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Inhibition of GRK2 (unknown origin) in presence of ATP at 5 uM
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to full length human GRK2 by Thermofluor thermal shift assay
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
Inhibition of bovine GRK2 S670A mutant after 5 mins in presence of ATP by phosphorimaging assay
Assay data:31 Active, 13 Activity ≤ 1 µM, 34 Tested
Inhibition of GRK2 (unknown origin)
Assay data:5 Active, 4 Activity ≤ 1 µM, 5 Tested
Inhibition of human PKCalpha active using MBP as substrate after 60 mins in presence of [gamma-32]ATP by scintillation counting
Assay data:24 Active, 2 Activity ≤ 1 µM, 92 Tested
Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubated for 60 mins followed by substrate addition measured after 10 mins by Lance TR-FRET assay
Assay data:84 Active, 73 Activity ≤ 1 µM, 92 Tested
Inhibition of recombinant human N-terminal GST-tagged ROCK2 catalytic domain (1 to 553 residues) expressed in baculovirus expression system using STK 2-biotin as substrate measured after 60 mins by HTRF/TR-FRET assay
Assay data:83 Active, 59 Activity ≤ 1 µM, 92 Tested
Inhibition of bovine GRK2 S670A mutant expressed in Baculovirus expression system assessed as decrease in phosphorylation of urea-washed bovine rod outer segments preincubated for 30 mins followed by ATP addition and light exposure measured after 5 to 10 mins by SDS-PAGE analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method
Assay data:23 Active, 16 Activity ≤ 1 µM, 27 Tested
Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB
Assay data:4302 Active, 250 Activity ≤ 1 nM, 2931 Activity ≤ 1 µM, 4302 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
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