|
Inhibition of ErbB1 relative to control
|
None
|
5.6
nM
|
|
|
Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay
|
None
|
200.0
nM
|
|
|
Inhibition of human BTK by enzymatic assay
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of BLK
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of BMX
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of RET
|
Homo sapiens
|
37.0
nM
|
|
|
Inhibition of recombinant Btk after 60 mins
|
None
|
0.5
nM
|
|
|
Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis
|
Homo sapiens
|
7.5
nM
|
|
|
Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of cell proliferation of human Rec1 cells at 5 uM after 24 hrs by MTT assay
|
Homo sapiens
|
3.0
%
|
|
|
Inhibition of BTK (unknown origin)
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of human recombinant BTK incubated for 5 mins by HTRF kinase assay
|
Homo sapiens
|
4.0
nM
|
|
|
Inhibition of BTK (unknown origin) after 1 hr by TR-FRET assay
|
Homo sapiens
|
4.0
nM
|
|
|
In Vitro Inhibition Assay: Measurements were performed in a reaction volume of 50 μL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 μM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25 μL of 1× Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1× Lance buffer were added in a 25 μL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. The TR-FRET signal was measured on a multimode plate reader with an excitation wavelength (πEx) of 330 nm and detection wavelengths (πEm) of 615 and 665 nm. Activity was determined by the ratio of the fluorescence at 665 nm to that at 615 nm. For each compound, enzyme activity was measured at various concentrations of compound. Negative control reactions were performed in the absence of inhibitor in replicates of six, and two no-enzyme controls were used to determine baseline fluorescence levels.
|
Homo sapiens
|
0.72
nM
|
|
|
Time-Resolved Fluorescence Resonance Energy Transfer Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology.
|
Homo sapiens
|
0.72
nM
|
|
Time-Resolved Fluorescence Resonance Energy Transfer Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology.
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition Assay: When setting conditions for the measurement of the inhibitory effect of the compounds on FGFR2 kinase activity, FL-Peptide 22 (Caliper Life Sciences, Inc.) was used as a substrate. The purified recombinant human FGFR2 protein used in the test was purchased from Carna Biosciences, Inc. In the measurement of the inhibitory effect of the compounds, first, a test compound was gradually diluted with dimethylsulfoxide (DMSO) to a concentration that was 20 times higher than the final concentration. Next, the purified human FGFR2 protein, FL-Peptide 22 (final concentration: 1.5 .mu.M), magnesium chloride (final concentration: 5 mM), ATP (final concentration: 75 .mu.M), and the test compound DMSO solution (final concentration of DMSO: 5%) were added to a reaction buffer (15 mM Tris-HCl pH 7.5, 0.01% Tween-20, 2 mM DTT), and the mixture was incubated at 25.degree. C. for 120 minutes to perform a kinase reaction. EDTA (final concentration: 30 mM) diluted with a separation buffer.
|
Homo sapiens
|
280.0
nM
|
|
|
In Vitro Inhibition Assay: Measurements were performed in a reaction volume of 50 μL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 μM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25 μL of 1× Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1× Lance buffer were added in a 25 μL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. The TR-FRET signal was measured on a multimode plate reader with an excitation wavelength (πEx) of 330 nm and detection wavelengths (πEm) of 615 and 665 nm. Activity was determined by the ratio of the fluorescence at 665 nm to that at 615 nm. For each compound, enzyme activity was measured at various concentrations of compound. Negative control reactions were performed in the absence of inhibitor in replicates of six, and two no-enzyme controls were used to determine baseline fluorescence levels.
|
Homo sapiens
|
97.0
nM
|
|
|
In Vitro Inhibition Assay: Measurements were performed in a reaction volume of 50 μL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 μM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25 μL of 1× Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1× Lance buffer were added in a 25 μL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour. The TR-FRET signal was measured on a multimode plate reader with an excitation wavelength (πEx) of 330 nm and detection wavelengths (πEm) of 615 and 665 nm. Activity was determined by the ratio of the fluorescence at 665 nm to that at 615 nm. For each compound, enzyme activity was measured at various concentrations of compound. Negative control reactions were performed in the absence of inhibitor in replicates of six, and two no-enzyme controls were used to determine baseline fluorescence levels.
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of BTK (unknown origin) assessed as reduction in phosphorylation of coumarin and fluorescein-labeled FRET peptide substrate at 10 uM incubated for 1 hr by Z-Lyte assay relative to control
|
Homo sapiens
|
100.13
%
|
|
|
Inhibition of BTK (unknown origin) assessed as reduction in phosphorylation of coumarin and fluorescein-labeled FRET peptide substrate incubated for 1 hr by Z-Lyte assay
|
Homo sapiens
|
0.64
nM
|
|
|
Irreversible inhibition of recombinant BTK (unknown origin) incubated for 1 hr by FRET assay
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay
|
Homo sapiens
|
0.3
nM
|
|
|
Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay
|
Homo sapiens
|
0.34
nM
|
|
|
Inhibition of PF-06658607 binding to BTK in human Ramos cells after 1 hr by gel-based ABPP assay
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of PF-06658607 binding to recombinant C-terminal FLAG-tagged FAM213A (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay
|
Homo sapiens
|
900.0
nM
|
|
|
Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. Measurements were performed in a reaction volume of 50 uL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 uM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25uL of 1x Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1x Lance buffer were added in a 25 uL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour.
|
Homo sapiens
|
0.72
nM
|
|
Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. Measurements were performed in a reaction volume of 50 uL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 uM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25uL of 1x Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1x Lance buffer were added in a 25 uL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour.
|
Homo sapiens
|
0.5
nM
|
|
Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Btk kinase activity was determined using a time-resolved fluorescence resonance energy transfer (TR-FRET) methodology. Measurements were performed in a reaction volume of 50 uL using 96-well assay plates. Kinase enzyme, inhibitor, ATP (at the Km for the kinase), and 1 uM peptide substrate (Biotin-AVLESEEELYSSARQ-NH2) were incubated in a reaction buffer composed of 20 mM Tris, 50 mM NaCl, MgCl2 (5-25 mM depending on the kinase), MnCl2 (0-10 mM), 1 mM DTT, 0.1 mM EDTA, 0.01% bovine serum albumin, 0.005% Tween-20, and 10% DMSO at pH 7.4 for one hour. The reaction was quenched by the addition of 1.2 equivalents of EDTA (relative to divalent cation) in 25uL of 1x Lance buffer (Perkin-Elmer). Streptavidin-APC (Perkin-Elmer) and Eu-labeled p-Tyr100 antibody (Perkin-Elmer) in 1x Lance buffer were added in a 25 uL volume to give final concentrations of 100 nM and 2.5 nM, respectively, and the mixture was allowed to incubate for one hour.
|
Homo sapiens
|
1.4
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
11.7
nM
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
11.7
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.8
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
77.8
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
9.4
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
0.1
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
2.0
nM
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
2.0
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
262.6
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
2.3
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
95.6
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
3.7
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
16.2
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
6.5
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
86.1
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
3.3
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
2.2
nM
|
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
10.4
nM
|
|
HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kinase assay. Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
10.4
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
11.7
nM
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
11.7
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.8
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
77.8
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
9.4
nM
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
0.1
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
2.0
nM
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
2.0
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
0.5
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
262.6
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
2.3
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
None
|
95.6
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
3.7
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
16.2
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
6.5
