| Compound ID |
Cluster
|
Compound Type
|
Target Name | Img | Activity | Assay Description | Source | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|
|
Type
|
Relation
|
Value
|
Unit
|
||||||||
| NAs.000283 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
Residual Activity | = | 97.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.000283 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Residual Activity | = | 80.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.000318 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
Residual Activity | = | 77.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.000318 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Residual Activity | = | 22.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.000539 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
Residual Activity | = | 92.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.000539 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Residual Activity | = | 42.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.001019 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
Residual Activity | = | 92.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.001019 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Residual Activity | = | 45.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.001310 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
Residual Activity | = | 87.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.001310 | 7 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Residual Activity | = | 88.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.002871 | 2 | all-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
EC50 | = | 1519.0 | nM | Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphorylation preincubated for 15 mins followed by incubation with PP2a for 60 mins measured 60 mins post okadaic acid/Cy5-labelled SAMS and ATP addition by TR-FRET assay | CHEMBL3853317 | |
| NAs.002871 | 2 | all-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Activity | = | 103.0 | % | Activation of recombinant human AMPK alpha1/beta1/gamma1 using Cy5-labelled SAMS as substrate assessed as protection from Thr172 residue dephosphorylation preincubated for 15 mins followed by incubation with PP2a for 60 mins measured 60 mins post okadaic acid/Cy5-labelled SAMS and ATP addition by TR-FRET assay relative to AMP | CHEMBL3853317 | |
| NAs.002871 | 2 | all-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Kd | = | 3700.0 | nM | Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assay | CHEMBL3853317 | |
| NAs.002871 | 2 | all-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Activity | None | None | None | Activation of human recombinant AMPKalpha1beta1gamma1 expressed in Escherichia coli at 10 uM incubated for 1 hr using serine/threonine kinase substrate | CHEMBL4130473 | |
| NAs.003723 | 2 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
Residual Activity | = | 96.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.003723 | 2 | ribose-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 | |
Residual Activity | = | 75.0 | % | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | CHEMBL2218924 | |
| NAs.006075 | 7 | base-match | AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 |  |
EC50 | = | 630.96 | nM | Activation of full length human His/GST-tagged AMPK alpha1/beta1/gamma1 expressed in baculovirus expression system after 1 hr by Z'Lyte assay | CHEMBL3856285 | |