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TargetEukaryotic translation initiation factor 2-alpha kinase 1
LigandBDBM50442166
Substrate/Competitorn/a
Meas. Tech.ChEMBL_993291 (CHEMBL2443948)
IC50 460±n/a nM
Citation Axten, JMRomeril, SPShu, ARalph, JMedina, JRFeng, YLi, WHGrant, SWHeerding, DAMinthorn, EMencken, TGaul, NGoetz, AStanley, THassell, AMGampe, RTAtkins, CKumar, R Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development. ACS Med Chem Lett4:964-8 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Eukaryotic translation initiation factor 2-alpha kinase 1
Name:Eukaryotic translation initiation factor 2-alpha kinase 1
Synonyms:E2AK1_HUMAN | EIF2AK1 | HRI | KIAA1369
Type:PROTEIN
Mol. Mass.:71098.55
Organism:Homo sapiens (Human)
Description:ChEMBL_1467744
Residue:630
Sequence:
MQGGNSGVRKREEEGDGAGAVAAPPAIDFPAEGPDPEYDESDVPAEIQVLKEPLQQPTFP
FAVANQLLLVSLLEHLSHVHEPNPLRSRQVFKLLCQTFIKMGLLSSFTCSDEFSSLRLHH
NRAITHLMRSAKERVRQDPCEDISRIQKIRSREVALEAQTSRYLNEFEELAILGKGGYGR
VYKVRNKLDGQYYAIKKILIKGATKTVCMKVLREVKVLAGLQHPNIVGYHTAWIEHVHVI
QPRADRAAIELPSLEVLSDQEEDREQCGVKNDESSSSSIIFAEPTPEKEKRFGESDTENQ
NNKSVKYTTNLVIRESGELESTLELQENGLAGLSASSIVEQQLPLRRNSHLEESFTSTEE
SSEENVNFLGQTEAQYHLMLHIQMQLCELSLWDWIVERNKRGREYVDESACPYVMANVAT
KIFQELVEGVFYIHNMGIVHRDLKPRNIFLHGPDQQVKIGDFGLACTDILQKNTDWTNRN
GKRTPTHTSRVGTCLYASPEQLEGSEYDAKSDMYSLGVVLLELFQPFGTEMERAEVLTGL
RTGQLPESLRKRCPVQAKYIQHLTRRNSSQRPSAIQLLQSELFQNSGNVNLTLQMKIIEQ
EKEIAELKKQLNLLSQDKGVRDDGKDGGVG
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50442166
n/a
NameBDBM50442166
Synonyms:CHEMBL2441340
TypeSmall organic molecule
Emp. Form.C23H21FN6O
Mol. Mass.416.4508
SMILESCc1cccc(CC(=O)N2CCc3c2ccc(-c2cn(C)c4ncnc(N)c24)c3F)n1
Structure
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