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
86.1
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
3.3
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
2.2
nM
|
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
10.4
nM
|
|
In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction conditions were 1 uM ATP, one hour incubation with inhibitor, and kinase activity detected using 33-ATP phosphorylation of an appropriately selected peptide substrate.
|
Homo sapiens
|
10.4
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
|
919.0
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
|
10.0
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
|
399.0
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
|
43.0
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
|
589.0
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
|
305.0
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
|
42.0
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
|
103.0
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
|
148.0
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
|
243.0
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
|
31.0
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
|
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
|
97.0
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
|
25.0
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
|
27.0
nM
|
|
|
Inhibition of N-terminal His-tagged full length human recombinant BTK expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay
|
Homo sapiens
|
0.34
nM
|
|
|
Inhibition of human BTK using KVEKIGEGTYGVVYK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition by filter binding method
|
Homo sapiens
|
0.11
nM
|
|
|
Inhibition of human TEC using poly[Glu:Tyr] as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition by filter binding method
|
Homo sapiens
|
1.86
nM
|
|
|
Inhibition of BTK (unknown origin) preincubated for 1 hr followed by ATP addition measured after 1 hr by immobilized metal ion affinity-based fluorescence polarization assay
|
Homo sapiens
|
1.5
nM
|
|
|
Inhibition of TEC (unknown origin) after 2 hrs by LanthaScreen assay
|
Homo sapiens
|
7.0
nM
|
|
|
Inhibition of recombinant human cytoplasmic His-tagged ERBB2 expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
91.0
%
|
|
|
Inhibition of BTK in human whole blood-derived CD19+ B cells assessed as suppression of anti-IgM stimulated-CD69 expression preincubated for 1 hr followed by IgM stimulation for 18 hrs by FACS analysis
|
Homo sapiens
|
12.0
nM
|
|
|
Inhibition of recombinant human full length His-tagged BTK expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
101.0
%
|
|
|
Inhibition of cytoplasmic recombinant human full length His-tagged BMX expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
99.0
%
|
|
|
Inhibition of human full length GST-tagged TXK expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
93.0
%
|
|
|
Inhibition of recombinant human full length His-tagged BLK expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
102.0
%
|
|
|
Inhibition of recombinant human catalytic GST-tagged JAK3 expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
80.0
%
|
|
|
Inhibition of recombinant human cytoplasmic GST-tagged EGFR expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
89.0
%
|
|
|
Inhibition of recombinant human cytoplasmic GST-tagged LTK expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
81.0
%
|
|
|
Inhibition of recombinant human cytoplasmic GST-tagged ERBB4 expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
93.0
%
|
|
|
Inhibition of recombinant human cytoplasmic full length His-tagged TEC expressed in baculovirus at 1 uM by Z'-LYTE assay
|
Homo sapiens
|
100.0
%
|
|
|
Inhibition of BTK in human whole blood derived-basophils assessed as suppression of IgE mediated-FcepsilonR ligation-stimulated CD63 expression
|
Homo sapiens
|
171.0
nM
|
|
|
Inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
|
Homo sapiens
|
12.0
nM
|
|
|
Inhibition of full length recombinant human N-terminal GST-tagged BMX expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
|
Homo sapiens
|
8.0
nM
|
|
|
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
|
Homo sapiens
|
146.0
nM
|
|
|
Inhibition of recombinant human N-terminal GST-tagged wild-type EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
|
Homo sapiens
|
123.0
nM
|
|
|
Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
|
Homo sapiens
|
4.8
nM
|
|
|
Inhibition of wild type N-terminal GST-fused human EGFR cytoplasmic domain expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 25 mins by HTRF assay
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 15 mins by HTRF assay
|
Homo sapiens
|
120.0
nM
|
|
|
Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 20 mins by HTRF assay
|
Homo sapiens
|
390.0
nM
|
|
|
Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
|
Homo sapiens
|
450.0
nM
|
|
