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TargetCorticotropin-releasing factor receptor 1
LigandBDBM50351387
Substrate/Competitorn/a
Meas. Tech.ChEMBL_764453 (CHEMBL1821005)
IC50 7±n/a nM
Citation Saito, TObitsu, TKondo, TMatsui, TNagao, YKusumi, KMatsumura, NUeno, SKishi, AKatsumata, SKagamiishi, YNakai, HToda, M 6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists. Bioorg Med Chem19:5432-45 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Corticotropin-releasing factor receptor 1
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:
MGRRPQLRLVKALLLLGLNPVSTSLQDQRCENLSLTSNVSGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRSIRCLRNIIHWNLISAFILRNATWFVVQLTVSPEV
HQSNVAWCRLVTAAYNYFHVTNFFWMFGEGCYLHTAIVLTYSTDRLRKWMFVCIGWGVPF
PIIVAWAIGKLHYDNEKCWFGKRPGVYTDYIYQGPMILVLLINFIFLFNIVRILMTKLRA
STTSETIQYRKAVKATLVLLPLLGITYMLFFVNPGEDEVSRVVFIYFNSFLESFQGFFVS
VFYCFLNSEVRSAIRKRWRRWQDKHSIRARVARAMSIPTSPTRVSFHSIKQSTAV
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  Blast E-value cutoff:
BDBM50351387
n/a
NameBDBM50351387
Synonyms:CHEMBL1819077
TypeSmall organic molecule
Emp. Form.C22H27ClN4O
Mol. Mass.398.929
SMILESCCC(CC)Nc1c2CCCc2nc2c(c(C)nn12)-c1ccc(OC)cc1Cl |(23.48,-13.44,;22.13,-14.18,;22.1,-15.72,;23.42,-16.52,;24.77,-15.77,;20.75,-16.47,;20.72,-18.01,;19.37,-18.75,;17.91,-18.25,;16.98,-19.48,;17.87,-20.74,;19.34,-20.29,;20.67,-21.09,;22.02,-20.33,;23.48,-20.82,;24.4,-19.59,;25.94,-19.61,;23.51,-18.34,;22.04,-18.8,;23.94,-22.29,;22.89,-23.42,;23.35,-24.89,;24.85,-25.23,;25.31,-26.7,;24.27,-27.83,;25.9,-24.09,;25.44,-22.62,;26.47,-21.49,)|
Structure
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