Trade Names
Synonyms
Status
Molecule Category UNKNOWN
UNII 1X70OSD4VX
EPA CompTox DTXSID60893450

Structure

InChI Key XYFPWWZEPKGCCK-GOSISDBHSA-N
Smiles C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1
InChI
InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1

Physicochemical Descriptors

Property Name Value
Molecular Formula C25H24N6O2
Molecular Weight 440.51
AlogP 4.22
Hydrogen Bond Acceptor 7.0
Hydrogen Bond Donor 1.0
Number of Rotational Bond 5.0
Polar Surface Area 99.16
Molecular species NEUTRAL
Aromatic Rings 4.0
Heavy Atoms 33.0

Bioactivity

Mechanism of Action Action Reference
Tyrosine-protein kinase BTK inhibitor INHIBITOR FDA
Protein: Tyrosine-protein kinase BTK

Description: Tyrosine-protein kinase BTK

Organism : Homo sapiens

Q06187 ENSG00000010671
Targets EC50(nM) IC50(nM) Kd(nM) Ki(nM) Inhibition(%)
Adhesion
- 120 - - -
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2B Cytochrome P450 2B6
- 11100 - - -
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2C Cytochrome P450 2C19
- 19000-33500 - - -
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2C Cytochrome P450 2C8
- 7900 - - -
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2C Cytochrome P450 2C9
- 8500-9690 - - -
Enzyme Cytochrome P450 Cytochrome P450 family 3 Cytochrome P450 family 3A Cytochrome P450 3A4
- 11000-40800 - - -
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase Alk family
- - - - 81
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase Csk family
- 2 - - -
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase EGFR family
49 1-390 1 - 89
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase JakA family
- 10-146 37 - 80
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase JakB family
- 10-146 37 - 80
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase PDGFR family
- 5545 - - -
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase Ret family
- 5-37 - - -
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase Src family
- 0-1 - - 102
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase Tec family
- 0-10350 2 5-425 99-101
Ion channel Voltage-gated ion channel Potassium channels Voltage-gated potassium channel
- 1100-7700 - 1100 1
Membrane receptor
- 120 - - -
Transcription factor Nuclear receptor Nuclear hormone receptor subfamily 4 Nuclear hormone receptor subfamily 4 group A Nuclear hormone receptor subfamily 4 group A member 3
- 78 - - -
Unclassified protein
- 900 - - -
Assay Description Organism Bioactivity Reference
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

Related Entries

Cross References

Resources Reference
ChEBI 76612
ChEMBL CHEMBL1873475
DrugBank DB09053
DrugCentral 4810
FDA SRS 1X70OSD4VX
Guide to Pharmacology 6912
KEGG D10223
PDB 1E8
PharmGKB PA166121346
PubChem 24821094
SureChEMBL SCHEMBL201859
ZINC ZINC000035328014