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
|
Homo sapiens
|
640.0
nM
|
|
|
Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells after 60 mins by ADP-Glo kinase assay
|
Homo sapiens
|
0.34
nM
|
|
|
Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant after 72 hrs by MTT assay
|
Homo sapiens
|
39.0
nM
|
|
|
Inhibition of BMX (unknown origin)
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of EGFR (unknown origin)
|
Homo sapiens
|
5.6
nM
|
|
|
Inhibition of Her2 (unknown origin)
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of recombinant human BTK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
0.4
nM
|
|
|
Inhibition of recombinant full-length N-terminal His-tagged human BTK C481S mutant expressed in baculovirus infected Sf9 insect cells using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
14.4
nM
|
|
|
Antiproliferative activity against human TMD8 cells after 72 hrs by MTT assay
|
Homo sapiens
|
10.0
nM
|
|
|
Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay
|
Homo sapiens
|
920.0
nM
|
|
|
Inhibition of recombinant human BLK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of recombinant human ErbB4 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
1.8
nM
|
|
|
Inhibition of recombinant human EGFR using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
1.2
nM
|
|
|
Inhibition of recombinant human TEC using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of recombinant human TXK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
3.0
nM
|
|
|
Inhibition of recombinant human ITK using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
13.9
nM
|
|
|
Inhibition of recombinant human RET using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
5.2
nM
|
|
|
Inhibition of recombinant human ErbB2 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
1.5
nM
|
|
|
Inhibition of recombinant human BMX using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISA
|
Homo sapiens
|
5.8
nM
|
|
|
Inhibition of N-terminal DYKDDDDK tagged biotinylated activated human recombinant BTK using FITC-labeled Srctide peptide substrate by mobility shift assay
|
Homo sapiens
|
0.54
nM
|
|
|
Inhibition of N-terminal DYKDDDDK tagged biotinylated unactivated human recombinant BTK using FITC-labeled Srctide peptide substrate by by mobility shift assay
|
Homo sapiens
|
0.33
nM
|
|
|
Inhibition of full length human N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus expression system using biotinylated substrate after 50 mins by HTRF assay
|
Homo sapiens
|
5.49
nM
|
|
|
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781-end residues) expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) peptide as substrate after 60 mins by ADP-Glo assay
|
Homo sapiens
|
100.0
nM
|
|
|
Inhibition of full length recombinant human N-terminal His-tagged BTK expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) peptide as substrate after 60 mins by ADP-Glo assay
|
Homo sapiens
|
0.4
nM
|
|
|
Inhibition of recombinant full length human N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells at 200 nM using poly (4:1 Glu, Tyr) as substrate after 60 mins by ADP-Glo assay relative to control
|
Homo sapiens
|
100.0
%
|
|
|
Inhibition of recombinant full length human N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (4:1 Glu, Tyr) as substrate after 60 mins by ADP-Glo assay
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of human full length BTK using FITC-AHA-EEPLYWSFPAKKK-NH2 as substrate after 90 mins by microfluid mobility shift assay
|
Homo sapiens
|
0.2
nM
|
|
|
Inhibition of BTK in human PBMC assessed as reduction in anti-IgM-induced CD69 expression incubated for 1 hr by flow cytometric analysis
|
Homo sapiens
|
4.6
nM
|
|
|
Inhibition of BTK in whole blood (unknown origin)
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of EGFR (unknown origin) at 1 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
|
Inhibition of recombinant full-length N-terminal His-tagged human BTK expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay
|
Homo sapiens
|
0.3
nM
|
|
|
Inhibition of recombinant N-terminal GST-tagged human JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay
|
Homo sapiens
|
16.1
nM
|
|
|
Inhibition of recombinant human full-length N-terminal His6-tagged BTK expressed in baculovirus infected Sf21insect cells using poly (4:1 Glu, Tyr) as substrate measured after 1 hr by ELISA
|
Homo sapiens
|
0.6
nM
|
|
|
Inhibition of human ErbB2 using using poly (4:1 Glu, Tyr) as substrate measured after 1 hr in presence of [gamma-33P]ATP
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of human ITK using using myelin basic protein as substrate measured after 1 hr in presence of [gamma-33P]ATP
|
Homo sapiens
|
10.7
nM
|
|
|
Inhibition of BTK in human PBMC
|
Homo sapiens
|
4.6
nM
|
|
|
Inhibition of BTK in human WBC
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of recombinant human full length N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus expression system using FITC-AHA-EEPLYWSFPAKKK-NH2 substrate measured after 90 mins by off-chip mobility shift assay
|
Homo sapiens
|
0.2
nM
|
|
|
Inhibition of BTK in goat anti-human IgM F(ab')2-stimulated human PBMC assessed as suppression of BCR-induced CD69 expression on B cells pretreated for 1 hr followed by blood stimulation measured after overnight incubation by flow cytometry
|
Homo sapiens
|
4.6
nM
|
|
|
Inhibition of BTK in human whole blood
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of human ERG
|
Homo sapiens
|
1.1
%
|
|
|
Inhibition of BTK (unknown origin)
|
Homo sapiens
|
0.5
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
|
-3.39
%
|
|
|
Inhibition of BTK (unknown origin)
|
Homo sapiens
|
0.21
nM
|
|
|
Inhibition of MKK7 beta1 S273D/T275D double mutant (unknown origin) using JNK1 K55M mutant as substrate by ADP-Glo assay
|
Homo sapiens
|
78.0
nM
|
|
|
Inhibition of BTK (unknown origin) in the presence of ATP by caliper mobility shift assay
|
Homo sapiens
|
1.2
nM
|
|
|
Inhibition of human recombinant EGFR using Ulight-CAGAGAIETDKEYYTVKD measured after 15 mins in the presence of ATP by LANCE method
|
Homo sapiens
|
12.0
nM
|
|
|
Inhibition of human recombinant HER2 using biotinyl-beta amyloid beta amyloid beta AAEEEEYFELVAKKK measured after 10 mins in the presence of ATP by HTRF assay
|
Homo sapiens
|
22.0
nM
|
|
|
Inhibition of HER4 (unknown origin)
|
Homo sapiens
|
0.6
nM
|
|
|
Inhibition of human recombinant JAK3 using Ulight-CAGAGAIETDKEYYTVKD measured after 60 mins in the presence of ATP by LANCE method
|
Homo sapiens
|
22.0
nM
|
|
|
Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay
|
Homo sapiens
|
3.89
nM
|
|
|
Inhibition of BTK (unknown origin) after 60 mins by FRET assay
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of full-length human recombinant BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate measured after 60 mins by caliper assay
|
Homo sapiens
|
2.3
nM
|
|
|
Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by HTRF assay
|
Homo sapiens
|
16.0
nM
|
|
|
Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated CD69 expression on B cells preincubated for 60 mins followed by anti-IgM antibody/IL4 stimulation and measured after 16 hrs by flow cytometry
|
Homo sapiens
|
66.0
nM
|
|
|
Binding affinity to DNA-tagged recombinant BTK (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
1.9
nM
|
|
|
Binding affinity to DNA-tagged recombinant BMX (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
1.6
nM
|
|
|
Binding affinity to DNA-tagged recombinant TEC (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
1.7
nM
|
|
|
Binding affinity to DNA-tagged recombinant ITK (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
57.0
nM
|
|
|
Binding affinity to DNA-tagged recombinant EGFR (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
6.9
nM
|
|
|
Binding affinity to DNA-tagged recombinant ERBB2 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
1.2
nM
|
|
|
Binding affinity to DNA-tagged recombinant ERBB4 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
2.4
nM
|
|
|
Binding affinity to DNA-tagged recombinant JAK3 (unknown origin) measured after 1 hr by biotinylated-ligand affinity bead-based qPCR analysis
|
Homo sapiens
|
37.0
nM
|
|
|
Inhibition of BTK in human basophils assessed as reduction in anti-IgE mouse IgG1 antibody Le2-stimulated CD63 expression on basophil preincubated for 30 mins in presence of IgE antibody B11 followed by anti-IgE mouse IgG1 antibody Le2 stimulation and measured after 15 mins by flow cytometry
|
Homo sapiens
|
230.0
nM
|
|
|
Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells at 10 uM using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay relative to control
|
Homo sapiens
|
99.76
%
|
|
|
Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay
|
Homo sapiens
|
1.8
nM
|
|
|
Antiproliferative activity against human Ramos cells at 40 uM measured after 72 hrs by CCK-8 assay relative to control
|
Homo sapiens
|
81.2
%
|
|
|
Antiproliferative activity against human Raji cells at 40 uM measured after 72 hrs by CCK-8 assay relative to control
|
Homo sapiens
|
76.23
%
|
|
|
Inhibition of human recombinant full length N-terminal His tagged BTK C481S mutant expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay
|
Homo sapiens
|
17.0
nM
|
|
|
Inhibition of human recombinant full-length BTK at 100 nM using poly (4:1 Glu, Tyr) peptide substrate after 60 mins by ADP-Glo assay relative to control
|
Homo sapiens
|
99.4
%
|
|
|
Inhibition of recombinant full-length human N-terminal GST-fused BTK (2 to 659 residues) expressed in baculovirus expression system using biotin-labelled peptide as substrate measured after 50 mins by TR-FRET assay
|
Homo sapiens
|
5.49
nM
|
|
|
Antiproliferative activity against human DOHH2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
Homo sapiens
|
33.4
nM
|
|
|
Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
Homo sapiens
|
874.2
nM
|
|
|
Antiproliferative activity against human WSU-DLCL2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
Homo sapiens
|
487.2
nM
|
|
|
Cytotoxicity against human PBMC assessed as inhibition of cell proliferation at 30 uM after 72 hrs by CellTiter-Glo luminescent cell viability assay relative to control
|
Homo sapiens
|
69.0
%
|
|
|
Inhibition of full-length recombinant human C-terminal His-tagged SRC cytoplasmic domain expressed in baculovirus expression system using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
|
Homo sapiens
|
38.0
nM
|
|
|
Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
|
Homo sapiens
|
3.4
nM
|
|
|
Inhibition of full-length human His-tagged BTK expressed in baculovirus expression system using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
|
Homo sapiens
|
0.1
nM
|
|
|
Inhibition of human EGFR cytoplasmic domain expressed in baculovirus expression system using FITC-C6-KKAEEEEYFELVAKK-NH2 as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
|
Homo sapiens
|
18.0
nM
|
|
|
Inhibition of BTK (unknown origin) by ELISA
|
Homo sapiens
|
0.6
nM
|
|
|
Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of EGFR (unknown origin)
|
Homo sapiens
|
12.0
nM
|
|
|
Inhibition of JAK3 (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay
|
Homo sapiens
|
3.5
nM
|
|
|
Inhibition of EGFR (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay
|
Homo sapiens
|
0.75
nM
|
|
|
Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay
|
Homo sapiens
|
0.3
nM
|
|
|
Inhibition of human BTK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
0.46
nM
|
|
|
Inhibition of ITK (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay
|
Homo sapiens
|
3.0
nM
|
|
|
Inhibition of TEC (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay
|
Homo sapiens
|
0.57
nM
|
|
|
Inhibition of HER2 (unknown origin) preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay
|
Homo sapiens
|
19.0
nM
|
|
|
Inhibition of human BLK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
0.23
nM
|
|
|
Inhibition of human BMX using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of human BRK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
18.0
nM
|
|
|
Inhibition of human HER4 using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
0.25
nM
|
|
|
Inhibition of human FGR using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
1.82
nM
|
|
|
Inhibition of human FRK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
79.0
nM
|
|
|
Inhibition of human LCK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
2.85
nM
|
|
|
Inhibition of human TXK using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
|
Homo sapiens
|
2.89
nM
|
|
|
Inhibition of EGFR in human A431 cells assessed as reduction in EGFR phosphorylation at Tyr1068 residues preincubated for 1 hr followed by human EGF stimulation and measured after 10 mins by HTRF assay
|
Homo sapiens
|
101.0
nM
|
|
|
Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis
|
Homo sapiens
|
76.9
nM
|
|
|
Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay
|
Homo sapiens
|
46.7
nM
|
|
|
Inhibition of BTK (unknown origin) by ADP-gloassay
|
Homo sapiens
|
0.7
nM
|
|
|
Inhibition of N-terminal His-tagged MKK7 beta1 S273D/T275D double mutant (unknown origin) expressed in insect cells using JNK1 K55M mutant as substrate by ADP-Glo assay
|
Homo sapiens
|
78.0
nM
|
|
|
Inhibition of wild type EGFR (unknown origin) by HTRF assay
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of EGFR L858R/T790M double mutant (unknown origin) by HTRF assay
|
Homo sapiens
|
40.0
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
|
15.23
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
13.6
%
|
|
|
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
|
0.11
%
|
|
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
|
-0.31
%
|
|
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
|
-0.31
%
|
|
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
|
0.11
%
|
|
|
Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay
|
Homo sapiens
|
0.3
nM
|
|
|
Inhibition of recombinant human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay
|
Homo sapiens
|
20.3
nM
|
|
|
Inhibition of BTK (unknown origin)
|
Homo sapiens
|
2.2
nM
|
|
|
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
|
Homo sapiens
|
16.1
nM
|
|
|
Inhibition of BTK in human whole blood cells after 1 hr by ELISA
|
Homo sapiens
|
105.0
nM
|
|
|
Inhibition of recombinant human BTK using fluoresceinated peptide as substrate after 60 mins fluorescence assay
|
Homo sapiens
|
0.08
nM
|
|
|
Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of His-tagged BTK (unknown origin) after 1.5 hrs by HTRF analysis
|
Homo sapiens
|
425.0
nM
|
|
|
Inhibition of HER1 (unknown origin)
|
Homo sapiens
|
30.0
nM
|
|
|
Inhibition of HER4 (unknown origin)
|
Homo sapiens
|
30.0
nM
|
|
|
Inhibition of BTK in human whole blood cells after 30 mins by ELISA
|
Homo sapiens
|
200.0
nM
|
|
|
Inhibition of BTK in human whole blood cells after 120 mins by ELISA
|
Homo sapiens
|
57.5
nM
|
|
|
Inhibition of BTK in human whole blood assessed as reduction in polyclonal anti-IgM antibody/human IL4-stimulated CD69 cell surface expression on B cells incubated for 16 hrs by FACS analysis
|
Homo sapiens
|
66.0
nM
|
|
|
Inhibition of EGF-induced EGFR phosphorylation in human A431 cells preincubated for 24 hrs followed by EGF stimulation and measured after 10 mins by HTRF based immunoassay
|
Homo sapiens
|
45.0
nM
|
|
|
Inhibition of BTK in vitamin D3 differentiated human THP1 cells assessed as inhibition of FCgammaR-induced IL8 production measured after 24 hrs by immunoblot analysis
|
Homo sapiens
|
5.0
nM
|
|
|
Inhibition of BMX (unknown origin)
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of ERBB4 (unknown origin)
|
Homo sapiens
|
7.0
nM
|
|
|
Inhibition of EGFR (unknown origin)
|
Homo sapiens
|
16.0
nM
|
|
|
Inhibition of full length human unphosphorylated BTK using FITC-Ahx-TSELKKVVALYDYMPMNAND-NH2 as substrate incubated for 60 mins in presence of ATP at Km concentration
|
Homo sapiens
|
5.0
nM
|
|
|
Inhibition of wild type BTK (unknown origin)
|
Homo sapiens
|
2.2
nM
|
|
|
Inhibition of GP6 in human whole blood assessed as protein-mediated platelet aggregation preincubated for 15 mins followed by collagen stimulation and measured for 10 mins by multiple electrode aggregometry
|
Homo sapiens
|
120.0
nM
|
|
|
Inhibition of human platelet adhesion to immobilised CRP-XL at 1 umol/L preincubated for 4 mins followed by CRP-XL addition and measured after 45 mins relative to control
|
Homo sapiens
|
70.0
%
|
|
|
Inhibition of human platelet lamellipodia formation on CRP-XL 1 umol/L preincubated for 4 mins followed by CRP-XL addition and measured after 45 mins (Rvb = 69%)
|
Homo sapiens
|
11.0
%
|
|
|
Inhibition of BTK (unknown origin) One-hour enzymatic assay without pre-incubation
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of BTK (unknown origin) at 1 uM by caliper mobility shift assay relative to control
|
Homo sapiens
|
99.6
%
|
|
|
Inhibition of BTK (unknown origin) at 0.1 uM by caliper mobility shift assay relative to control
|
Homo sapiens
|
99.3
%
|
|
|
Inhibition of BTK (unknown origin) by caliper mobility shift assay
|
Homo sapiens
|
810.0
nM
|
|
|
Inhibition of BMX (unknown origin)
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of Tec (unknown origin)
|
Homo sapiens
|
78.0
nM
|
|
|
Inhibition of ITK (unknown origin)
|
Homo sapiens
|
10.7
nM
|
|
|
Inhibition of BLK (unknown origin)
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of recombinant human EGFR using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 15 mins by LANCE assay
|
Homo sapiens
|
5.6
nM
|
|
|
Inhibition of ErBB2 (unknown origin)
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of recombinant human JAK3 using Ulight-CAGAGAIETDKEYYTVKD as substrate incubate for 60 mins by LANCE assay
|
Homo sapiens
|
16.1
nM
|
|
|
Inhibition of CSK (unknown origin)
|
Homo sapiens
|
2.3
nM
|
|
|
Inhibition of RET (unknown origin)
|
Homo sapiens
|
36.5
nM
|
|
|
Inhibition of FGR (unknown origin)
|
Homo sapiens
|
2.3
nM
|
|
|
Inhibition of FRK (unknown origin)
|
Homo sapiens
|
29.2
nM
|
|
|
Inhibition of FLT3 (unknown origin)
|
Homo sapiens
|
73.0
nM
|
|
|
Inhibition of HCK (unknown origin)
|
Homo sapiens
|
3.7
nM
|
|
|
Inhibition of recombinant human YES using biotinyl-beta Abeta-Abeta AYQAEENTYDEYEN as substrate incubate for 30 mins by LANCE assay
|
Homo sapiens
|
6.5
nM
|
|
|
Inhibition of recombinant human FYN using biotinyl-beta Abeta-Abeta AYQAEENTYDEYEN as substrate incubate for 60 mins by LANCE assay
|
Homo sapiens
|
96.0
nM
|
|
|
Inhibition of recombinant human LCK using Ulight-Poly GAT[EAY(1:1:1)]n as substrate incubate for 10 mins by LANCE assay
|
Homo sapiens
|
33.2
nM
|
|
|
Inhibition of recombinant human LYN using biotinyl-beta Abeta-Abeta AKVEKIGEGTYGVVYK as substrate incubate for 120 mins by LANCE assay
|
Homo sapiens
|
200.0
nM
|
|
|
Inhibition of recombinant human SRC using Ulight-Poly GAT[EAY(1:1:1)]n as substrate incubate for 10 mins by LANCE assay
|
Homo sapiens
|
171.0
nM
|
|
|
Inhibition of SRC (unknown origin)
|
Homo sapiens
|
119.2
nM
|
|
|
Inhibition of HCK (unknown origin)
|
Homo sapiens
|
15.3
nM
|
|
|
Inhibition of SRC S345C mutant (unknown origin)
|
Homo sapiens
|
15.88
nM
|
|
|
Inhibition of SRC T338M/S345C double mutant (unknown origin)
|
Homo sapiens
|
243.7
nM
|
|
|
Inhibition of BTK (unknown origin)
|
Homo sapiens
|
0.72
nM
|
|
|
Inhibition of BTK T333M mutant (unknown origin)
|
Homo sapiens
|
66.0
nM
|
|
|
Inhibition of EGFR (unknown origin)
|
Homo sapiens
|
96.0
nM
|
|
|
Inhibition of EGFR T790M mutant (unknown origin)
|
Homo sapiens
|
51.0
nM
|
|
|
Inhibition of recombinant human GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system using Tyr 04 peptide as substrate preincubated for 1 hr by Z'-LYTE assay
|
Homo sapiens
|
5.3
nM
|
|
|
Inhibition of His-tagged recombinant human His-tagged full length BTK expressed in baculovirus expression system using Tyr01 peptide as substrate preincubated for 1 hr by Z'lyte assay
|
Homo sapiens
|
0.43
nM
|
|
|
Inhibition of His-tagged recombinant human TEC expressed in baculovirus expression system preincubated for 1 hr by Z'lyte assay
|
Homo sapiens
|
1.8
nM
|
|
|
Inhibition of His-tagged recombinant full length human His-tagged BMX cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of recombinant full length human GST-tagged ITK expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
|
Homo sapiens
|
168.0
nM
|
|
|
Inhibition of recombinant human N-terminal GST-tagged TXK (260 to 527 residues) expressed in baculovirus expression system using tyrosine-6 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of His-tagged human recombinant ERBB2 (676 to 1255 residues) expressed in baculovirus expression system using Tyr 06 as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
|
Homo sapiens
|
6.4
nM
|
|
|
Inhibition of recombinant human N-terminal GST-tagged ERBB4 catalytic domain (708 to 993 residues) expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
|
Homo sapiens
|
3.4
nM
|
|
|
Inhibition of recombinant human GST-tagged JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using tyrosine-6 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
|
Homo sapiens
|
32.0
nM
|
|
|
Inhibition of EGFR phosphorylation in human A431 cells
|
Homo sapiens
|
49.0
nM
|
|
|
Inhibition of recombinant full length human His-tagged BLK cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
|
Homo sapiens
|
0.1
nM
|
|
|
Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using TK1 as substrate incubated for 60 mins by HTRF assay
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of BTK (unknown origin) at 100 nM by ADP-Glo assay relative to control
|
Homo sapiens
|
101.0
%
|
|
|
Inhibition of BTK (unknown origin) by ADP-Glo assay
|
Homo sapiens
|
0.89
nM
|
|
|
Inhibition of EGFR (unknown origin) by ADP-Glo assay
|
Homo sapiens
|
2.5
nM
|
|
|
Inhibition of ITK (unknown origin) by ADP-Glo assay
|
Homo sapiens
|
99.0
nM
|
|
|
Inhibition of BLK (unknown origin) by ADP-Glo assay
|
Homo sapiens
|
1.1
nM
|
|
|
Inhibition of SRC (unknown origin) by ADP-Glo assay
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of BTK (unknown origin) using poly(Glu, Tyr) 4:1 as substrate incubated in presence of [gamma33P]ATP by image analyser
|
Homo sapiens
|
1.0
nM
|
|
|
Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
|
Homo sapiens
|
60.0
nM
|
|
|
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
|
Homo sapiens
|
30.0
nM
|
|
|
Antiproliferative activity against human NCI-H322M cells assessed as cell growth inhibition measured after 48 hrs by SRB assay
|
Homo sapiens
|
100.0
nM
|
|
|
Inhibition of full-length N-terminal GST tagged BTK (2 to 659 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA
|
Homo sapiens
|
0.9
nM
|
|
|
Inhibition of full-length N-terminal GST-tagged BMX (1 to 675 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA
|
Homo sapiens
|
0.4
nM
|
|
|
Inhibition of full-length N-terminal GST-tagged ITK (2 to 620 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA
|
Homo sapiens
|
5.0
nM
|
|
|
Inhibition of N-terminal DYKDDDD-tagged EGFR (669 to 1210 residues) (unknown origin) expressed in Sf21 insect cells using NH2-ETVYSEVRK-biotin as substrate preincubated for 1 hr followed by ATP addition and measured after 2 hrs by ELISA
|
Homo sapiens
|
1.7
nM
|
|
|
Inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA
|
Homo sapiens
|
0.8
nM
|
|
|
Inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA
|
Homo sapiens
|
2.7
nM
|
|
|
Inhibition of GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate incubated for 1 hrs by ELISA
|
Homo sapiens
|
0.9
nM
|
|
|
Inhibition of BTK phosphorylation in human U-937 cells incubated for 4 hrs by Western blot assay
|
Homo sapiens
|
1.7
nM
|
|
|
Inhibition of ITK phosphorylation in human Jurkat cells incubated for 4 hrs by Western blot assay
|
Homo sapiens
|
178.5
nM
|
|
|
Inhibition of EGFR phosphorylation in human A549 cells incubated for 4 hrs by Western blot assay
|
Homo sapiens
|
16.6
nM
|
|
|
Inhibition of wild type BTK (unknown origin) in presence of 1 mM ATP by microplate reader assay
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of BTK C481S mutant (unknown origin) in presence of 1 mM ATP by microplate reader assay
|
Homo sapiens
|
12.9
nM
|
|
|
Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue incubated for 24 hrs by Western blot analysis
|
Homo sapiens
|
1.09
nM
|
|
|
Inhibition of BTK in human Ramos cells assessed as reduction of IgM stimulated PLCgamma2 (Y1217) phosphorylation after 24 hrs by western blot assay
|
Homo sapiens
|
0.99
nM
|
|
|
Inhibition of BTK in human whole blood assessed as activation of anti-IgM-induced CD69 expression by flow cytometry analysis
|
Homo sapiens
|
8.14
nM
|
|
