STO609 [Ligand Id: 5274] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1182777
  • calcium/calmodulin dependent protein kinase kinase 1/CaM-kinase kinase alpha in Human [ChEMBL: CHEMBL5256] [GtoPdb: 1956] [UniProtKB: Q8N5S9]
Created with Highcharts 10.3.3ValuesChart context menuCaM-kinase kinase alphapKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
Created with Highcharts 10.3.3ValuesChart context menuCaM-kinase kinase betapKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
Created with Highcharts 10.3.3ValuesChart context menuInterferon-induced, double-stranded RNA-activated protein kinasepKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
calcium/calmodulin dependent protein kinase kinase 1/CaM-kinase kinase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5256] [GtoPdb: 1956] [UniProtKB: Q8N5S9]
GtoPdb - - 6.85 pIC50 140 nM IC50 J Biol Chem (2002) 277: 15813-8 [PMID:11867640]
ChEMBL Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET B 6.92 pIC50 120 nM IC50 J Med Chem (2023) 66: 15750-15760 [PMID:38009718]
calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
ChEMBL Inhibition of CaMKK2 (161 to 449 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) star cells incubated for 20 mins in presence of kinase tracer 236 by TR-FRET B 6.92 pIC50 120 nM IC50 J Med Chem (2023) 66: 15750-15760 [PMID:38009718]
GtoPdb - - 7.4 pIC50 40 nM IC50 J Biol Chem (2002) 277: 15813-8 [PMID:11867640]
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 human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 7 pIC50 <100 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]

ChEMBL data shown on this page come from version 35:

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]