Inhibition of Proto-oncogene tyrosine-protein kinase Kit
|
None
|
730.0
nM
|
|
Inhibition of vascular endothelial growth factor receptor 1
|
None
|
77.0
nM
|
|
Inhibition of Vascular endothelial growth factor receptor 2
|
None
|
37.0
nM
|
|
In vitro inhibition of KDR
|
None
|
63.0
nM
|
|
Inhibition of human Vascular endothelial growth factor receptor 2
|
Homo sapiens
|
160.0
nM
|
|
Inhibition of VEGF-induced proliferation of human umbilical vein endothelial cells
|
Homo sapiens
|
100.0
nM
|
|
Average Binding Constant for FLT4; NA=Not Active at 10 uM
|
Homo sapiens
|
190.0
nM
|
|
Average Binding Constant for VEGFR2; NA=Not Active at 10 uM
|
Homo sapiens
|
70.0
nM
|
|
Average Binding Constant for KIT; NA=Not Active at 10 uM
|
Homo sapiens
|
700.0
nM
|
|
Average Binding Constant for PDGFRB; NA=Not Active at 10 uM
|
Homo sapiens
|
58.0
nM
|
|
Inhibition of poly(Glu4-Tyr)peptide phosphorylation by recombinant VEGFR2 at 10 uM ATP
|
Homo sapiens
|
138.0
nM
|
|
Inhibitory activity against VEGF stimulated autophosphorylation of VEGFR2 expressed in KDR15 cells
|
Homo sapiens
|
15.0
nM
|
|
Inhibitory activity against VEGFR2 by HTRF assay
|
Homo sapiens
|
54.0
nM
|
|
Inhibitory activity against VEGFR1 by HTRF assay
|
Homo sapiens
|
140.0
nM
|
|
Inhibitory activity against VEGFR2 transiently transfected in 293 adenovirus transfected kidney cells by ELISA
|
Homo sapiens
|
21.0
nM
|
|
Inhibitory activity against VEGFR-2 using 2 uM ATP by HTRF assay
|
Homo sapiens
|
54.0
nM
|
|
Inhibitory activity against VEGFR-1 using 2 uM ATP by HTRF assay
|
Homo sapiens
|
140.0
nM
|
|
Inhibition of VEGFR2 by enzymatic assay
|
Homo sapiens
|
54.0
nM
|
|
Inhibition of VEGFR1 by enzymatic assay
|
Homo sapiens
|
140.0
nM
|
|
Inhibition of VEGFR2 in 293 adenovirus transfected kidney cells by cell-based ELISA assay
|
Homo sapiens
|
21.0
nM
|
|
Inhibition of VEGFR2 phosphorylation in presence of 2 uM ATP by HTRF assay
|
Homo sapiens
|
54.0
nM
|
|
Inhibition of VEGFR1 phosphorylation in presence of 2 uM ATP by HTRF assay
|
Homo sapiens
|
140.0
nM
|
|
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
|
Homo sapiens
|
21.0
nM
|
|
Inhibition of human EGFR in presence of 1 uM ATP
|
Homo sapiens
|
457.7
nM
|
|
Inhibition of human EGFR in presence of 1 mM ATP at <10000 nM
|
Homo sapiens
|
46.0
%
|
|
Inhibition of human VEGFR2 in presence of 1 uM ATP
|
Homo sapiens
|
198.3
nM
|
|
Inhibition of VEGFR1 by HTRF assay
|
None
|
54.0
nM
|
|
Inhibition of VEGFR2 by HTRF assay
|
None
|
140.0
nM
|
|
Inhibition of VEGFR2 by cell-based assay
|
None
|
21.0
nM
|
|
Inhibition of VEGFR2 assessed as blockade of pGAT-biotin phosphorylation in presence of 2 uM ATP by HTRF assay
|
None
|
54.0
nM
|
|
Inhibition of VEGFR1 assessed as blockade of pGAT-biotin phosphorylation in presence of 2 uM ATP by HTRF assay
|
None
|
140.0
nM
|
|
Inhibition of VEGFR2 assessed as blockade of pGAT-biotin phosphorylation in presence of 8 uM ATP by HTRF assay
|
None
|
42.0
nM
|
|
Inhibition of VEGFR1 assessed as blockade of pGAT-biotin phosphorylation in presence of 8 uM ATP by HTRF assay
|
None
|
110.0
nM
|
|
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
|
None
|
21.0
nM
|
|
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
|
None
|
16.0
nM
|
|
Inhibition of VEGF-induced phosphorylation of VEGFR2 by cell-based ELISA in presence of 8 uM ATP
|
None
|
16.0
nM
|
|
Inhibition of VEGFR2 by HTRF assay in presence of 2 uM ATP
|
None
|
54.0
nM
|
|
Inhibition of VEGFR2 by HTRF assay in presence of 8 uM ATP
|
None
|
42.0
nM
|
|
Inhibition of VEGFR1 by HTRF assay
|
None
|
140.0
nM
|
|
Inhibition of VEGFR1 by HTRF assay in presence of 8 uM ATP
|
None
|
110.0
nM
|
|
Inhibition of VEGF-induced phosphorylation of VEGFR2 by cell-based ELISA
|
None
|
21.0
nM
|
|
Binding constant for KIT(V559D) kinase domain
|
Homo sapiens
|
17.0
nM
|
|
Binding constant for CSF1R kinase domain
|
Homo sapiens
|
18.0
nM
|
|
Binding constant for VEGFR2 kinase domain
|
Homo sapiens
|
62.0
nM
|
|
Binding constant for DDR1 kinase domain
|
Homo sapiens
|
270.0
nM
|
|
Binding constant for KIT kinase domain
|
Homo sapiens
|
5.1
nM
|
|
Binding constant for FLT1 kinase domain
|
Homo sapiens
|
9.6
nM
|
|
Binding constant for KIT(V559D,V654A) kinase domain
|
Homo sapiens
|
210.0
nM
|
|
Binding constant for PDGFRA kinase domain
|
Homo sapiens
|
96.0
nM
|
|
Binding constant for PDGFRB kinase domain
|
Homo sapiens
|
25.0
nM
|
|
Binding constant for FLT4 kinase domain
|
Homo sapiens
|
330.0
nM
|
|
Inhibition of VEGFR2
|
None
|
42.0
nM
|
|
Inhibition of PDGFRbeta
|
None
|
490.0
nM
|
|
Inhibition of VEGF-induced HUVEC proliferation treated 1 hr before VEGF challenge measured 3 days by WST-8 assay
|
Homo sapiens
|
33.0
nM
|
|
Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assay
|
None
|
37.0
nM
|
|
Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation after 3 days by WST-8 assay
|
Homo sapiens
|
33.0
nM
|
|
Antiinflammatory activity in Lewis rat adjuvant arthritis model assessed as inhibition of paw edema at 10 mg/kg, po qd for 20 days relative to control
|
Rattus norvegicus
|
23.0
%
|
|
Binding affinity to human KIT incubated for 1 hr by kinase binding assay
|
Homo sapiens
|
5.1
nM
|
|
Binding constant for KIT kinase domain
|
None
|
5.1
nM
|
|
Binding constant for KIT(L576P) kinase domain
|
None
|
110.0
nM
|
|
Binding constant for KIT(V559D) kinase domain
|
None
|
17.0
nM
|
|
Binding constant for KIT(V559D,V654A) kinase domain
|
None
|
210.0
nM
|
|
Binding constant for DDR1 kinase domain
|
None
|
270.0
nM
|
|
Binding constant for FLT1 kinase domain
|
None
|
9.6
nM
|
|
Binding constant for FLT4 kinase domain
|
None
|
330.0
nM
|
|
Binding constant for VEGFR2 kinase domain
|
None
|
62.0
nM
|
|
Binding constant for PDGFRB kinase domain
|
None
|
25.0
nM
|
|
Binding constant for CSF1R kinase domain
|
None
|
45.0
nM
|
|
Binding constant for PDGFRA kinase domain
|
None
|
96.0
nM
|
|
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: FRK
|
None
|
316.23
nM
|
|
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: KIT
|
None
|
39.81
nM
|
|
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PDGFRB
|
None
|
79.43
nM
|
|
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: KDR
|
None
|
12.59
nM
|
|
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: FLT4
|
None
|
316.23
nM
|
|
PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: FLT1
|
None
|
158.49
nM
|
|
Inhibition of VEGFR3
|
None
|
195.0
nM
|
|
Inhibition of VEGFR2
|
None
|
43.0
nM
|
|
Inhibition of VEGFR1
|
None
|
110.0
nM
|
|
Antiangiogenic activity against wild AB-type transgenic zebrafish embryo expressing green fluorescent protein-labeled VEGFR2 assessed as inhibition of growth of intersegmental vessels treated at 24 hrs post fertilization measured after 48 hrs by alkaline phosphatase staining
|
Danio rerio
|
230.0
nM
|
|
Inhibition of KDR (unknown origin)
|
Homo sapiens
|
10.0
nM
|
|
Inhibition of VEGFR1 (unknown origin)
|
Homo sapiens
|
380.0
nM
|
|
Inhibition of VEGFR2 (unknown origin)
|
Homo sapiens
|
20.0
nM
|
|
PubChem BioAssay. VEGF stimulated ADSC/ECFC co-culture CD31-stained tube area decrease-IC50. (Class of assay: confirmatory)
|
None
|
110.9
nM
|
|
Inhibition of VGFR-2 (unknown origin) using poly-GluTyr (4:1) as substrate after 5 mins by Alpha Screen assay
|
Homo sapiens
|
180.0
nM
|
|
Inhibition of VGFR-2 (unknown origin)
|
Homo sapiens
|
43.0
nM
|
|
Inhibition of VEGFR-2 (unknown origin)
|
Homo sapiens
|
43.0
nM
|
|
Inhibition of human KDR using phosphatidylinositol 4,5-diphosphate as substrate at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
58.0
%
|
|
Inhibition of human EGFR using poly[Glu:Tyr] (4:1) as substrate at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
67.0
%
|
|
Inhibition of human FGFR1 using myelin basic protein as substrate at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
31.0
%
|
|
Inhibition of human Abl1 using myelin basic protein as substrate at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
25.0
%
|
|
Inhibition of human Src using myelin basic protein as substrate at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
16.0
%
|
|
Inhibition of human PDGFR-beta at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
72.0
%
|
|
Inhibition of human mTOR using PHAS-1 as substrate at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
49.0
%
|
|
Inhibition of human PI3K using phosphatidylinositol 4,5-diphosphate as substrate at 1 uM measured after 20 mins at 30 degC by liquid scintillation counting method in presence of [gamma-32P]-ATP
|
Homo sapiens
|
18.0
%
|
|
Inhibition of VEGFR1 (unknown origin)
|
Homo sapiens
|
100.0
nM
|
|
Inhibition of VEGFR2 (unknown origin)
|
Homo sapiens
|
100.0
nM
|
|