Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50131716
Substrate
n/a
Meas. Tech.
ChEMBL_51128 (CHEMBL663563)
Ki
1.9±n/a nM
Citation
 Jagoda, EContoreggi, CLee, MJKao, CHSzajek, LPListwak, SGold, PChrousos, GGreiner, EKim, BMJacobson, AERice, KCEckelman, W Autoradiographic visualization of corticotropin releasing hormone type 1 receptors with a nonpeptide ligand: synthesis of [(76)Br]MJL-1-109-2. J Med Chem 46:3559-62 (2003) [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:
BDBM50131716
Synonyms:
CHEMBL430892 | [3-(4-Bromo-2-chloro-phenyl)-2,5-dimethyl-[1,2,4]triazolo[1,5-a][1,3,5]triazin-7-yl]-bis-(2-methoxy-ethyl)-amine
Type:
Small organic molecule
Emp. Form.:
C19H23BrClN5O2
Mol. Mass.:
468.775
SMILES:
COCCN(CCOC)c1nc(C)nc2c(c(C)nn12)-c1ccc(Br)cc1Cl |(2.5,2.36,;1.17,3.13,;-.17,2.36,;-1.5,3.12,;-2.85,2.35,;-4.18,3.11,;-5.51,2.34,;-6.84,3.11,;-8.17,2.34,;-2.83,.81,;-4.16,.04,;-4.16,-1.51,;-5.51,-2.28,;-2.83,-2.28,;-1.49,-1.5,;-.03,-1.98,;.88,-.73,;2.42,-.73,;-.03,.52,;-1.49,.04,;.44,-3.44,;-.59,-4.58,;-.12,-6.04,;1.39,-6.36,;1.87,-7.83,;2.43,-5.21,;1.94,-3.75,;2.96,-2.61,)|
Structure:
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