A-769662 [Ligand Id: 10069] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL512504 (A-769662)
  • protein kinase AMP-activated catalytic subunit alpha 1/AMP-activated protein kinase, alpha-1 subunit in Rat [ChEMBL: CHEMBL4533] [GtoPdb: 1541] [UniProtKB: P54645]
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  • protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit gamma 3/protein kinase AMP-activated non-catalytic subunit gamma 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase, AMPK in Human [ChEMBL: CHEMBL2096907] [GtoPdb: 1544154515421541154715461543] [UniProtKB: O43741P54619P54646Q13131Q9UGI9Q9UGJ0Q9Y478]
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  • protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 in Human [ChEMBL: CHEMBL2111345] [GtoPdb: 154515411543] [UniProtKB: P54619Q13131Q9Y478]
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  • protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/AMPK alpha1/beta2/gamma1 in Human [ChEMBL: CHEMBL3038453] [GtoPdb: 154415451541] [UniProtKB: O43741P54619Q13131]
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  • protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMPK alpha2/beta1/gamma1 in Human [ChEMBL: CHEMBL3038455] [GtoPdb: 154515421543] [UniProtKB: P54619P54646Q9Y478]
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  • AMP kinase in Human [GtoPdb: 1540]
  • AMP kinase in Rat [GtoPdb: 1540]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase AMP-activated catalytic subunit alpha 1/AMP-activated protein kinase, alpha-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4533] [GtoPdb: 1541] [UniProtKB: P54645]
ChEMBL Activation of rat AMPK-alpha-1-alpha-2beta-1-gamma-1 kinase B 6.94 pEC50 116 nM EC50 J. Biol. Chem. (2007) 282: 32549-32560 [PMID:17855357]
protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit gamma 3/protein kinase AMP-activated non-catalytic subunit gamma 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase, AMPK in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096907] [GtoPdb: 1544154515421541154715461543] [UniProtKB: O43741P54619P54646Q13131Q9UGI9Q9UGJ0Q9Y478]
ChEMBL Activation of AMPK (unknown origin) by luminescence assay B 6.24 pEC50 576 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 5237-5242 [PMID:26471090]
protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111345] [GtoPdb: 154515411543] [UniProtKB: P54619Q13131Q9Y478]
ChEMBL Binding affinity to human recombinant N-terminal AVI-tagged phosphorylated AMPK alpha1beta1gamma1 expressed in Escherichia coli BL21 cells after 1 to 10 mins by biolayer interferometry B 6.29 pKd 510 nM Kd J. Med. Chem. (2016) 59: 2879-2893 [PMID:26510622]
ChEMBL Binding affinity for full length human N-terminal His/BAP-tagged AMPK alpha1/beta1/gamma1 expressed in Escherichia coli BL21-CodonPlus by surface plasmon resonance method B 6.31 pKd 487 nM Kd Bioorg Med Chem Lett (2016) 26: 5139-5148 [PMID:27727125]
protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/AMPK alpha1/beta2/gamma1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038453] [GtoPdb: 154415451541] [UniProtKB: O43741P54619Q13131]
ChEMBL Binding affinity to human recombinant N-terminal AVI-tagged phosphorylated AMPK alpha1beta2gamma1 expressed in Escherichia coli BL21 cells after 1 to 10 mins by biolayer interferometry B 4.84 pKd 14500 nM Kd J. Med. Chem. (2016) 59: 2879-2893 [PMID:26510622]
protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMPK alpha2/beta1/gamma1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038455] [GtoPdb: 154515421543] [UniProtKB: P54619P54646Q9Y478]
ChEMBL Activation of human AMPK alpha2/beta1/gamma1 expressed in Escherichia coli BL21 B 6.41 pEC50 390 nM EC50 J Med Chem (2018) 61: 6421-6467 [PMID:29620890]
AMP kinase in Human [GtoPdb: 1540]
GtoPdb Activation of AMPK partially purified from HEK cells. - 5.96 pEC50 1100 nM EC50 Cell Metab. (2006) 3: 403-16 [PMID:16753576]
AMP kinase in Rat [GtoPdb: 1540]
GtoPdb Activation of baculovirus expressed α1,β1,&gamma1 recombinant isoform of AMPK. - 6.15 pEC50 700 nM EC50 Cell Metab. (2006) 3: 403-16 [PMID:16753576]
GtoPdb Activation of AMPK purified from rat liver, which contains α1 and α2 catalytic subunits, with β1 and γ1 regulatory subunits. - 6.94 pEC50 116 nM EC50 J. Biol. Chem. (2007) 282: 32549-60 [PMID:17855357]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]