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N-alpha-(2-carboxyl)benzoyl-N5-(2-fluoro-1-iminoethyl)ornithine amide (CID 54756938) - Compound BioActivity Data
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BioActivity Outcomes:
Active(21)
 
 
Inactive(4)
 
 
Inconclusive(3)
 
 
Unspecified(34)
 
 
Top Targets:
PAD(2)
 
 
BioAssay Types:
Literature(62)
 
 
 
 
 
BioActivity Types:
IC50(8)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 62    Data Row: 62   Total Pages: 2   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID136930637]
IC50 0.4Irreversible inhibition of PAD4 Q346A mutant assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins [AID627438, Type: Literature]
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2
[SID136930637]
IC50 1.1Irreversible inhibition of PAD4 Q346E mutant assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins [AID627437, Type: Literature]
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3
[SID136930637]
IC50 1.4Irreversible inhibition of PAD1 assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins by fluorometric analysis [AID627372, Type: Literature]
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4
[SID136930637]
IC50 1.9Irreversible inhibition of PAD4 assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins by fluorometric analysis [AID627371, Type: Literature]
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5
[SID136930637]
IC50 4.6Irreversible inhibition of PAD4 R374K mutant assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins [AID627439, Type: Literature]
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6
[SID136930637]
IC50 32Irreversible inhibition of PAD4 R374A mutant assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins [AID627440, Type: Literature]
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7
[SID136930637]
IC50 34Irreversible inhibition of PAD3 assessed as hydrolysis of benzoyl-L-arginine ethyl ester preincubated for 15 mins measured after 15 mins by fluorometric analysis [AID627374, Type: Literature]
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8
[SID136930637]
Irreversible inhibition of PAD1 assessed as residual activity at 1 mM measured after 20 hrs by colorimetric assay [AID627375, Type: Literature]
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9
[SID136930637]
Irreversible inhibition of PAD2 assessed as residual activity at 1 mM measured after 20 hrs by colorimetric assay [AID627426, Type: Literature]
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10
[SID136930637]
Irreversible inhibition of PAD3 assessed as residual activity at 1 mM measured after 20 hrs by colorimetric assay [AID627427, Type: Literature]
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11
[SID136930637]
Irreversible inhibition of PAD4 assessed as residual activity at 1 mM measured after 20 hrs by colorimetric assay [AID627428, Type: Literature]
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12
[SID136930637]
Induction of human HL60 cell differentiation assessed as increase in PAD4 expression level at 10 uM after 6 hrs by Western blotting [AID627446, Type: Literature]
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13
[SID136930637]
Induction of human HL60 cell differentiation assessed as increase in PAD4 expression level at 1 uM after 12 hrs by Western blotting [AID627447, Type: Literature]
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14
[SID136930637]
Induction of human HL60 cell differentiation assessed as increase in PAD4 expression level at 1 uM after 24 hrs by Western blotting [AID627448, Type: Literature]
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15
[SID136930637]
Inhibition of PAD4 in calcium ionophore A23187 stimulated-human HL60 granulocytes assessed as reduction in deaminated histone H3 at 1 uM after 30 mins by Western blotting [AID627442, Type: Literature]Protein-arginine deiminase type-4 [gi:296439260]
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16
[SID136930637]
Inhibition of PAD4 in calcium ionophore A23187 stimulated-human HL60 granulocytes assessed as reduction in deaminated histone H3 at 100 uM after 48 hrs by Western blotting [AID627443, Type: Literature]Protein-arginine deiminase type-4 [gi:296439260]
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17
[SID136930637]
Irreversible inhibition of PAD1 assessed as citrulline formation at 1 mM measured after 20 hrs by colorimetric assay in presence of 2 mM benzoyl-L-arginine ethyl ester [AID626681, Type: Literature]
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18
[SID136930637]
Irreversible inhibition of PAD2 assessed as residual activity at 1 mM measured after 20 hrs by colorimetric assay in presence of 2 mM benzoyl-L-arginine ethyl ester [AID626722, Type: Literature]
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19
[SID136930637]
Irreversible inhibition of PAD3 assessed as residual activity at 1 mM measured after 20 hrs by colorimetric assay in presence of 2 mM benzoyl-L-arginine ethyl ester [AID626723, Type: Literature]
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20
[SID136930637]
Irreversible inhibition of PAD4 assessed as residual activity at 1 mM measured after 20 hrs by colorimetric assay in presence of 2 mM benzoyl-L-arginine ethyl ester [AID626724, Type: Literature]
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21
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as induction of PARP cleavage at 50 ug/ml measured up to 8 hrs by Western blotting [AID626671, Type: Literature]
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22
[SID136930637]
Induction of human HL60 cell differentiation assessed as increase in PAD4 expression level after 24 hrs by Western blotting [AID626672, Type: Literature]
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23
[SID136930637]
Induction of human HL60 cell differentiation assessed as increase in PAD4 expression level at 1 to 10 uM by Western blotting [AID626673, Type: Literature]
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24
[SID136930637]
Selectivity ratio of IC50 for PAD4 R374K mutant to IC50 for wild type PAD4 [AID626675, Type: Literature]
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25
[SID136930637]
Selectivity ratio of IC50 for PAD4 R374A mutant to IC50 for wild type PAD4 [AID626676, Type: Literature]
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26
[SID136930637]
Ratio of Kcat to Km for PAD4 Q346A mutant [AID626677, Type: Literature]
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27
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as late apoptotic cells at 50 ug/ml after 4 hrs by annexin V/propidium iodide staining method relative to control [AID626665, Type: Literature]
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28
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as necrotic cells at 50 ug/ml after 4 hrs by annexin V/propidium iodide staining method relative to control [AID626666, Type: Literature]
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29
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as viable cells at 50 ug/ml after 8 hrs by annexin V/propidium iodide staining method relative to control [AID626667, Type: Literature]
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30
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as early apoptotic cells at 50 ug/ml after 8 hrs by annexin V/propidium iodide staining method relative to control [AID626668, Type: Literature]
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31
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as late apoptotic cells at 50 ug/ml after 8 hrs by annexin V/propidium iodide staining method relative to control [AID626669, Type: Literature]
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32
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as necrotic cells at 50 ug/ml after 8 hrs by annexin V/propidium iodide staining method relative to control relative to control [AID626670, Type: Literature]
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33
[SID136930637]
Selectivity ratio of PAD1 over PAD2 [AID626729, Type: Literature]
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34
[SID136930637]
Selectivity ratio of PAD1 over PAD3 [AID626730, Type: Literature]
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35
[SID136930637]
Ratio of Kcat to Km for PAD4 R347K mutant [AID626678, Type: Literature]
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36
[SID136930637]
Ratio of Kcat to Km for PAD4 R347A mutant [AID626679, Type: Literature]
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37
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as viable cells at 50 ug/ml after 2 hrs by annexin V/propidium iodide staining method relative to control [AID626659, Type: Literature]
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38
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as early apoptotic cells at 50 ug/ml after 2 hrs by annexin V/propidium iodide staining method relative to control [AID626660, Type: Literature]
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39
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as late apoptotic cells at 50 ug/ml after 2 hrs by annexin V/propidium iodide staining method relative to control [AID626661, Type: Literature]
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40
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as necrotic cells at 50 ug/ml after 2 hrs by annexin V/propidium iodide staining method relative to control [AID626662, Type: Literature]
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41
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as viable cells at 50 ug/ml after 4 hrs by annexin V/propidium iodide staining method relative to control [AID626663, Type: Literature]
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42
[SID136930637]
Induction of apoptosis in human TK6 cells assessed as early apoptotic cells at 50 ug/ml after 4 hrs by annexin V/propidium iodide staining method relative to control [AID626664, Type: Literature]
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43
[SID136930637]
Ratio of Kinact to Ki for PAD2 [AID627434, Type: Literature]
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44
[SID136930637]
Ratio of Kinact to Ki for PAD3 [AID627435, Type: Literature]
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45
[SID136930637]
Ratio of Kinact to Ki for PAD4 [AID627436, Type: Literature]
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46
[SID136930637]
Irreversible inhibition of PAD1 assessed as residual activity measured after 20 hrs by colorimetric assay [AID627429, Type: Literature]
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47
[SID136930637]
Selectivity ratio of PAD1 over PAD4 [AID626731, Type: Literature]
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48
[SID136930637]
Ratio of Kinact to Ki for F-amidine to compound for PAD1 [AID626732, Type: Literature]
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49
[SID136930637]
Ratio of Kinact to Ki for F-amidine to compound for PAD2 [AID626733, Type: Literature]
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50
[SID136930637]
Ratio of Kinact to Ki for F-amidine to compound for PAD3 [AID626734, Type: Literature]
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