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 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]
