Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50087559
Substrate
n/a
Meas. Tech.
ChEBML_51284
Ki
2.3±n/a nM
Citation
 Hsin, LWWebster, ELChrousos, GPGold, PWEckelman, WCContoreggi, CRice, KC Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor. Bioorg Med Chem Lett 10:707-10 (2000) [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:
BDBM50087559
Synonyms:
CHEMBL164206 | Cyclopropylmethyl-propyl-[2,5,6-trimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-amine
Type:
Small organic molecule
Emp. Form.:
C25H34N4
Mol. Mass.:
390.5643
SMILES:
CCCN(CC1CC1)c1nc(C)nc2n(c(C)c(C)c12)-c1c(C)cc(C)cc1C |(2.88,-3.62,;4.39,-3.31,;5.41,-4.46,;6.91,-4.14,;7.4,-2.67,;6.37,-1.52,;6.03,-.01,;4.9,-1.05,;7.96,-5.28,;7.47,-6.74,;8.52,-7.89,;8.03,-9.36,;10.01,-7.57,;10.48,-6.1,;11.88,-5.48,;11.72,-3.95,;12.86,-2.92,;10.22,-3.62,;9.6,-2.22,;9.46,-4.95,;13.21,-6.25,;13.21,-7.79,;11.88,-8.56,;14.54,-8.56,;15.89,-7.79,;17.23,-8.56,;15.89,-6.24,;14.54,-5.47,;14.54,-3.93,)|
Structure:
Search PDB for entries with ligand similarity: