Reaction Details  Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50155966
Substrate
n/a
Meas. Tech.
ChEMBL_306679 (CHEMBL830013)
IC50
4.1±n/a nM
Citation
 Dzierba, CD; Takvorian, AG; Rafalski, M; Kasireddy-Polam, P; Wong, H; Molski, TF; Zhang, G; Li, YW; Lelas, S; Peng, Y; McElroy, JF; Zaczek, RC; Taub, RA; Combs, AP; Gilligan, PJ; Trainor, GL Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists. J Med Chem 47:5783-90 (2004) [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:
BDBM50155966
Synonyms:
4-(2-Bromo-4-isopropyl-phenyl)-8-(ethyl-furan-2-ylmethyl-amino)-6-methyl-3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-one | CHEMBL188858
Type:
Small organic molecule
Emp. Form.:
C24H27BrN4O2
Mol. Mass.:
483.401
SMILES:
CCN(Cc1ccco1)c1cc(C)nc2N(CC(=O)Nc12)c1ccc(cc1Br)C(C)C
Structure:
Search PDB for entries with ligand similarity: