Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay
|
Trypanosoma brucei brucei
|
29.0
nM
|
|
Inhibition of human HDAC1
|
Homo sapiens
|
0.03
nM
|
|
Inhibition of human HDAC2
|
Homo sapiens
|
0.06
nM
|
|
Inhibition of human HDAC3
|
Homo sapiens
|
2.1
nM
|
|
Inhibition of human HDAC8
|
Homo sapiens
|
0.5
nM
|
|
Inhibition of human HDAC4
|
Homo sapiens
|
0.3
nM
|
|
Inhibition of human HDAC5
|
Homo sapiens
|
2.1
nM
|
|
Inhibition of human HDAC7
|
Homo sapiens
|
66.6
nM
|
|
Inhibition of human HDAC9
|
Homo sapiens
|
3.8
nM
|
|
Inhibition of human HDAC6
|
Homo sapiens
|
16.9
nM
|
|
Inhibition of human HDAC10
|
Homo sapiens
|
0.05
nM
|
|
Inhibition of human HDAC11
|
Homo sapiens
|
0.07
nM
|
|
Inhibition of full length recombinant human HDAC1 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis
|
Homo sapiens
|
0.11
nM
|
|
Inhibition of full length recombinant human HDAC2 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis
|
Homo sapiens
|
0.33
nM
|
|
Inhibition of full length recombinant human HDAC3/NCOR2 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis
|
Homo sapiens
|
4.86
nM
|
|
Inhibition of full length recombinant human HDAC6 expressed in baculovirus infected Sf9 cells using RHKK-Ac as substrate by fluorescence analysis
|
Homo sapiens
|
76.8
nM
|
|
Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA at 10 uM preincubated for 10 mins followed by substrate addition measured after 10 mins
|
Homo sapiens
|
50.0
%
|
|
Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS at 10 uM preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis
|
Homo sapiens
|
50.0
%
|
|
Inhibition of Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method
|
Schistosoma mansoni
|
303.4
nM
|
|
Inhibition of human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method
|
Homo sapiens
|
64.4
nM
|
|
Binding affinity to human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method
|
Homo sapiens
|
22.7
nM
|
|
Binding affinity to Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method
|
Schistosoma mansoni
|
28.4
nM
|
|
Inhibition of human His-thioredoxin-tagged HDAC8 mL6 mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method
|
Homo sapiens
|
93.0
nM
|
|
Inhibition of human His-thioredoxin-tagged HDAC8 mL1/mL6 mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method
|
Homo sapiens
|
94.0
nM
|
|
Inhibition of human His-thioredoxin-tagged HDAC8 mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method
|
Homo sapiens
|
169.0
nM
|
|
Inhibition of human His-thioredoxin-tagged HDAC8 mL1/mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method
|
Homo sapiens
|
217.0
nM
|
|
Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method
|
Homo sapiens
|
0.48
nM
|
|
Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay
|
Homo sapiens
|
6.5
nM
|
|
Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method
|
Homo sapiens
|
7.3
nM
|
|
Inhibition of human recombinant HDAC2 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method
|
Homo sapiens
|
31.0
nM
|
|
Inhibition of human recombinant HDAC3 using fluorogenic HDAC substrate after 10 mins by spectrophotometric method
|
Homo sapiens
|
4.3
nM
|
|
Inhibition of human recombinant HDAC8 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method
|
Homo sapiens
|
24.0
nM
|
|
Inhibition of human recombinant HDAC4 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method
|
Homo sapiens
|
6.7
nM
|
|
Inhibition of human recombinant HDAC5 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method
|
Homo sapiens
|
4.3
nM
|
|
Inhibition of human recombinant HDAC7 using fluorogenic HDAC substrate class 2a after 45 mins by fluorimetrc method
|
Homo sapiens
|
1.7
nM
|
|
Inhibition of human recombinant HDAC9 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method
|
Homo sapiens
|
5.3
nM
|
|
Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate after 30 mins by fluorimetrc method
|
Homo sapiens
|
350.0
nM
|
|
Inhibition of human recombinant HDAC10 using fluorogenic HDAC substrate after 45 mins by fluorimetrc method
|
Homo sapiens
|
4.4
nM
|
|
Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
|
Homo sapiens
|
0.617
nM
|
|
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
|
Homo sapiens
|
2.16
nM
|
|
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
|
Homo sapiens
|
4.61
nM
|
|
Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
|
Homo sapiens
|
5.95
nM
|
|
Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
|
Homo sapiens
|
4.04
nM
|
|
Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay
|
Homo sapiens
|
6.7
nM
|
|
Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
|
Homo sapiens
|
1.96
nM
|
|
Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay
|
Homo sapiens
|
10.0
nM
|
|
Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay
|
Homo sapiens
|
39.81
nM
|
|
Inhibition of HDAC1 (unknown origin)
|
Homo sapiens
|
4.26
nM
|
|
Inhibition of HDAC2 (unknown origin)
|
Homo sapiens
|
4.26
nM
|
|
Inhibition of recombinant full length human HDAC1 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
|
Homo sapiens
|
0.62
nM
|
|
Inhibition of recombinant full length human HDAC2 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
|
Homo sapiens
|
2.16
nM
|
|
Inhibition of recombinant full length human HDAC4 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
|
Homo sapiens
|
4.61
nM
|
|
Inhibition of recombinant full length human HDAC5 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
|
Homo sapiens
|
5.95
nM
|
|
Inhibition of recombinant full length human HDAC7 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
|
Homo sapiens
|
4.04
nM
|
|
Inhibition of recombinant full length human HDAC9 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
|
Homo sapiens
|
6.7
nM
|
|
Inhibition of recombinant full length human HDAC10 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay
|
Homo sapiens
|
1.96
nM
|
|
Inhibition of human HDAC1 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay
|
Homo sapiens
|
0.1
nM
|
|
Inhibition of human HDAC2 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay
|
Homo sapiens
|
0.3
nM
|
|
Inhibition of human HDAC3/NcoR2 expressed in sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay
|
Homo sapiens
|
5.0
nM
|
|
Inhibition of human HDAC8 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKAcKAc) as substrate by fluorescence-based assay
|
Homo sapiens
|
4.0
nM
|
|
Inhibition of human HDAC4 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay
|
Homo sapiens
|
0.6
nM
|
|
Inhibition of human HDAC5 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay
|
Homo sapiens
|
4.0
nM
|
|
Inhibition of human HDAC7 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay
|
Homo sapiens
|
119.0
nM
|
|
Inhibition of human HDAC9 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay
|
Homo sapiens
|
32.0
nM
|
|
Inhibition of human HDAC6 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay
|
Homo sapiens
|
77.0
nM
|
|
Inhibition of HDAC10 (unknown origin)
|
Homo sapiens
|
0.5
nM
|
|
Inhibition of human HDAC11 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay
|
Homo sapiens
|
0.4
nM
|
|
Inhibition of recombinant full length C-terminal FLAG His-tagged human HDAC1 expressed in baculovirus infected Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorimetry analysis
|
Homo sapiens
|
0.11
nM
|
|
Inhibition of recombinant full length C-terminal GST fusion-tagged human HDAC2 expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorimetry analysis
|
Homo sapiens
|
0.33
nM
|
|
Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells using RHK-K(Ac)-AMCas substrate measured after 60 mins by fluorimetry analysis
|
Homo sapiens
|
4.86
nM
|
|
Inhibition of recombinant full length N-terminal GST fusion-tagged human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHK-K(Ac)-AMC as substrate measured after 90 mins by fluorimetry analysis
|
Homo sapiens
|
76.8
nM
|
|
Antimalarial activity against asexual blood stage quinine-resistant Plasmodium falcipuram C2A assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
|
Plasmodium falciparum
|
2.52
nM
|
|
Antimalarial activity against asexual blood stage wild-type Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
|
Plasmodium falciparum
|
4.01
nM
|
|
Antimalarial activity against asexual blood stage chloroquine-resistant Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
|
Plasmodium falciparum
|
7.09
nM
|
|
Cytotoxicity against human HepG2 cells incubated for 72 hrs by CCK-8 assay
|
Homo sapiens
|
30.0
nM
|
|
Cytotoxicity against HEK293T cells incubated for 72 hrs by CCK-8 assay
|
Homo sapiens
|
60.0
nM
|
|
Antimalarial activity against asexual blood stage chloroquine-resistant Plasmodium falcipuram GB4 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
|
Plasmodium falciparum
|
1.75
nM
|
|
Antimalarial activity against asexual blood stage sulfadoxine-pyrimethamine/mefloquine-resistant Plasmodium falcipuram CP286 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
|
Plasmodium falciparum
|
2.04
nM
|
|
In vivo inhibition of C-terminal glmS fused HDAC1 in Plasmodium falcipuram 3D7 assessed as inhibition of parasite growth incubated for 4 hrs followed by compound washout and replacement with fresh medium with compounds measured after 68 hrs by SYBR Green I staining based fluorescence analysis
|
Plasmodium falciparum
|
5.59
nM
|
|
In vivo inhibition of C-terminal TY1 fused HDAC1 in Plasmodium falcipuram 3D7 assessed as inhibition of parasite growth incubated for 4 hrs followed by compound washout and replacement with fresh medium with compounds measured after 68 hrs by SYBR Green I staining based fluorescence analysis
|
Plasmodium falciparum
|
19.15
nM
|
|
Inhibition of recombinant human full length C-terminal His tagged HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 insect cells using Ac-peptide as substrate incubated for 4 hrs
|
Homo sapiens
|
1.1
nM
|
|
Inhibition of recombinant human full length C-terminal His/FLAG tagged HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs
|
Homo sapiens
|
0.46
nM
|
|
Inhibition of human C-terminal His tagged HDAC3 (1 to 428 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs
|
Homo sapiens
|
2.1
nM
|
|
Inhibition of recombinant human full length N-terminal GST tagged HDAC6 (1 to 1215 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs
|
Homo sapiens
|
34.9
nM
|
|
Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus-infected Sf9 insect cells using Ac-peptide as substrate incubated for 4 hrs followed by trypsin addition and further incubated for 2 hrs
|
Homo sapiens
|
9.2
nM
|
|