Reaction Details |
| Report a problem with these data |
Target | Corticotropin-releasing factor receptor 1 |
---|
Ligand | BDBM50293912 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_572729 (CHEMBL1030153) |
---|
IC50 | 1.9±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 Chem52:4173-91 (2009) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Corticotropin-releasing factor receptor 1 |
---|
Name: | Corticotropin-releasing factor receptor 1 |
Synonyms: | CRF-R | CRF-R2 Alpha | CRF1 | CRFR | CRFR1 | CRFR1_HUMAN | CRH-R 1 | CRHR | CRHR1 | Corticotropin releasing factor receptor 1 | Corticotropin-releasing factor receptor 1 (CRF-1) | Corticotropin-releasing factor receptor 1 (CRF1) | Corticotropin-releasing hormone receptor 1 |
Type: | Enzyme |
Mol. Mass.: | 50744.31 |
Organism: | Homo sapiens (Human) |
Description: | P34998 |
Residue: | 444 |
Sequence: | MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRPGCTHWGDQADGALEVGAPWSGAPFQVRRSIRCLR
NIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGC
YLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYI
YQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFF
VNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARV
ARAMSIPTSPTRVSFHSIKQSTAV
|
|
|
BDBM50293912 |
---|
n/a |
---|
Name | BDBM50293912 |
Synonyms: | (R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-methoxy-2,5-dimethylphenylamino)pyrazin-2(1H)-one | CHEMBL559437 |
Type | Small organic molecule |
Emp. Form. | C19H24ClN3O3 |
Mol. Mass. | 377.865 |
SMILES | COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O |r| |
Structure |
|