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TargetCorticotropin-releasing factor receptor 1
LigandBDBM50203620
Substrate/Competitorn/a
Meas. Tech.ChEMBL_454261 (CHEMBL903444)
Ki 1400±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
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  Blast E-value cutoff:
BDBM50203620
n/a
NameBDBM50203620
Synonyms:8-(2-chloro-4,6-dimethyl-phenyl)-2-methyl-3-morpholin-4-ylmethyl-8H-1,3a,7,8-tetraaza-cyclopenta[a]indene | CHEMBL440232
TypeSmall organic molecule
Emp. Form.C22H24ClN5O
Mol. Mass.409.912
SMILESCc1nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n2c1CN1CCOCC1 |(-8.79,-40.1,;-7.37,-39.52,;-6.06,-40.33,;-4.88,-39.35,;-3.34,-39.24,;-2.35,-40.42,;-.84,-40.15,;-.32,-38.7,;.15,-41.32,;-.38,-42.78,;.61,-43.96,;-1.9,-43.04,;-2.89,-41.86,;-4.4,-42.13,;-2.97,-37.75,;-1.6,-37.03,;-1.54,-35.48,;-2.92,-34.59,;-4.22,-35.38,;-4.28,-36.92,;-5.46,-37.91,;-7,-38.03,;-7.99,-36.85,;-7.46,-35.4,;-5.95,-35.14,;-5.43,-33.7,;-6.41,-32.52,;-7.93,-32.78,;-8.46,-34.23,)|
Structure
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