Reaction Details  Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50155967
Substrate
n/a
Meas. Tech.
ChEMBL_1522583 (CHEMBL3631936)
Ki
2.4±n/a nM
Citation
 Stehouwer, JS; Bourke, CH; Owens, MJ; Voll, RJ; Kilts, CD; Goodman, MM Synthesis, binding affinity, radiolabeling, and microPET evaluation of 4-(2-substituted-4-substituted)-8-(dialkylamino)-6-methyl-1-substituted-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-ones as ligands for brain corticotropin-releasing factor type-1 (CRF1) receptors. Bioorg Med Chem Lett 25:5111-4 (2015) [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:
415
Sequence:
MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
Inhibitor
Name:
BDBM50155967
Synonyms:
4-(2-Bromo-4-isopropyl-phenyl)-8-(butyl-ethyl-amino)-6-methyl-3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-one | CHEMBL186252
Type:
Small organic molecule
Emp. Form.:
C23H31BrN4O
Mol. Mass.:
459.422
SMILES:
CCCCN(CC)c1cc(C)nc2N(CC(=O)Nc12)c1ccc(cc1Br)C(C)C
Structure:
Search PDB for entries with ligand similarity: