Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50501032
Substrate
n/a
Meas. Tech.
ChEMBL_1575834 (CHEMBL3801877)
IC50
1.2±n/a nM
Citation
 Ahuja, VTHartz, RAMolski, TFMattson, GKLentz, KAGrace, JELodge, NJBronson, JJMacor, JE Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF?) receptor antagonists. Bioorg Med Chem Lett 26:2184-7 (2016) [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:
BDBM50501032
Synonyms:
CHEMBL3799870
Type:
Small organic molecule
Emp. Form.:
C24H24ClF2N5O4
Mol. Mass.:
519.928
SMILES:
Cc1cc(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3)C3CC3)c2=O)c(C)nc1OC(F)F |r|
Structure:
Search PDB for entries with ligand similarity: