Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50351370
Substrate
n/a
Meas. Tech.
ChEMBL_764454 (CHEMBL1821006)
EC50
170±n/a nM
Citation
 Saito, TObitsu, TKondo, TMatsui, TNagao, YKusumi, KMatsumura, NUeno, SKishi, AKatsumata, SKagamiishi, YNakai, HToda, M 6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists. Bioorg Med Chem 19:5432-45 (2011) [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:
BDBM50351370
Synonyms:
CHEMBL1819060
Type:
Small organic molecule
Emp. Form.:
C23H30N4O
Mol. Mass.:
378.5105
SMILES:
CCC(CC)Nc1c2CCCc2nc2c(c(C)nn12)-c1ccc(OC)cc1C |(-2.08,4.74,;-3.43,3.99,;-3.46,2.45,;-2.14,1.66,;-.79,2.41,;-4.8,1.71,;-4.83,.17,;-6.18,-.57,;-7.64,-.07,;-8.57,-1.3,;-7.69,-2.56,;-6.21,-2.12,;-4.89,-2.91,;-3.53,-2.16,;-2.08,-2.65,;-1.16,-1.42,;.38,-1.43,;-2.05,-.16,;-3.51,-.62,;-1.62,-4.12,;-2.66,-5.25,;-2.21,-6.72,;-.7,-7.05,;-.24,-8.52,;-1.29,-9.66,;.34,-5.91,;-.12,-4.45,;.92,-3.31,)|
Structure:
Search PDB for entries with ligand similarity: