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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM20977
Substrate
125I-Tyr(0)-ovine-CRF
Meas. Tech.
Receptor Binding Assay
pH
7±n/a
Temperature
296.15±n/a K
IC50
0.82±0.2 nM
Citation
 Dzierba, CD; Tebben, AJ; Wilde, RG; Takvorian, AG; Rafalski, M; Kasireddy-Polam, P; Klaczkiewicz, JD; Pechulis, AD; Davis, AL; Sweet, MP; Woo, AM; Yang, Z; Ebeltoft, SM; Molski, TF; Zhang, G; Zaczek, RC; Trainor, GL; Combs, AP; Gilligan, PJ Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling. J Med Chem 50:2269-72 (2007) [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:
BDBM20977
Synonyms:
8-[butyl(ethyl)amino]-4-(2,6-dimethoxypyridin-3-yl)-6-methyl-1H,2H,3H,4H-pyrido[2,3-b]pyrazin-2-one | CHEMBL186097 | Pyridopyrazinone, 2a
Type:
Small organic molecule
Emp. Form.:
C21H29N5O3
Mol. Mass.:
399.4867
SMILES:
CCCCN(CC)c1cc(C)nc2N(CC(=O)Nc12)c1ccc(OC)nc1OC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
125I-Tyr(0)-ovine-CRF
Synonyms:
Ovine Tyr-CRF | oCRF
Type:
radiolabeled substrate
Mol. Mass.:
4833.46
Organism:
Ovis aries (sheep)
Description:
n/a
Residue:
42
Sequence:
YSQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA