| Reaction Details |
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 | Report a problem with these data |
| Target | Eukaryotic translation initiation factor 2-alpha kinase 1 |
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| Ligand | BDBM50396528 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_862848 (CHEMBL2172950) |
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| IC50 | 12080±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 |
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| Synonyms: | E2AK1_HUMAN | EIF2AK1 | HRI | KIAA1369 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 71098.55 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_1467744 |
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| Residue: | 630 |
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| Sequence: | MQGGNSGVRKREEEGDGAGAVAAPPAIDFPAEGPDPEYDESDVPAEIQVLKEPLQQPTFP
FAVANQLLLVSLLEHLSHVHEPNPLRSRQVFKLLCQTFIKMGLLSSFTCSDEFSSLRLHH
NRAITHLMRSAKERVRQDPCEDISRIQKIRSREVALEAQTSRYLNEFEELAILGKGGYGR
VYKVRNKLDGQYYAIKKILIKGATKTVCMKVLREVKVLAGLQHPNIVGYHTAWIEHVHVI
QPRADRAAIELPSLEVLSDQEEDREQCGVKNDESSSSSIIFAEPTPEKEKRFGESDTENQ
NNKSVKYTTNLVIRESGELESTLELQENGLAGLSASSIVEQQLPLRRNSHLEESFTSTEE
SSEENVNFLGQTEAQYHLMLHIQMQLCELSLWDWIVERNKRGREYVDESACPYVMANVAT
KIFQELVEGVFYIHNMGIVHRDLKPRNIFLHGPDQQVKIGDFGLACTDILQKNTDWTNRN
GKRTPTHTSRVGTCLYASPEQLEGSEYDAKSDMYSLGVVLLELFQPFGTEMERAEVLTGL
RTGQLPESLRKRCPVQAKYIQHLTRRNSSQRPSAIQLLQSELFQNSGNVNLTLQMKIIEQ
EKEIAELKKQLNLLSQDKGVRDDGKDGGVG
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| BDBM50396528 |
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| n/a |
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| Name | BDBM50396528 |
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| Synonyms: | CHEMBL2171128 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H22N4OS |
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| Mol. Mass. | 462.565 |
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| SMILES | Nc1ncc(-c2cccnc2)c2scc(-c3ccc4N(CCc4c3)C(=O)Cc3ccccc3)c12 |
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| Structure | 
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