Inhibition of CDK2/Cyclin A by radiometric assay
|
None
|
47.0
nM
|
|
Inhibition of CDK1/Cyclin B by radiometric assay
|
None
|
190.0
nM
|
|
Inhibition of CDK4/Cyclin D1
|
None
|
67.0
nM
|
|
Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by alamar blue assay
|
Homo sapiens
|
82.0
nM
|
|
Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by alamar blue assay
|
Homo sapiens
|
350.0
nM
|
|
Antiproliferative activity against human MRC5 cells assessed as cell viability after 72 hrs by alamar blue assay
|
Homo sapiens
|
980.0
nM
|
|
Binding constant for CDC2L1 kinase domain
|
None
|
8.4
nM
|
|
Binding constant for DYRK1A kinase domain
|
None
|
120.0
nM
|
|
Binding constant for ERK8 kinase domain
|
None
|
120.0
nM
|
|
Binding constant for PFTAIRE2 kinase domain
|
None
|
62.0
nM
|
|
Binding constant for CASK kinase domain
|
None
|
24.0
nM
|
|
Binding constant for CDC2L5 kinase domain
|
None
|
3.2
nM
|
|
Binding constant for CLK1 kinase domain
|
None
|
990.0
nM
|
|
Binding constant for PCTK2 kinase domain
|
None
|
0.95
nM
|
|
Binding constant for CDK4-cyclinD1 kinase domain
|
None
|
20.0
nM
|
|
Binding constant for CDK4-cyclinD3 kinase domain
|
None
|
12.0
nM
|
|
Binding constant for CDK3 kinase domain
|
None
|
60.0
nM
|
|
Binding constant for CDK9 kinase domain
|
None
|
5.8
nM
|
|
Binding constant for CDK2 kinase domain
|
None
|
30.0
nM
|
|
Binding constant for CDK7 kinase domain
|
None
|
2.8
nM
|
|
Binding constant for GSK3B kinase domain
|
None
|
11.0
nM
|
|
Binding constant for PCTK3 kinase domain
|
None
|
14.0
nM
|
|
Binding constant for ERK5 kinase domain
|
None
|
42.0
nM
|
|
Binding constant for CDKL5 kinase domain
|
None
|
2.6
nM
|
|
Binding constant for CLK3 kinase domain
|
None
|
370.0
nM
|
|
Binding constant for DYRK1B kinase domain
|
None
|
290.0
nM
|
|
Binding constant for CDK5 kinase domain
|
None
|
700.0
nM
|
|
Binding constant for MAK kinase domain
|
None
|
97.0
nM
|
|
Binding constant for PCTK1 kinase domain
|
None
|
1.1
nM
|
|
Binding constant for PFTK1 kinase domain
|
None
|
16.0
nM
|
|
Binding constant for ICK kinase domain
|
None
|
8.3
nM
|
|
Binding constant for TAOK2 kinase domain
|
None
|
50.0
nM
|
|
Binding constant for TAOK3 kinase domain
|
None
|
57.0
nM
|
|
Binding constant for GSK3A kinase domain
|
None
|
23.0
nM
|
|
Binding constant for TAOK1 kinase domain
|
None
|
130.0
nM
|
|
Binding constant for CDC2L2 kinase domain
|
None
|
5.2
nM
|
|
Inhibition of CDK2/cyclin A (unknown origin) by radiometric filter binding assay
|
Homo sapiens
|
47.0
nM
|
|
Inhibition of CDK1/cyclin B (unknown origin) by radiometric filter binding assay
|
Homo sapiens
|
200.0
nM
|
|
Inhibition of CDK5/p35 (unknown origin) by DELFIA assay
|
Homo sapiens
|
13.0
nM
|
|
Inhibition of CDK9/cyclin T (unknown origin)
|
Homo sapiens
|
10.0
nM
|
|
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by Alamar blue assay
|
Homo sapiens
|
80.0
nM
|
|
Inhibition of CDK4/cyclin D1 (unknown origin) by ELISA
|
Homo sapiens
|
200.0
nM
|
|
Inhibition of CDK6/cyclin D3 (unknown origin) by ELISA
|
Homo sapiens
|
200.0
nM
|
|
Inhibition of GSK3beta (unknown origin) by radiometric filter binding assay
|
Homo sapiens
|
200.0
nM
|
|
Inhibition of CDK9/cyclin T (unknown origin)
|
Homo sapiens
|
10.0
nM
|
|
Inhibition of human full length C-terminal His6-tagged CDK1/N-terminal GST-tagged cyclin B expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate
|
Homo sapiens
|
190.0
nM
|
|
Inhibition of human full length C-terminal His6-tagged CDK2/N-terminal GST-tagged cyclin A expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate
|
Homo sapiens
|
44.0
nM
|
|
