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TargetEukaryotic translation initiation factor 2-alpha kinase 1
LigandBDBM50414894
Substrate/Competitorn/a
Meas. Tech.ChEMBL_589403 (CHEMBL1058424)
IC50 6.31±n/a nM
Citation Rosen, MDWoods, CRGoldberg, SDHack, MDBounds, ADYang, YWagaman, PCPhuong, VKAmeriks, APBarrett, TDKanelakis, KCChuang, JCChang, JShankley, NPRabinowitz, MH Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase. Bioorg Med Chem Lett19:6548-51 (2009) [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:
BDBM50414894
n/a
NameBDBM50414894
Synonyms:CHEMBL573760
TypeSmall organic molecule
Emp. Form.C19H15Cl2N3O3
Mol. Mass.404.247
SMILESCOc1cc2C(=O)c3c(NCc4c(Cl)cccc4Cl)[nH]nc3-c2cc1OC
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: