| 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 | BDBM50072073 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1467744 (CHEMBL3412170) |
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| IC50 | >10000±n/a nM |
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| Citation |  Smith, AL; Andrews, KL; Beckmann, H; Bellon, SF; Beltran, PJ; Booker, S; Chen, H; Chung, YA; D'Angelo, ND; Dao, J; Dellamaggiore, KR; Jaeckel, P; Kendall, R; Labitzke, K; Long, AM; Materna-Reichelt, S; Mitchell, P; Norman, MH; Powers, D; Rose, M; Shaffer, PL; Wu, MM; Lipford, JR Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J Med Chem58:1426-41 (2015) [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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| BDBM50072073 |
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| n/a |
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| Name | BDBM50072073 |
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| Synonyms: | CHEMBL3407848 |
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| Type | Small organic molecule |
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| Emp. Form. | C33H27N5O5 |
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| Mol. Mass. | 573.598 |
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| SMILES | COc1cc2nccc(Oc3ccc(NC(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)nc3)c2cc1OC |
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| Structure | 
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