F)(F)F)c(C)c1
Structure:
Search PDB for entries with ligand similarity: