Reaction Details |
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Target | Eukaryotic translation initiation factor 2-alpha kinase 1 |
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Ligand | BDBM50414875 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_589403 (CHEMBL1058424) |
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IC50 | 1258.93±n/a nM |
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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 Lett19:6548-51 (2009) [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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BDBM50414875 |
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n/a |
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Name | BDBM50414875 |
Synonyms: | CHEMBL575915 |
Type | Small organic molecule |
Emp. Form. | C19H17Cl2N3O2 |
Mol. Mass. | 390.263 |
SMILES | COc1cc2Cc3c(NCc4ccc(Cl)cc4Cl)[nH]nc3-c2cc1OC |
Structure |
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