Inhibition of recombinant human full length C-terminal His6-tagged CDK2/N-terminal GST-tagged cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate
|
Homo sapiens
|
510.0
nM
|
|
Inhibition of recombinant human full length N-terminal His6-tagged CDK5/N-terminal GST-tagged p25 expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate
|
Homo sapiens
|
18.0
nM
|
|
Inhibition of recombinant human full length C-terminal His6-tagged CDK9/cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate
|
Homo sapiens
|
100.0
nM
|
|
Inhibition of recombinant human N-terminal GST-tagged CDK4/cyclin D1 expressed in baculovirus infected sf cells
|
Homo sapiens
|
67.0
nM
|
|
Inhibition of CDK6/cyclin D (unknown origin)
|
Homo sapiens
|
660.0
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
|
250.0
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
|
203.0
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
|
8.0
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
|
7.0
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
|
169.0
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
|
131.0
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
|
7.0
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
|
12.0
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
|
33.0
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
|
58.0
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
|
253.0
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
|
933.0
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
|
737.0
nM
|
|
Protection against cisplatin-induced cell death in neonatal mouse HEI-OC1 cells assessed as reduction in caspase-3/7 activity
|
Mus musculus
|
380.0
nM
|
|
Protection against cisplatin-induced toxicity in P3 mouse cochlear explants assessed as increase in outer hair cell count incubated for 24 hrs by phalloidin staining based confocal microscopy
|
Mus musculus
|
25.0
nM
|
|
Inhibition of C-terminal His6-tagged human full length CDK2/N-terminal GST-tagged human full length Cyclin A using histone H1 and [gamma-32P]-ATP incubated for 30 mins by phosphorimage based assay
|
Homo sapiens
|
47.0
nM
|
|
Inhibition of CDK2 (unknown origin)
|
Homo sapiens
|
47.0
nM
|
|
Inhibition of CDK9 (unknown origin)
|
Homo sapiens
|
10.0
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
|
9.78
%
|
|
Antiproliferative activity against human AsPC1 cells after 72 hrs by prestoblue assay
|
Homo sapiens
|
533.0
nM
|
|
Antiproliferative activity against human BxPC3 cells after 72 hrs by prestoblue assay
|
Homo sapiens
|
640.0
nM
|
|
Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by prestoblue assay
|
Homo sapiens
|
411.0
nM
|
|
Antiproliferative activity against human SUIT2 cells after 72 hrs by prestoblue assay
|
Homo sapiens
|
557.0
nM
|
|
Inhibition of CDK4/Cyclin D1 (unknown origin) using GST-tagged pRb (769 to 921 residues) as substrate measured after 30 mins by ELISA
|
Homo sapiens
|
100.0
nM
|
|
Inhibition of recombinant human full-length C-terminal His6-tagged CDK9/human full-length untagged cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate
|
Homo sapiens
|
10.0
nM
|
|
Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate
|
Homo sapiens
|
360.0
nM
|
|
Inhibition of recombinant full-length human C-terminal His6-tagged CDK1/human full-length N-terminal GST-tagged Cyclin B expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate measured after 2 hrs in presence of gamma[32P] ATP by topcount scintillation counting method
|
Homo sapiens
|
210.0
nM
|
|
Inhibition of human recombinant full-length N-terminal His6-tagged CDK5/recombinant human full-length N-terminal GST-tagged p35 using biotinylated-histone H1 as substrate after 30 mins by DELFIA
|
Homo sapiens
|
513.0
nM
|
|
Inhibition of CDK6/Cyclin D3 (unknown origin) using GST-tagged pRb (769 to 921 residues) as substrate measured after 30 mins by ELISA
|
Homo sapiens
|
170.0
nM
|
|
Inhibition of recombinant GST-tagged human full length CDK14/cyclin Y (2 to end residues) preincubated for 30 mins by Lantha screen eu binding assay
|
Homo sapiens
|
19.8
nM
|
|
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by cell titer glo-based luminescence assay
|
Homo sapiens
|
132.0
nM
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
19.26
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
4.32
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
3.89
%
|
|
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
|
9.19
%
|
|
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
|
4.42
%
|
|
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
|
3.03
%
|
|
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
|
9.19
%
|
|
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
|
4.42
%
|
|
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
|
3.03
%
|
|
Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay
|
Homo sapiens
|
710.0
nM
|
|
Inhibition of CDK4 (unknown origin)
|
Homo sapiens
|
18.0
nM
|
|
Inhibition of CDK1 (unknown origin)
|
Homo sapiens
|
210.0
nM
|
|
Inhibition of CDK2 (unknown origin)
|
Homo sapiens
|
47.0
nM
|
|
Inhibition of CDK4 (unknown origin)
|
Homo sapiens
|
100.0
nM
|
|
Inhibition of CDK5 (unknown origin)
|
Homo sapiens
|
13.0
nM
|
|
Inhibition of CDK6 (unknown origin)
|
Homo sapiens
|
170.0
nM
|
|
Inhibition of CDK9 (unknown origin)
|
Homo sapiens
|
10.0
nM
|
|
Inhibition of CDK1/cyclin B1 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay
|
Homo sapiens
|
89.0
nM
|
|
Inhibition of CDK2/cyclin A2 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay
|
Homo sapiens
|
32.0
nM
|
|
Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay
|
Homo sapiens
|
166.0
nM
|
|
Inhibition of CDK4/cyclin D3 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay
|
Homo sapiens
|
72.0
nM
|
|
Inhibition of CDK9/cyclin T1 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay
|
Homo sapiens
|
5.0
nM
|
|
Inhibition of C-terminal His6-tagged human full length CDK1/N-terminal GST-tagged human full length cyclin B expressed in baculovirus infected Sf21 cells using histone H1 as substrate measured after 2 hrs in presence of ATP by radiometric filter-binding assay
|
Homo sapiens
|
210.0
nM
|
|
Inhibition of CDK2/cyclin A (unknown origin) using histone H1 as substrate measured after 4 hrs in presence of ATP by radiometric filter-binding assay
|
Homo sapiens
|
47.0
nM
|
|
Inhibition of CDK6/cyclin D3 (unknown origin) incubated for 30 mins in presence of ATP by fluorescence based analysis
|
Homo sapiens
|
170.0
nM
|
|
Inhibition of CDK3/cyclin E1 (unknown origin)
|
Homo sapiens
|
360.0
nM
|
|
Inhibition of CDK9/cyclin T1 (unknown origin)
|
Homo sapiens
|
10.0
nM
|
|
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay
|
Homo sapiens
|
391.0
nM
|
|
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 96 hrs by Celltiter-Glo luminescent assay
|
Homo sapiens
|
425.0
nM
|
|
Cytotoxicity against human LX2 cells assessed as inhibition of cell growth at 100 uM measured after 96 hrs by Celltiter-Glo luminescent assay
|
Homo sapiens
|
39.4
%
|
|
Inhibition of CDK1/cyclin B (unknown origin)
|
Homo sapiens
|
210.0
nM
|
|
Inhibition of CDK2/cyclin A (unknown origin)
|
Homo sapiens
|
47.0
nM
|
|
Inhibition of CDK3/cyclin E (unknown origin)
|
Homo sapiens
|
360.0
nM
|
|
Inhibition of CDK9/cyclin T (unknown origin)
|
Homo sapiens
|
10.0
nM
|
|