Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50340107
Substrate
n/a
Meas. Tech.
ChEMBL_741114 (CHEMBL1764385)
IC50
>10000±n/a nM
Citation
 Zuev, D; Mattson, RJ; Huang, H; Mattson, GK; Zueva, L; Nielsen, JM; Kozlowski, ES; Huang, XS; Wu, D; Gao, Q; Lodge, NJ; Bronson, JJ; Macor, JE Potential CRF1R PET imaging agents: N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines. Bioorg Med Chem Lett 21:2484-8 (2011) [PubMed]  Article 
Target
Name:
Corticotropin-releasing factor receptor 1
Synonyms:
CRF-R | CRF1 | CRFR1_RAT | CRH-R 1 | Corticotropin releasing factor receptor | Corticotropin releasing factor receptor 1 | Corticotropin-releasing Factor Receptor 1 | Corticotropin-releasing hormone receptor 1 | Crhr | Crhr1
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
47870.75
Organism:
Rattus norvegicus (rat)
Description:
Receptor binding assays were performed using rat cortex homogenate.
Residue:
415
Sequence:
MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPAGQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAVIINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEVHQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPFPIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
  
Inhibitor
Name:
BDBM50340107
Synonyms:
8-(2,4-dimethoxypyrimidin-5-yl)-N-(3-fluoropropyl)-N-(2-methoxyethyl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine | CHEMBL1762825
Type:
Small organic molecule
Emp. Form.:
C19H26FN7O3
Mol. Mass.:
419.4532
SMILES:
COCCN(CCCF)c1nc(C)nc2c(c(C)nn12)-c1cnc(OC)nc1OC |(20.11,-25.39,;21.44,-24.61,;22.77,-25.38,;24.1,-24.6,;25.44,-25.37,;26.77,-24.6,;28.11,-25.36,;29.44,-24.59,;30.78,-25.35,;25.45,-26.91,;24.12,-27.68,;24.11,-29.23,;22.78,-29.99,;25.45,-30,;26.78,-29.22,;28.25,-29.7,;29.17,-28.45,;30.71,-28.45,;28.25,-27.19,;26.78,-27.67,;29.08,-31,;28.28,-32.32,;29.02,-33.66,;30.56,-33.7,;31.31,-35.04,;30.51,-36.36,;31.36,-32.37,;30.61,-31.03,;31.41,-29.71,;32.95,-29.73,)|
Structure:
Search PDB for entries with ligand similarity: