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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM20971
Substrate
125I-Tyr(0)-ovine-CRF
Meas. Tech.
Receptor Binding Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
3.7±n/a nM
Citation
 Chen, YL; Obach, RS; Braselton, J; Corman, ML; Forman, J; Freeman, J; Gallaschun, RJ; Mansbach, R; Schmidt, AW; Sprouse, JS; Tingley Iii, FD; Winston, E; Schulz, DW 2-Aryloxy-4-alkylaminopyridines: Discovery of Novel Corticotropin-Releasing Factor 1 Antagonists. J Med Chem 51:1385-92 (2008) [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:
BDBM20971
Synonyms:
2-Arylamino-4-alkyloxypyridine, 13 | 3,6-dimethyl-4-(pentan-3-yloxy)-N-(2,4,6-trimethylphenyl)pyridin-2-amine
Type:
Small organic molecule
Emp. Form.:
C21H30N2O
Mol. Mass.:
326.4757
SMILES:
CCC(CC)Oc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C
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