Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50340104
Substrate
n/a
Meas. Tech.
ChEMBL_741114 (CHEMBL1764385)
IC50
6.5±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:
BDBM50340104
Synonyms:
3-((3-fluoropropyl)(8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-yl)amino)propanenitrile | CHEMBL1762822
Type:
Small organic molecule
Emp. Form.:
C20H24FN7O
Mol. Mass.:
397.4493
SMILES:
COc1ccc(-c2c(C)nn3c(nc(C)nc23)N(CCCF)CCC#N)c(C)n1 |(31.44,-21.09,;32.23,-19.77,;31.49,-18.43,;29.95,-18.4,;29.2,-17.05,;30,-15.73,;29.17,-14.43,;30.08,-13.18,;31.62,-13.18,;29.17,-11.93,;27.7,-12.41,;26.36,-11.64,;25.03,-12.41,;25.03,-13.96,;23.7,-14.73,;26.37,-14.73,;27.7,-13.96,;26.36,-10.1,;27.69,-9.33,;29.03,-10.09,;30.36,-9.32,;31.69,-10.09,;25.02,-9.34,;23.69,-10.11,;22.35,-9.34,;21.02,-8.58,;31.53,-15.76,;32.33,-14.43,;32.28,-17.1,)|
Structure:
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