Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50320269
Substrate
n/a
Meas. Tech.
ChEMBL_635601 (CHEMBL1118836)
IC50
2.3±n/a nM
Citation
 Schmitz, WD; Brenner, AB; Bronson, JJ; Ditta, JL; Griffin, CR; Li, YW; Lodge, NJ; Molski, TF; Olson, RE; Zhuo, X; Macor, JE 5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists. Bioorg Med Chem Lett 20:3579-83 (2010) [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:
BDBM50320269
Synonyms:
(R)-1-(1-cyclopropyl-2-methoxyethyl)-5-(6-methoxy-2-(trifluoromethyl)pyridin-3-ylamino)-3-methyl-1,2,4-triazin-6(1H)-one | CHEMBL1082358
Type:
Small organic molecule
Emp. Form.:
C17H20F3N5O3
Mol. Mass.:
399.3676
SMILES:
COC[C@@H](C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O |r|
Structure:
Search PDB for entries with ligand similarity: