Target
Corticotropin-releasing factor receptor 1
Ligand
BDBM29460
Substrate
125I-Tyr(0)-ovine-CRF
Meas. Tech.
In Vitro Binding Autoradiography
pH
7.2±n/a
Temperature
296.15±n/a K
IC50
2.48±0.34 nM
Citation
 Gilligan, PJHe, LClarke, TTivitmahaisoon, PLelas, SLi, YWHeman, KFitzgerald, LMiller, KZhang, GMarshall, AKrause, CMcElroy, JWard, KShen, HWong, HGrossman, SNemeth, GZaczek, RArneric, SPHartig, PRobertson, DWTrainor, 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:
BDBM29460
Synonyms:
Pyrazolo[1,5-a]-1,3,5-triazine, 12-29
Type:
Small organic molecule
Emp. Form.:
C21H26N6O2
Mol. Mass.:
394.4701
SMILES:
CCN(CCC#N)c1nc(C)nc2c(c(C)nn12)-c1c(C)cc(OC)cc1OC |(-2.1,10.44,;-2.59,8.98,;-1.57,7.83,;-.06,8.13,;.43,9.59,;1.94,9.89,;3.43,10.29,;-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,;1.01,.52,;2.34,1.29,;1.01,-1.02,;-.33,-1.79,;-.33,-3.33,;1.01,-4.1,;-1.66,-1.02,;-1.66,.52,;-2.99,1.29,;-4.33,.52,)|
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