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ChEMBL ligand: CHEMBL2441340 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3] | ||||||||
ChEMBL | Inhibition of HRI (unknown origin) assessed as EIF2AK1 phosphorylation | B | 6.34 | pIC50 | 460 | nM | IC50 | ACS Med Chem Lett (2013) 4: 964-968 [PMID:24900593] |
eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5] | ||||||||
ChEMBL | Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | ACS Med Chem Lett (2013) 4: 964-968 [PMID:24900593] |
ChEMBL | Inhibition of GST-tagged PERK cytoplasmic domain (536 to 1116) (unknown origin) assessed as biotinylated His6-tagged EIF2alpha phosphorylation preincubated for 30 mins followed by ATP and eIF2alpha addition measured after 1 hr by HTRF assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | ACS Med Chem Lett (2013) 4: 964-968 [PMID:24900593] |
GtoPdb | Biochemical activity | - | 9.1 | pIC50 | 0.8 | nM | IC50 | ACS Med Chem Lett (2013) 4: 964-8 [PMID:24900593] |
eukaryotic translation initiation factor 2 alpha kinase 4/Eukaryotic translation initiation factor 2-alpha kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5358] [GtoPdb: 2018] [UniProtKB: Q9P2K8] | ||||||||
ChEMBL | Inhibition of GCN2 (unknown origin) assessed as EIF2AK4 phosphorylation | B | 5.47 | pIC50 | 3388 | nM | IC50 | ACS Med Chem Lett (2013) 4: 964-968 [PMID:24900593] |
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] | ||||||||
ChEMBL | Inhibition of PKR (unknown origin) assessed as EIF2AK2 phosphorylation | B | 6.04 | pIC50 | 905 | nM | IC50 | ACS Med Chem Lett (2013) 4: 964-968 [PMID:24900593] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]