Reaction Details Report a problem with these data
Target
Eukaryotic translation initiation factor 2-alpha kinase 1
Ligand
BDBM50396531
Substrate
n/a
Meas. Tech.
ChEMBL_862848 (CHEMBL2172950)
IC50
1863±n/a nM
Citation
Axten, JM; Medina, JR; Feng, Y; Shu, A; Romeril, SP; Grant, SW; Li, WH; Heerding, DA; Minthorn, E; Mencken, T; Atkins, C; Liu, Q; Rabindran, S; Kumar, R; Hong, X; Goetz, A; Stanley, T; Taylor, JD; Sigethy, SD; Tomberlin, GH; Hassell, AM; Kahler, KM; Shewchuk, LM; Gampe, 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 Chem 55:7193-207 (2012) [PubMed] Article
More Info.:
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