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TargetEukaryotic translation initiation factor 2-alpha kinase 1
LigandBDBM50396534
Substrate/Competitorn/a
Meas. Tech.ChEMBL_862848 (CHEMBL2172950)
IC50 420±n/a nM
Citation Axten, JMMedina, JRFeng, YShu, ARomeril, SPGrant, SWLi, WHHeerding, DAMinthorn, EMencken, TAtkins, CLiu, QRabindran, SKumar, RHong, XGoetz, AStanley, TTaylor, JDSigethy, SDTomberlin, GHHassell, AMKahler, KMShewchuk, LMGampe, RT Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem55:7193-207 (2012) [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:
BDBM50396534
n/a
NameBDBM50396534
Synonyms:CHEMBL2171124
TypeSmall organic molecule
Emp. Form.C24H20F3N5O
Mol. Mass.451.4437
SMILESCn1cc(-c2ccc3N(CCc3c2)C(=O)Cc2cccc(c2)C(F)(F)F)c2c(N)ncnc12
Structure
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