thiolactomycin (CID 445629) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(19)
 
 
Inactive(119)
 
 
Inconclusive(14)
 
 
Unspecified(50)
 
 
Top Targets:
HELICc(5)
 
 
 
Pyr redox dim(5)
 
 
KAS III(4)
 
 
 
7TM GPCR Srx(4)
 
 
PIKKc TOR(4)
 
 
BioAssay Types:
Confirmatory(125)
 
 
 
 
 
Literature(64)
 
 
 
 
 
Screening(10)
 
 
Summary(1)
 
 
BioActivity Types:
Potency(125)
 
 
 
 
 
IC50(16)
 
 
 
 
Kd(2)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 195    Data Row: 202   Total Pages: 5   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID50106765]
Potency 1qHTS Validation Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) [AID1705, Type: confirmatory]Chain A, Human Ape1 Endonuclease With Bound Abasic Dna And Mn2+ Ion [gi:6980812]
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2
[SID50106765]
Potency 1.9953Confirmation qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) [AID2572, Type: confirmatory]Chain A, Human Ape1 Endonuclease With Bound Abasic Dna And Mn2+ Ion [gi:6980812]
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3
[SID50106765]
Potency 3.1623qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) [AID2517, Type: confirmatory]Chain A, Human Ape1 Endonuclease With Bound Abasic Dna And Mn2+ Ion [gi:6980812]
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4
[SID103551068]
IC50 4Inhibitory activity against KasA from Mycobacterium tuberculosis H37Rv [AID259392, Type: Literature]3-oxoacyl-[acyl-carrier-protein] synthase 3 [gi:61223756]
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5
[SID103551068]
MIC 6Inhibitory activity against Escherichia coli ANSI [AID259386, Type: Literature]
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6
[SID103551068]
IC50 6Inhibitory activity against KasB from Mycobacterium tuberculosis H37Rv [AID259391, Type: Literature]3-oxoacyl-[acyl-carrier-protein] synthase 2 [gi:54040801]
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7
[SID50106765]
Potency 8.9125qHTS Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) [AID2549, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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8
[SID50106765]
Potency 8.9125qHTS Validation Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) [AID2353, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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9
[SID50106765]
Potency 11.2202Counterscreen for RECQ1 Inhibitors: ADP Fluorescence Polarization Displacement Assay [AID2711, Type: confirmatory]
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10
[SID50106765]
Potency 11.2202Counterscreen for BLMA Inhibitors: ADP Fluorescence Polarization Displacement Assay [AID2712, Type: confirmatory]
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11
[SID103551068]
IC50 12Inhibitory activity against FabB from Escherichia coli ANSI [AID259388, Type: Literature]
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12
[SID50106765]
Potency 14.1254qHTS for Inhibitors of Polymerase Eta [AID588591, Type: confirmatory]DNA polymerase eta [Homo sapiens] [gi:5729982]
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13
[SID50106765]
Potency 14.1254qHTS for Inhibitors of Polymerase Eta [AID588591, Type: confirmatory]DNA polymerase eta [Homo sapiens] [gi:5729982]
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14
[SID50106765]
Potency 25.1189qHTS Assay for Inhibitors of DNA Polymerase Beta [AID485314, Type: confirmatory]DNA polymerase beta [Homo sapiens] [gi:4505931]
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15
[SID50106765]
Potency 25.1189qHTS Assay for Inhibitors of DNA Polymerase Beta [AID485314, Type: confirmatory]DNA polymerase beta [Homo sapiens] [gi:4505931]
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16
[SID50106765]
Potency 39.8107Confirmation qHTS Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) [AID2708, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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17
[SID103551068]
IC50 49Antimicrobial activity against Plasmodium falciparum [AID496819, Type: Literature]
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18
[SID50106765]
Potency 50.1187qHTS Validation Assay for Inhibitors for MPP8 Chromodomain Interactions with Methylated Histone Tails [AID488949, Type: confirmatory]MPHOSPH8 gene product [Homo sapiens] [gi:41055989]
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19
[SID103551068]
 Binding affinity to Escherichia coli K12 KAS 3 expressed in Escherichia coli BL21 by STD-NMR spectroscopy [AID393124, Type: Literature]
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20
[SID46391893]
 Experimentally measured binding affinity data derived from PDB [AID1811, Type: Literature]Chain A, The Structure Of Beta-Ketoacyl-[acyl Carrier Protein] Synthase I In Complex With Thiolactom [gi:10120827]
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21
[SID53813060]
 Experimentally measured binding affinity data derived from PDB [AID1811, Type: Literature]Chain A, Beta-Ketoacyl-Acp Synthase I (Kas) From E. Coli With Bound Inhibitor Thiolactomycin [gi:163931073]
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22
[SID103551068]
IC50 20Inhibition of recombinant Plasmodium falciparum falcipain-2 [AID474758, Type: Literature]
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23
[SID103551068]
IC50 20Antiplasmodial activity against Plasmodium falciparum W2 [AID590136, Type: Literature]
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24
[SID103551068]
IC50 50Antimalarial activity against chloroquine-sensitive Plasmodium falciparum W2 by [3H]hypoxanthine uptake [AID345869, Type: Literature]
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25
[SID103551068]
IC50 50Antimalarial activity against chloroquine-resistant Plasmodium falciparum D6 by [3H]hypoxanthine uptake [AID345870, Type: Literature]
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26
[SID103551068]
Kd 55.4Inhibition of Staphylococcus aureus recombinant GST-tagged KAS3 expressed in Escherichia coli (DE3) at 1:10 protein to drug ratio by fluorescence quenching analysis [AID634362, Type: Literature]
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27
[SID103551068]
MIC 62.5Inhibitory activity against Mycobacterium tuberculosis H37Rv [AID259387, Type: Literature]
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28
[SID103551068]
IC50 74.9Inhibitory activity against recombinant Mycobacterium tuberculosis beta-ketoacyl-Acyl Carrier Protein synthase mtFabH condensing enzyme [AID40464, Type: Literature]
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29
[SID103551068]
IC50 75Inhibition of Mycobacterium tuberculosis FabH [AID309336, Type: Literature]3-oxoacyl-[acyl-carrier-protein] synthase 3 [gi:61223756]
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30
[SID103551068]
IC50 87Inhibitory activity against FabH from Mycobacterium tuberculosis H37Rv [AID259390, Type: Literature]3-oxoacyl-[acyl-carrier-protein] synthase 3 [gi:61223756]
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31
[SID103551068]
IC50 100Inhibitory activity against human FAS1 [AID259393, Type: Literature]Fatty acid synthase [gi:269849686]
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32
[SID103551068]
IC50 100Inhibitory activity against human FAS1 [AID259393, Type: Literature]Fatty acid synthase [gi:269849686]
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33
[SID103551068]
IC50 100Inhibitory activity against human FAS1 [AID259393, Type: Literature]Fatty acid synthase [gi:269849686]
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34
[SID103551068]
IC50 100Inhibition of Plasmodium falciparum W2 recombinant falcipain-2 [AID590137, Type: Literature]
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35
[SID103551068]
IC50 100Antimicrobial activity against chloroquine-resistant Plasmodium falciparum W2 [AID474757, Type: Literature]
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36
[SID103551068]
Kd 121Binding affinity to Escherichia coli K12 KAS 3 expressed in Escherichia coli BL21 by fluorescence quenching analysis [AID393125, Type: Literature]3-oxoacyl-[acyl-carrier-protein] synthase 3 [gi:68566320]
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37
[SID103551068]
MIC 128Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay [AID590140, Type: Literature]
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38
[SID103551068]
MIC 128Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3114 after 20 hrs by twofold serial broth dilution method [AID427044, Type: Literature]
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39
[SID103551068]
MIC 128Antibacterial activity against Escherichia coli after 20 hrs by twofold serial broth dilution method [AID427048, Type: Literature]
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40
[SID103551068]
MIC 128Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolates after 20 hrs by twofold serial broth dilution method [AID427050, Type: Literature]
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41
[SID103551068]
MIC 256Antibacterial activity against Enterococcus faecalis KCTC 2011 after 20 hrs by twofold serial broth dilution method [AID427045, Type: Literature]
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42
[SID103551068]
MIC 256Antibacterial activity against Staphylococcus aureus KCTC 1621 after 20 hrs by twofold serial broth dilution method [AID427046, Type: Literature]
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43
[SID103551068]
IC50 330Inhibition of Plasmodium falciparum KAS3 expressed in Escherichia coli assessed as transfer of [1-14C]acetyl-CoA to [1-14C]acetyl-ACP [AID345868, Type: Literature]
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44
[SID103551068]
 Antimicrobial activity against methicillin-resistant Staphylococcus aureus COL after 20 hrs [AID380447, Type: Literature]
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45
[SID103551068]
 Antimicrobial activity against vancomycin-sensitive Enterococcus faecalis CL8516 after 20 hrs [AID380448, Type: Literature]
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46
[SID103551068]
 Antimicrobial activity against vancomycin-resistant Enterococcus faecium CL5791 after 20 hrs [AID380449, Type: Literature]
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47
[SID103551068]
 Antimicrobial activity against wild type Escherichia coli after 20 hrs [AID380450, Type: Literature]
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48
[SID103551068]
 Antimicrobial activity against envA transfected Escherichia coli after 20 hrs [AID380451, Type: Literature]
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49
[SID103551068]
 Antibacterial activity against Staphylococcus aureus Smith by agar dilution method [AID388055, Type: Literature]
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50
[SID103551068]
 Antibacterial activity against Moraxella catarrhalis ATCC 25238 by agar dilution method [AID388056, Type: Literature]
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