Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50460176
Substrate
n/a
Meas. Tech.
ChEMBL_1768936 (CHEMBL4221048)
IC50
48±n/a nM
Citation
 Kojima, TMochizuki, MTakai, THoashi, YMorimoto, SSeto, MNakamura, MKobayashi, KSako, YTanaka, MKanzaki, NKosugi, YYano, TAso, K Discovery of 1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazoles as novel class of corticotropin releasing factor 1 receptor antagonists. Bioorg Med Chem 26:2229-2250 (2018) [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:
BDBM50460176
Synonyms:
CHEMBL4229125
Type:
Small organic molecule
Emp. Form.:
C21H19ClF5N3O2
Mol. Mass.:
475.839
SMILES:
COc1ccc(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c32)c(C)c1
Structure:
Search PDB for entries with ligand similarity: