Reaction Details Report a problem with these data
Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM20959
Substrate
125I-Tyr(0)-ovine-CRF
Meas. Tech.
Receptor Binding Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
3.2±n/a nM
Citation
 Chen, YL; Braselton, J; Forman, J; Gallaschun, RJ; Mansbach, R; Schmidt, AW; Seeger, TF; Sprouse, JS; Tingley, FD; Winston, E; Schulz, DW Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists. J Med Chem 51:1377-84 (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:
BDBM20959
Synonyms:
2-Aryloxy-4-alkoxy-pyridine, 40 | 2-[4-(methoxymethyl)-2,6-dimethylphenoxy]-3,6-dimethyl-4-(pentan-3-yloxy)pyridine
Type:
Small organic molecule
Emp. Form.:
C22H31NO3
Mol. Mass.:
357.4864
SMILES:
CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(COC)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