Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50074420
Substrate
n/a
Meas. Tech.
ChEMBL_51131 (CHEMBL664192)
Ki
29±n/a nM
Citation
 Hodge, CNAldrich, PEWasserman, ZRFernandez, CHNemeth, GAArvanitis, ACheeseman, RSChorvat, RJCiganek, EChristos, TEGilligan, PJKrenitsky, PScholfield, EStrucely, P Corticotropin-releasing hormone receptor antagonists: framework design and synthesis guided by ligand conformational studies. J Med Chem 42:819-32 (1999) [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:
BDBM50074420
Synonyms:
1-(2-Bromo-4,6-dimethoxy-phenyl)-4,6-dimethyl-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile | CHEMBL169838
Type:
Small organic molecule
Emp. Form.:
C18H16BrN3O2
Mol. Mass.:
386.243
SMILES:
COc1cc(Br)c(c(OC)c1)-n1cc(C#N)c2c(C)cc(C)nc12 |(12.47,-15.06,;10.97,-14.75,;10.48,-13.3,;11.5,-12.14,;11.01,-10.69,;12.02,-9.53,;9.5,-10.37,;8.48,-11.53,;6.98,-11.21,;5.96,-12.35,;8.97,-12.98,;9.03,-8.92,;9.92,-7.66,;9.01,-6.42,;9.48,-4.95,;9.95,-3.48,;7.54,-6.91,;6.21,-6.14,;6.21,-4.6,;4.88,-6.91,;4.88,-8.45,;3.55,-9.22,;6.21,-9.22,;7.56,-8.45,)|
Structure:
Search PDB for entries with ligand similarity: