| Compound ID |
Cluster
|
Compound Type
|
Target Name | Img | Activity | Assay Description | Source | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|
|
Type
|
Relation
|
Value
|
Unit
|
||||||||
| NAs.000023 | 7 | all-match | AMP-activated protein kinase, alpha-2 subunit |  |
Thermal melting change | = | 1.4 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| NAs.000083 | 7 | ribose-match | AMP-activated protein kinase, alpha-1 subunit |  |
Ki | < | 6309.57 | nM | PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKAA1 | CHEMBL1201862 | |
| 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.000283 | 7 | ribose-match | AMP-activated protein kinase, AMPK | |
Residual Activity | = | 86.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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 | |
Residual Activity | = | 88.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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.000283 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit | |
Thermal melting change | = | 0.6 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| 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.000318 | 7 | ribose-match | AMP-activated protein kinase, AMPK | |
Residual Activity | = | 64.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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 | |
Residual Activity | = | 22.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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.000389 | 7 | ribose-match | AMP-activated protein kinase, alpha-1 subunit |  |
Kd | > | 30000.0 | nM | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | CHEMBL3991601 | |
| NAs.000389 | 7 | ribose-match | AMP-activated protein kinase, gamma-1 subunit | |
Kd | > | 30000.0 | nM | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | CHEMBL3991601 | |
| NAs.000389 | 7 | ribose-match | AMP-activated protein kinase, gamma-2 subunit | |
Kd | > | 30000.0 | nM | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | CHEMBL3991601 | |
| NAs.000539 | 7 | ribose-match | AMP-activated protein kinase, AMPK |  |
Residual Activity | = | 48.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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 | |
Residual Activity | = | 95.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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 | = | 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.000995 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit |  |
Thermal melting change | = | 0.2 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| 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.001019 | 7 | ribose-match | AMP-activated protein kinase, AMPK | |
Residual Activity | = | 87.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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 | |
Residual Activity | = | 50.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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, alpha-2 subunit | |
Thermal melting change | = | 0.3 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| NAs.001065 | 7 | all-match | AMP-activated protein kinase, alpha-1 subunit |  |
Ki | = | 15848.93 | nM | PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKAA1 | CHEMBL1201862 | |
| NAs.001156 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit |  |
Thermal melting change | = | 0.2 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| NAs.001163 | 7 | base-match | AMP-activated protein kinase, alpha-2 subunit |  |
Thermal melting change | = | -0.6 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| NAs.001167 | 7 | base-match | AMP-activated protein kinase, AMPK |  |
Inhibition | = | -12.0 | % | Inhibition of AMPK (unknown origin) at 1 uM by [33P]-ATP filter-binding assay | CHEMBL2424535 | |
| NAs.001310 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit |  |
Thermal melting change | = | -0.7 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| NAs.001310 | 7 | ribose-match | AMP-activated protein kinase, AMPK | |
Residual Activity | = | 90.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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.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 | |
Residual Activity | = | 99.0 | % | Millipore: Percentage of residual kinase activity of PRKAA2 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.001420 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit |  |
Thermal melting change | = | 0.2 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| NAs.001541 | 7 | all-match | AMP-activated protein kinase, alpha-2 subunit |  |
Activity | = | 22.0 | % | Inhibition of recombinant AMPK (unknown origin) assessed as residual activity using [gamma-33P]ATP as substrate at 1 uM | CHEMBL2331324 | |
| NAs.001855 | 7 | all-match | AMP-activated protein kinase, AMPK |  |
Percent Effect | = | 5.252999999999999 | % | AMP-dependent Kinase enzyme assay. An in vitro enzyme assay that detects ADP turnover that is directly proportional to AMPK activity. This uses naive AMPK that is activated during the assay with MK-8722 | CHEMBL3988442 | |
| NAs.002476 | 7 | base-match | AMP-activated protein kinase, AMPK |  |
Inhibition | = | 78.0 | % | Inhibition of AMPK (unknown origin) at 30 uM by microfluidic mobility shift assay relative to control | CHEMBL2417369 | |
| NAs.002742 | 7 | ribose-match | AMP-activated protein kinase, alpha-1 subunit |  |
Inhibition | = | 1.05 | % | GSK_PKIS: AMPKA1 (A1B1G1) mean inhibition at 0.1 uM [Nanosyn] | CHEMBL1961873 | |
| NAs.002742 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit | |
Inhibition | = | -1.1 | % | GSK_PKIS: AMPKA2 (A2B1G1) mean inhibition at 0.1 uM [Nanosyn] | CHEMBL1961873 | |
| NAs.002742 | 7 | ribose-match | AMP-activated protein kinase, alpha-1 subunit | |
Inhibition | = | 3.79 | % | GSK_PKIS: AMPKA1 (A1B1G1) mean inhibition at 1 uM [Nanosyn] | CHEMBL1961873 | |
| NAs.002742 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit | |
Inhibition | = | 1.47 | % | GSK_PKIS: AMPKA2 (A2B1G1) mean inhibition at 1 uM [Nanosyn] | CHEMBL1961873 | |
| NAs.002770 | 7 | ribose-match | AMP-activated protein kinase, gamma-2 subunit |  |
Kd | > | 30000.0 | nM | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | CHEMBL3991601 | |
| NAs.002770 | 7 | ribose-match | AMP-activated protein kinase, gamma-1 subunit | |
Kd | > | 30000.0 | nM | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | CHEMBL3991601 | |
| NAs.002770 | 7 | ribose-match | AMP-activated protein kinase, alpha-1 subunit | |
Kd | > | 30000.0 | nM | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | CHEMBL3991601 | |
| NAs.002770 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit | |
Thermal melting change | = | 0.4 | degrees C | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | CHEMBL1145498 | |
| NAs.002770 | 7 | ribose-match | AMP-activated protein kinase, alpha-1 subunit | |
Kd | > | 10000.0 | nM | Binding constant for AMPK-alpha1 kinase domain | CHEMBL1150977 | |
| NAs.002770 | 7 | ribose-match | AMP-activated protein kinase, alpha-1 subunit | |
Kd | None | None | None | Average Binding Constant for PRKAA1; NA=Not Active at 10 uM | CHEMBL1144455 | |
| NAs.002770 | 7 | ribose-match | AMP-activated protein kinase, alpha-2 subunit | |
Kd | > | 10000.0 | nM | Binding constant for AMPK-alpha2 kinase domain | CHEMBL1150977 | |
| NAs.002871 | 2 | all-match | AMP-activated protein kinase, AMPK |  |
EC50 | = | 5900.0 | nM | Activation of human AMPK after 15 mins | CHEMBL1687696 | |
| 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 | |