Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50340103
Substrate
n/a
Meas. Tech.
ChEMBL_741114 (CHEMBL1764385)
IC50
1.9±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:
BDBM50340103
Synonyms:
CHEMBL1762821 | N-(3-fluoropropyl)-8-(6-methoxy-2-methylpyridin-3-yl)-N-(2-methoxyethyl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
Type:
Small organic molecule
Emp. Form.:
C20H27FN6O2
Mol. Mass.:
402.4658
SMILES:
COCCN(CCCF)c1nc(C)nc2c(c(C)nn12)-c1ccc(OC)nc1C |(4.19,-10.05,;5.52,-9.27,;6.86,-10.04,;8.19,-9.27,;9.53,-10.03,;10.86,-9.26,;12.19,-10.02,;13.53,-9.25,;14.86,-10.02,;9.53,-11.57,;8.2,-12.34,;8.2,-13.89,;6.87,-14.66,;9.54,-14.66,;10.87,-13.89,;12.34,-14.36,;13.25,-13.11,;14.79,-13.11,;12.34,-11.86,;10.87,-12.34,;13.18,-15.65,;12.38,-16.98,;13.13,-18.32,;14.67,-18.35,;15.43,-19.69,;14.64,-21.01,;15.46,-17.01,;14.71,-15.67,;15.5,-14.35,)|
Structure:
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