Reaction Details Report a problem with these data
Target
Eukaryotic translation initiation factor 2-alpha kinase 1
Ligand
BDBM50414878
Substrate
n/a
Meas. Tech.
ChEMBL_589403 (CHEMBL1058424)
IC50
794.33±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:
BDBM50414878
Synonyms:
CHEMBL575914
Type:
Small organic molecule
Emp. Form.:
C19H18ClN3O
Mol. Mass.:
339.819
SMILES:
COc1cccc-2c1Cc1c(NCc3c(C)cccc3Cl)[nH]nc-21
Structure:
Search PDB for entries with ligand similarity: