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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM50313857
Substrate
n/a
Meas. Tech.
ChEMBL_615438 (CHEMBL1106905)
IC50
65±n/a nM
Citation
 Hartz, RA; Ahuja, VT; Schmitz, WD; Molski, TF; Mattson, GK; Lodge, NJ; Bronson, JJ; Macor, JE Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. Bioorg Med Chem Lett 20:1890-4 (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:
BDBM50313857
Synonyms:
(R)-5-chloro-1-(1-cyclopropylethyl)-3-(2,4,6-trimethylpyridin-3-ylamino)pyrazin-2(1H)-one | CHEMBL1085683
Type:
Small organic molecule
Emp. Form.:
C17H21ClN4O
Mol. Mass.:
332.828
SMILES:
C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(C)nc2C)c1=O |r|
Structure:
Search PDB for entries with ligand similarity: