Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50058166
Substrate
n/a
Meas. Tech.
ChEMBL_51280 (CHEMBL664982)
IC50
>10000±n/a nM
Citation
 Chen, YLMansbach, RSWinter, SMBrooks, ECollins, JCorman, MLDunaiskis, ARFaraci, WSGallaschun, RJSchmidt, ASchulz, DW Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. J Med Chem 40:1749-54 (1997) [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:
BDBM50058166
Synonyms:
2,5-Dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine | CHEMBL300278
Type:
Small organic molecule
Emp. Form.:
C17H20N4
Mol. Mass.:
280.3675
SMILES:
Cc1cn(-c2c(C)cc(C)cc2C)c2nc(C)nc(N)c12 |(6.98,.43,;6.51,-1.03,;7.42,-2.27,;6.51,-3.53,;6.99,-5,;8.48,-5.3,;9.51,-4.16,;8.96,-6.76,;7.93,-7.91,;8.41,-9.38,;6.43,-7.58,;5.95,-6.13,;4.44,-5.81,;5.04,-3.05,;3.71,-3.82,;2.38,-3.05,;1.03,-3.82,;2.38,-1.51,;3.71,-.73,;3.69,.81,;5.04,-1.5,)|
Structure:
Search PDB for entries with ligand similarity: