Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50293976
Substrate
n/a
Meas. Tech.
ChEMBL_572726 (CHEMBL1030150)
IC50
910±n/a nM
Citation
Hartz, RA; Ahuja, VT; Arvanitis, AG; Rafalski, M; Yue, EW; Denhart, DJ; Schmitz, WD; Ditta, JL; Deskus, JA; Brenner, AB; Hobbs, FW; Payne, J; Lelas, S; Li, YW; Molski, TF; Mattson, GK; Peng, Y; Wong, H; Grace, JE; Lentz, KA; Qian-Cutrone, J; Zhuo, X; Shu, YZ; Lodge, NJ; Zaczek, R; Combs, AP; Olson, RE; Bronson, JJ; Mattson, RJ; Macor, JE Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists. J Med Chem 52:4173-91 (2009) [PubMed] Article
More Info.:
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:
BDBM50293976
Synonyms:
(R)-3-[4-(Benzyloxy)-2,5-dimethylphenylamino]-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)pyrazin-2(1H)-one | CHEMBL561034
Type:
Small organic molecule
Emp. Form.:
C25H28ClN3O3
Mol. Mass.:
453.961
SMILES:
COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OCc3ccccc3)cc2C)c1=O |r|