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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM29432
Substrate
125I-Tyr(0)-ovine-CRF
Meas. Tech.
In Vitro Binding Autoradiography
pH
7.2±n/a
Temperature
296.15±n/a K
IC50
11.52±2.46 nM
Citation
 Gilligan, PJ; He, L; Clarke, T; Tivitmahaisoon, P; Lelas, S; Li, YW; Heman, K; Fitzgerald, L; Miller, K; Zhang, G; Marshall, A; Krause, C; McElroy, J; Ward, K; Shen, H; Wong, H; Grossman, S; Nemeth, G; Zaczek, R; Arneric, SP; Hartig, P; Robertson, DW; Trainor, G 8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists. J Med Chem 52:3073-83 (2009) [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:
BDBM29432
Synonyms:
Pyrazolo[1,5-a]-1,3,5-triazine, 12-1
Type:
Small organic molecule
Emp. Form.:
C20H27N5O3
Mol. Mass.:
385.4601
SMILES:
COCCN(CCOC)c1nc(C)nc2c(c(C)nn12)-c1ccc(OC)cc1
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