Binding affinity to N-terminal GST-His-tagged recombinant human PAK1 kinase domain expressed in Escherichia coli BL21 using KKRNRRLSVA as sustrate preincubated for 10 mins followed by ATP addition measured after 60 mins by FRET-based Z'Lyte assay
|
Homo sapiens
|
36.0
nM
|
|
Binding affinity to N-terminal GST-tagged recombinant human PAK4 kinase domain expressed in Escherichia coli using KKRNRRLSVA as substrate preincubated for 10 mins followed by ATP addition measured after 60 mins by FRET-based Z'Lyte assay
|
Homo sapiens
|
15.0
nM
|
|
Cytotoxicity against human MDA-MB-436 cells assessed as reduction in cell viability after 24 to 48 hrs by Celltiter-glo luminescence assay
|
Homo sapiens
|
0.79
nM
|
|
Binding affinity to N-terminal His-6-tagged recombinant human PAK1 using peptide substrate
|
Homo sapiens
|
15.0
nM
|
|
Binding affinity to N-terminal His-6-tagged recombinant human PAK4 using peptide substrate
|
Homo sapiens
|
36.0
nM
|
|
Inhibition of PAK1 (unknown origin) using Syntide2 peptide substrate by pyruvate kinase and lactate dehydrogenase coupled assay
|
Homo sapiens
|
39.0
nM
|
|
Inhibition of N-terminal His6-tagged human recombinant PAK4 (300 to 591 amino acids) using peptide-7 substrate by pyruvate kinase and lactate dehydrogenase coupled assay
|
Homo sapiens
|
15.0
nM
|
|
Inhibition of PAK1 (unknown origin) using Syntide2 peptide as substrate by pyruvate kinase/lactate dehydrogenase coupled assay
|
Homo sapiens
|
13.7
nM
|
|
Inhibition of PAK2 (unknown origin)
|
Homo sapiens
|
190.0
nM
|
|
Inhibition of PAK3 (unknown origin)
|
Homo sapiens
|
99.0
nM
|
|
Inhibition of N-terminal His6-tagged recombinant human PAK4 kinase domain (300 to 591) using peptide 7 as substrate by pyruvate kinase/lactate dehydrogenase coupled assay
|
Homo sapiens
|
18.7
nM
|
|
Inhibition of PAK5 (unknown origin) using peptide 7 as substrate by pyruvate kinase/lactate dehydrogenase coupled assay
|
Homo sapiens
|
18.1
nM
|
|
Inhibition of PAK6 (unknown origin) using peptide 7 as substrate by pyruvate kinase/lactate dehydrogenase coupled assay
|
Homo sapiens
|
17.1
nM
|
|
Enzymatic Assay: The enzymatic activity of PAK4 KD was measured by its ability to catalyzed the transfer of a phosphate residue from a nucleoside triphosphate to an amino acid side chain of a commercially available peptide (amino acid sequence EVPRRKSLVGTPYWM).
|
Homo sapiens
|
20.0
nM
|
|
Enzymatic Assay: The enzymatic activity of PAK4 KD was measured by its ability to catalyzed the transfer of a phosphate residue from a nucleoside triphosphate to an amino acid side chain of a commercially available peptide (amino acid sequence EVPRRKSLVGTPYWM).
|
Homo sapiens
|
3.9
nM
|
|
Inhibition of recombinant human GST-tagged PAK4 (295 to 591 residues) expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged PAK5 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged PAK6 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged ARG expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged CDK7/cyclin H/MNAT1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged CHK1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged CHK2 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged FLT3 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged GSK3beta expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged LynB expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged MARK1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged MARK3 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human GST-tagged Mer expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged MST1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged PHKgamma 1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged PRKACA expressed in Escherichia coli at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length PKCalpha expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged PKCtheta expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human PRKAA1 at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human PRKAA2 at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged RET expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged RSK2 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged RSK3 expressed in insect cells at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged RSK4 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged SRC expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged TSSK1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human His-tagged TRKA (441 to 796 residues) expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged YES expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged KHS1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged SIK2 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged PAK1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged PAK2 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length His-tagged PAK3 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged YSK1 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged MST3 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human full length GST-tagged MST4 expressed in Baculovirus at 1 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human adenosine A1 receptor expressed in CHO cells at 10 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human adenosine A2A receptor expressed in HEK293 cells at 10 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
Inhibition of recombinant human 5HT transporter expressed in CHO cells at 10 uM relative to control
|
Homo sapiens
|
75.0
%
|
|
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.
|
Homo sapiens
|
939.0
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.
|
Homo sapiens
|
981.0
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.
|
Homo sapiens
|
343.0
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.
|
Homo sapiens
|
275.0
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.
|
Homo sapiens
|
408.0
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.
|
Homo sapiens
|
14.0
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.
