Binding constant for EGFR kinase domain
|
Homo sapiens
|
15.0
nM
|
|
Binding constant for KIT(V559D) kinase domain
|
Homo sapiens
|
3.2
nM
|
|
Binding constant for full-length TNNI3K
|
Homo sapiens
|
220.0
nM
|
|
Binding constant for CSF1R kinase domain
|
Homo sapiens
|
5.6
nM
|
|
Binding constant for RET(M918T) kinase domain
|
Homo sapiens
|
20.0
nM
|
|
Binding constant for VEGFR2 kinase domain
|
Homo sapiens
|
26.0
nM
|
|
Binding constant for DDR1 kinase domain
|
Homo sapiens
|
260.0
nM
|
|
Binding constant for KIT kinase domain
|
Homo sapiens
|
3.7
nM
|
|
Binding constant for KIT(D816V) kinase domain
|
Homo sapiens
|
410.0
nM
|
|
Binding constant for FLT1 kinase domain
|
Homo sapiens
|
12.0
nM
|
|
Binding constant for RET kinase domain
|
Homo sapiens
|
14.0
nM
|
|
Binding constant for CIT kinase domain
|
Homo sapiens
|
300.0
nM
|
|
Binding constant for RAF1 kinase domain
|
Homo sapiens
|
880.0
nM
|
|
Binding constant for KIT(V559D,T670I) kinase domain
|
Homo sapiens
|
13.0
nM
|
|
Binding constant for LCK kinase domain
|
Homo sapiens
|
360.0
nM
|
|
Binding constant for FLT3 kinase domain
|
Homo sapiens
|
71.0
nM
|
|
Binding constant for KIT(V559D,V654A) kinase domain
|
Homo sapiens
|
23.0
nM
|
|
Binding constant for LYN kinase domain
|
Homo sapiens
|
160.0
nM
|
|
Binding constant for PDGFRA kinase domain
|
Homo sapiens
|
10.0
nM
|
|
Binding constant for BRAF kinase domain
|
Homo sapiens
|
630.0
nM
|
|
Binding constant for BRAF(V600E) kinase domain
|
Homo sapiens
|
280.0
nM
|
|
Binding constant for PDGFRB kinase domain
|
Homo sapiens
|
9.1
nM
|
|
Binding constant for ZAK kinase domain
|
Homo sapiens
|
8.0
nM
|
|
Binding constant for EPHA6 kinase domain
|
Homo sapiens
|
490.0
nM
|
|
Binding constant for FLT4 kinase domain
|
Homo sapiens
|
9.7
nM
|
|
Binding constant for FRK kinase domain
|
Homo sapiens
|
99.0
nM
|
|
Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assay
|
None
|
3.0
nM
|
|
Binding affinity to human KIT incubated for 1 hr by kinase binding assay
|
Homo sapiens
|
3.7
nM
|
|
Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay
|
Homo sapiens
|
410.0
nM
|
|
Binding constant for EPHA6 kinase domain
|
None
|
490.0
nM
|
|
Binding constant for ZAK kinase domain
|
None
|
8.0
nM
|
|
Binding constant for KIT kinase domain
|
None
|
3.7
nM
|
|
Binding constant for KIT(A829P) kinase domain
|
None
|
15.0
nM
|
|
Binding constant for KIT(D816H) kinase domain
|
None
|
180.0
nM
|
|
Binding constant for KIT(D816V) kinase domain
|
None
|
410.0
nM
|
|
Binding constant for KIT(L576P) kinase domain
|
None
|
1.3
nM
|
|
Binding constant for KIT(V559D) kinase domain
|
None
|
3.2
nM
|
|
Binding constant for KIT(V559D,T670I) kinase domain
|
None
|
13.0
nM
|
|
Binding constant for KIT(V559D,V654A) kinase domain
|
None
|
23.0
nM
|
|
Binding constant for DDR1 kinase domain
|
None
|
260.0
nM
|
|
Binding constant for FLT1 kinase domain
|
None
|
12.0
nM
|
|
Binding constant for FLT4 kinase domain
|
None
|
9.7
nM
|
|
Binding constant for FRK kinase domain
|
None
|
99.0
nM
|
|
Binding constant for VEGFR2 kinase domain
|
None
|
26.0
nM
|
|
Binding constant for LYN kinase domain
|
None
|
160.0
nM
|
|
Binding constant for PDGFRB kinase domain
|
None
|
9.1
nM
|
|
Binding constant for RAF1 kinase domain
|
None
|
880.0
nM
|
|
Binding constant for FLT3 kinase domain
|
None
|
71.0
nM
|
|
Binding constant for FLT3(K663Q) kinase domain
|
None
|
54.0
nM
|
|
Binding constant for BRAF kinase domain
|
None
|
630.0
nM
|
|
Binding constant for BRAF(V600E) kinase domain
|
None
|
280.0
nM
|
|
Binding constant for ABL1(F317L)-non phosphorylated kinase domain
|
None
|
910.0
nM
|
|
Binding constant for ABL1(Q252H)-non phosphorylated kinase domain
|
None
|
670.0
nM
|
|
Binding constant for ABL1-non phosphorylated kinase domain
|
None
|
680.0
nM
|
|
Binding constant for CSF1R kinase domain
|
None
|
5.6
nM
|
|
Binding constant for EGFR(L747-E749del, A750P) kinase domain
|
None
|
960.0
nM
|
|
Binding constant for LCK kinase domain
|
None
|
360.0
nM
|
|
Binding constant for PDGFRA kinase domain
|
None
|
10.0
nM
|
|
Binding constant for CIT kinase domain
|
None
|
300.0
nM
|
|
Binding constant for TNNI3K kinase domain
|
None
|
220.0
nM
|
|
Binding constant for RET kinase domain
|
None
|
14.0
nM
|
|
Binding constant for RET(M918T) kinase domain
|
None
|
20.0
nM
|
|
Binding constant for YSK4 kinase domain
|
None
|
200.0
nM
|
|
Inhibition of VEGFR3
|
None
|
6.0
nM
|
|
Inhibition of VEGFR2
|
None
|
3.0
nM
|
|
Inhibition of VEGFR1
|
None
|
2.0
nM
|
|
SANGER: Inhibition of human NCI-H1648 cell growth in a cell viability assay.
|
Homo sapiens
|
685.64
nM
|
|
SANGER: Inhibition of human SK-N-DZ cell growth in a cell viability assay.
|
Homo sapiens
|
549.04
nM
|
|
SANGER: Inhibition of human A204 cell growth in a cell viability assay.
|
Homo sapiens
|
518.54
nM
|
|
SANGER: Inhibition of human CGTH-W-1 cell growth in a cell viability assay.
|
Homo sapiens
|
669.97
nM
|
|
SANGER: Inhibition of human DU-145 cell growth in a cell viability assay.
|
Homo sapiens
|
469.35
nM
|
|
SANGER: Inhibition of human EoL-1-cell cell growth in a cell viability assay.
|
Homo sapiens
|
0.9439
nM
|
|
Inhibition of RET (unknown origin)
|
Homo sapiens
|
90.0
nM
|
|
Inhibition of wild type RET (unknown origin) by cellular phosphorylation assay
|
Homo sapiens
|
66.0
nM
|
|
Inhibition of VEGFR1 (unknown origin)
|
Homo sapiens
|
2.0
nM
|
|
Inhibition of VEGFR2 (unknown origin)
|
Homo sapiens
|
3.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
3.0
nM
|
|
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
|
Homo sapiens
|
1.0
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
|
81.0
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
|
117.0
nM
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
10.17
%
|
|
Binding affinity to FRK (unknown origin)
|
Homo sapiens
|
99.0
nM
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
19.26
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
14.48
%
|
|
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
|
-0.04
%
|
|
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
|
-0.03
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.04
%
|
|
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
|
-0.03
%
|
|
Inhibition of VEGFR2 (unknown origin)
|
Homo sapiens
|
3.0
nM
|
|
Inhibition of VEGFR3 (unknown origin)
|
Homo sapiens
|
6.0
nM
|
|
Inhibition of VEGFR1 (unknown origin)
|
Homo sapiens
|
2.0
nM
|
|