显示 1 到 16 条，共 16 条数据 每页数据量:
Compound ID
Cluster
Compound Type
Target Name Img Activity Assay Description Source
Type
Relation
Value
Unit
NAs.000083 7 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.000083 Ki < 6309.57 nM PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKAA1 CHEMBL1201862
NAs.000389 7 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.000389 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.001065 7 all-match AMP-activated protein kinase, alpha-1 subunit NAs.001065 Ki = 15848.93 nM PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKAA1 CHEMBL1201862
NAs.002742 7 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.002742 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-1 subunit NAs.002742 Inhibition = 3.79 % GSK_PKIS: AMPKA1 (A1B1G1) mean inhibition at 1 uM [Nanosyn] CHEMBL1961873
NAs.002770 7 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.002770 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-1 subunit NAs.002770 Kd > 10000.0 nM Binding constant for AMPK-alpha1 kinase domain CHEMBL1150977
NAs.002770 7 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.002770 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.003215 2 all-match AMP-activated protein kinase, alpha-1 subunit NAs.003215 Ki < 1584.89 nM PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKAA1 CHEMBL1201862
NAs.003270 7 all-match AMP-activated protein kinase, alpha-1 subunit NAs.003270 Ki = 125.89 nM PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKAA1 CHEMBL1201862
NAs.003271 7 base-match AMP-activated protein kinase, alpha-1 subunit NAs.003271 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.003485 2 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.003485 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.004092 7 all-match AMP-activated protein kinase, alpha-1 subunit NAs.004092 Ki = 50118.72 nM PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PRKAA1 CHEMBL1201862
NAs.005346 7 base-match AMP-activated protein kinase, alpha-1 subunit NAs.005346 IC50 > 10000.0 nM Mobility Shift Assay: Agents: 1-fold kinase buffer without MnCl2: 50 mM HEPES, pH 7.5, 0.0015% Brij-35, 10 mM MgCl2, 2 mM DTT. 1-fold kinase buffer with MnCl2: 50 mM HEPES, pH 7.5, 0.0015% Brij-35, 10 mM MgCl2, 10 mM MnCl2, 2 mM DTT. Termination solution: 100 mM HEPES, pH 7.5, 0.0015% Brij-35, 0.2% Coating Reagent#3, 50 mM EDTA. 2.5-fold kinase solution: The kinase was added to the 1-fold kinase buffer to form a 2.5-fold kinase solution. 2.5-fold substrate solution: FAM fluorescence-labelled polypeptide and ATP were added to the 1-fold kinase buffer to form a 2.5-fold substrate solution. Compounds: The final test concentration of the compound was 10 μM at maximum. Firstly, a 50-fold concentration (i.e. 500 μM) was prepared with 100% DMSO. The compound was diluted with 100% DMSO by 5 folds at 5 concentrations (successively 500 μM, 100 μM, 20 μM, 4 μM, and 0.8 μM). After diluting with 1-fold kinase buffer by 10 folds, 5 μl of the samples were transferred to a 384-well reaction plate. Two negative control wells and two positive control wells were set at each line respectively. Replication was made in a 96-well plate in five concentrations of 5-fold compound. 10% DMSO was added to the positive control well, and 5 μl of EDTA (250 mM) was added to the negative control well. Procedure: To the 384-well reaction plate was added 5-fold compound dissolved in 10% DMSO at 5 μl/well. To the 384-well reaction plate was added 2.5-fold kinase solution at 10 μl/well. The plate was incubated at room temperature for 10 mins. To the 384-well reaction plate was added 2.5-fold substrate solution at 10 μl/well. The plate was incubated at 28° C. for a certain period. 25 μl termination solution was added to terminate the reaction. CHEMBL3886794
NAs.008133 7 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.008133 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.008387 7 ribose-match AMP-activated protein kinase, alpha-1 subunit NAs.008387 Activity = 119.5 % Inhibition of recombinant full-length human AMPKalpha1 assessed as residual activity at 10 uM using AMARAASAAALARRR as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method CHEMBL4311992