|
Homo sapiens
|
67.0
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.
|
Homo sapiens
|
3.0
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.
|
Homo sapiens
|
210.0
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.
|
Homo sapiens
|
90.0
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.
|
Homo sapiens
|
13.0
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.
|
Homo sapiens
|
2.0
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.
|
Homo sapiens
|
802.0
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.
|
Homo sapiens
|
208.0
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.
|
Homo sapiens
|
667.0
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.
|
Homo sapiens
|
237.0
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.
|
Homo sapiens
|
658.0
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.
|
Homo sapiens
|
157.0
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.
|
Homo sapiens
|
114.0
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.
|
Homo sapiens
|
105.0
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.
|
Homo sapiens
|
29.0
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.
|
Homo sapiens
|
57.0
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.
|
Homo sapiens
|
349.0
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.
|
Homo sapiens
|
71.0
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.
|
Homo sapiens
|
3.0
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.
|
Homo sapiens
|
53.0
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.
|
Homo sapiens
|
668.0
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.
|
Homo sapiens
|
6.0
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.
|
Homo sapiens
|
935.0
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.
|
Homo sapiens
|
354.0
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.
|
Homo sapiens
|
66.0
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.
|
Homo sapiens
|
6.0
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.
|
Homo sapiens
|
5.0
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.
|
Homo sapiens
|
873.0
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.
|
Homo sapiens
|
974.0
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.
|
Homo sapiens
|
85.0
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.
|
Homo sapiens
|
244.0
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.
|
Homo sapiens
|
268.0
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.
|
Homo sapiens
|
808.0
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.
|
Homo sapiens
|
312.0
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.
|
Homo sapiens
|
728.0
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.
|
Homo sapiens
|
820.0
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.
|
Homo sapiens
|
100.0
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.
|
Homo sapiens
|
111.0
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.
|
Homo sapiens
|
4.0
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.
|
Homo sapiens
|
357.0
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.
|
Homo sapiens
|
434.0
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.
|
Homo sapiens
|
369.0
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.
|
Homo sapiens
|
17.0
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.
|
Homo sapiens
|
75.0
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.
|
Homo sapiens
|
377.0
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.
|
Homo sapiens
|
626.0
nM
|
|
Inhibition of recombinant human N-terminal GST-fused PAK4 (1 to 591 residues) expressed in baculovirus expression system using S2 as substrate measured after 40 mins by HTRF assay
|
Homo sapiens
|
7.0
nM
|
|
Inhibition of PAK1 (unknown origin) using S2 peptide as substrate
|
Homo sapiens
|
14.0
nM
|
|
Inhibition of recombinant human N-terminal His6-tagged PAK4 expressed in bacterial expression system by pyruvate kinase/LDH enzyme coupled assay
|
Homo sapiens
|
19.0
nM
|
|
Inhibition of PAK4 (unknown origin)
|
Homo sapiens
|
24.2
nM
|
|
Inhibition of PAK4 (unknown origin) using substrate S2 after 60 mins by HTRF assay
|
Homo sapiens
|
24.0
nM
|
|
Inhibition of full length human PAK4 using substrate S2 after 60 mins by HTRF assay
|
Homo sapiens
|
18.0
nM
|
|
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
|
Homo sapiens
|
463.0
nM
|
|
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay
|
Homo sapiens
|
39.0
nM
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
6.34
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
5.63
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
21.1
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
8.211
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.02
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.02
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.13
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.13
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.02
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.02
%
|
|
Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) pre incubated up to 60 mins followed by substrate and ATP addition
|
Homo sapiens
|
7.0
nM
|
|
Inhibition of full length recombinant human N-terminal GST/His6-tagged PAK1 expressed in sf9 insect cells using tetra LRRWSLG as substrate preincubated for 20 min followed by [gamma33P]ATP addition and measured after 120 mins by Hotspot assay
|
Homo sapiens
|
52.0
nM
|
|
Inhibition of full length recombinant human N-terminal GST/His6-tagged PAK4 expressed in baculovirus infected sf9 insect cells using tetra LRRWSLG as substrate preincubated for 20 min followed by [gamma33P]ATP addition and measured after 120 mins by Hotspot assay
|
Homo sapiens
|
38.0
nM
|
|
Inhibition of PAK1 (unknown origin)
|
Homo sapiens
|
39.0
nM
|
|
Inhibition of PAK4 (unknown origin)
|
Homo sapiens
|
15.0
nM
|
|
Inhibition of PAK1 (unknown origin)
|
Homo sapiens
|
36.0
nM
|
|
Inhibition of PAK4 (unknown origin)
|
Homo sapiens
|
15.0
nM
|
|
Inhibition of PAK1 (unknown origin) using Syntide2 peptide as substrate by pyruvate kinase/LDH dehydrogenase coupled assay
|
Homo sapiens
|
14.0
nM
|
|