Reaction Details |
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Target | Eukaryotic translation initiation factor 2-alpha kinase 1 |
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Ligand | BDBM50396536 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_862848 (CHEMBL2172950) |
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IC50 | 214±n/a nM |
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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 Chem55:7193-207 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Eukaryotic translation initiation factor 2-alpha kinase 1 |
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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
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BDBM50396536 |
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n/a |
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Name | BDBM50396536 |
Synonyms: | CHEMBL2171122 |
Type | Small organic molecule |
Emp. Form. | C23H20ClN5O |
Mol. Mass. | 417.891 |
SMILES | Cn1cc(-c2ccc3N(CCc3c2)C(=O)Cc2cccc(Cl)c2)c2c(N)ncnc12 |
Structure |
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