GSK2656157 [Ligand Id: 9544] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] | ||||||||
| ChEMBL | Inhibition of GST tagged human recombinant RIPK1 incubated for 4 hrs by ADP-Glo luminescence assay | B | 7.16 | pIC50 | 69.1 | nM | IC50 | J Med Chem (2022) 65: 14971-14999 [PMID:36346971] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
