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Target
Eukaryotic translation initiation factor 2-alpha kinase 1
Ligand
BDBM50414889
Substrate
n/a
Meas. Tech.
ChEMBL_589403 (CHEMBL1058424)
IC50
63.1±n/a nM
Citation
 Rosen, MD; Woods, CR; Goldberg, SD; Hack, MD; Bounds, AD; Yang, Y; Wagaman, PC; Phuong, VK; Ameriks, AP; Barrett, TD; Kanelakis, KC; Chuang, JC; Chang, J; Shankley, NP; Rabinowitz, MH Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase. Bioorg Med Chem Lett 19:6548-51 (2009) [PubMed]  Article 
Target
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:
MQGGNSGVRKREEEGDGAGAVAAPPAIDFPAEGPDPEYDESDVPAEIQVLKEPLQQPTFPFAVANQLLLVSLLEHLSHVHEPNPLRSRQVFKLLCQTFIKMGLLSSFTCSDEFSSLRLHHNRAITHLMRSAKERVRQDPCEDISRIQKIRSREVALEAQTSRYLNEFEELAILGKGGYGRVYKVRNKLDGQYYAIKKILIKGATKTVCMKVLREVKVLAGLQHPNIVGYHTAWIEHVHVIQPRADRAAIELPSLEVLSDQEEDREQCGVKNDESSSSSIIFAEPTPEKEKRFGESDTENQNNKSVKYTTNLVIRESGELESTLELQENGLAGLSASSIVEQQLPLRRNSHLEESFTSTEESSEENVNFLGQTEAQYHLMLHIQMQLCELSLWDWIVERNKRGREYVDESACPYVMANVATKIFQELVEGVFYIHNMGIVHRDLKPRNIFLHGPDQQVKIGDFGLACTDILQKNTDWTNRNGKRTPTHTSRVGTCLYASPEQLEGSEYDAKSDMYSLGVVLLELFQPFGTEMERAEVLTGLRTGQLPESLRKRCPVQAKYIQHLTRRNSSQRPSAIQLLQSELFQNSGNVNLTLQMKIIEQEKEIAELKKQLNLLSQDKGVRDDGKDGGVG
  
Inhibitor
Name:
BDBM50414889
Synonyms:
CHEMBL574443
Type:
Small organic molecule
Emp. Form.:
C20H21N3O2
Mol. Mass.:
335.3996
SMILES:
COc1cc2Cc3c(NCc4ccccc4C)[nH]nc3-c2cc1OC
Structure:
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