A-769662 [Ligand Id: 10069] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL512504 (A-769662) |
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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: 1544, 1545, 1542, 1541, 1547, 1546, 1543] [UniProtKB: O43741, P54619, P54646, Q13131, Q9UGI9, Q9UGJ0, Q9Y478] | ||||||||
| ChEMBL | Activation of AMPK (unknown origin) | B | 6.1 | pEC50 | 800 | nM | EC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| 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: 1545, 1541, 1543] [UniProtKB: P54619, Q13131, Q9Y478] | ||||||||
| 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] |
| ChEMBL | Activation of human AMPK alpha1/beta1/gamma1 expressed in baculovirus/Sf9 cells using SAMS peptide as substrate incubated for 15 mins by in presence of 33P-ATP by liquid scintillation counting method | B | 6.1 | pEC50 | 800 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 2443-2447 [PMID:31358465] |
| 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: 1544, 1545, 1541] [UniProtKB: O43741, P54619, Q13131] | ||||||||
| 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: 1545, 1542, 1543] [UniProtKB: P54619, P54646, Q9Y478] | ||||||||
| 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 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]
