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Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM29502
Substrate
125I-Tyr(0)-ovine-CRF
Meas. Tech.
In Vitro Binding Autoradiography
pH
7.2±n/a
Temperature
296.15±n/a K
IC50
17.6±4.3 nM
Citation
 Gilligan, PJ; Clarke, T; He, L; Lelas, S; Li, YW; Heman, K; Fitzgerald, L; Miller, K; Zhang, G; Marshall, A; Krause, C; McElroy, JF; Ward, K; Zeller, K; Wong, H; Bai, S; Saye, J; Grossman, S; Zaczek, R; Arneric, SP; Hartig, P; Robertson, D; Trainor, G Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. J Med Chem 52:3084-92 (2009) [PubMed]  Article  BDB Entry
Target
Name:
Corticotropin-releasing factor receptor 1
Synonyms:
CRF-R | CRF1 | CRH-R 1 | CRHR1 | Corticotropin releasing factor receptor | Corticotropin releasing factor receptor 1 | Corticotropin-releasing Factor Receptor 1 | Corticotropin-releasing hormone receptor 1
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:
BDBM29502
Synonyms:
Pyrazolo[1,5-a]-1,3,5-triazine, 13-27
Type:
Small organic molecule
Emp. Form.:
C18H24N6O
Mol. Mass.:
340.4228
SMILES:
CCCN(C)c1nc(C)nc2c(c(C)nn12)-c1ccc(OC)nc1C |(1.82,10.01,;.34,9.62,;-.06,8.13,;-1.57,7.83,;-2.59,8.98,;-2.07,6.37,;-3.58,6.06,;-4.07,4.61,;-5.58,4.3,;-3.05,3.45,;-1.54,3.75,;-.31,2.83,;.95,3.72,;2.41,3.23,;.49,5.19,;-1.05,5.21,;-.33,1.29,;-1.66,.52,;-1.66,-1.02,;-.33,-1.79,;-.33,-3.33,;1.01,-4.1,;1.01,-1.02,;1.01,.52,;2.34,1.29,)|
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