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TargetCorticotropin-releasing factor receptor 1
LigandBDBM50203616
Substrate/Competitorn/a
Meas. Tech.ChEMBL_454261 (CHEMBL903444)
Ki 700±n/a nM
Citation Han, XCiviello, RPin, SSBurris, KBalanda, LAKnipe, JRen, SFiedler, TBrowman, KEMacci, RTaber, MTZhang, JDubowchik, GM An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes. Bioorg Med Chem Lett17:2026-30 (2007) [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 | CRF-R2 Alpha | CRF1 | CRFR | CRFR1 | CRFR1_HUMAN | CRH-R 1 | CRHR | CRHR1 | Corticotropin releasing factor receptor 1 | Corticotropin-releasing factor receptor 1 (CRF-1) | Corticotropin-releasing factor receptor 1 (CRF1) | Corticotropin-releasing hormone receptor 1
Type:Enzyme
Mol. Mass.:50744.31
Organism:Homo sapiens (Human)
Description:P34998
Residue:444
Sequence:
MGGHPQLRLVKALLLLGLNPVSASLQDQHCESLSLASNISGLQCNASVDLIGTCWPRSPA
GQLVVRPCPAFFYGVRYNTTNNGYRECLANGSWAARVNYSECQEILNEEKKSKVHYHVAV
IINYLGHCISLVALLVAFVLFLRLRPGCTHWGDQADGALEVGAPWSGAPFQVRRSIRCLR
NIIHWNLISAFILRNATWFVVQLTMSPEVHQSNVGWCRLVTAAYNYFHVTNFFWMFGEGC
YLHTAIVLTYSTDRLRKWMFICIGWGVPFPIIVAWAIGKLYYDNEKCWFGKRPGVYTDYI
YQGPMILVLLINFIFLFNIVRILMTKLRASTTSETIQYRKAVKATLVLLPLLGITYMLFF
VNPGEDEVSRVVFIYFNSFLESFQGFFVSVFYCFLNSEVRSAIRKRWHRWQDKHSIRARV
ARAMSIPTSPTRVSFHSIKQSTAV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50203616
n/a
NameBDBM50203616
Synonyms:8-(2-chloro-4,6-dimethyl-phenyl)-2-methyl-3-(3-phenethyl-pyrrolidin-1-ylmethyl)-8H-1,3a,7,8-tetraaza-cyclopenta[a]indene | CHEMBL248163
TypeSmall organic molecule
Emp. Form.C30H32ClN5
Mol. Mass.498.062
SMILESCc1nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n2c1CN1CCC(CCc2ccccc2)C1 |w:26.30,(7.31,-23,;8.74,-22.42,;10.04,-23.23,;11.22,-22.24,;12.76,-22.13,;13.75,-23.32,;15.26,-23.05,;15.78,-21.6,;16.25,-24.22,;15.72,-25.68,;16.71,-26.85,;14.2,-25.94,;13.22,-24.76,;11.7,-25.02,;13.14,-20.65,;14.5,-19.92,;14.56,-18.38,;13.19,-17.49,;11.88,-18.28,;11.82,-19.82,;10.64,-20.81,;9.11,-20.92,;8.11,-19.75,;8.64,-18.3,;10.11,-17.88,;10.16,-16.34,;8.72,-15.81,;8.29,-14.33,;6.79,-13.96,;6.36,-12.49,;7.43,-11.38,;7.01,-9.9,;5.51,-9.53,;4.44,-10.65,;4.87,-12.12,;7.77,-17.03,)|
Structure
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