4-hydroxy-1-methyl-3-(5-oxo-2,5-dihydro-1H-pyrazol-3-yl)-2(1H)-quinolinone (CID 54687581) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(10)
 
 
Inactive(557)
 
 
Inconclusive(8)
 
 
Unspecified(1)
 
 
Top Targets:
7TM GPCR Srx(19)
 
 
alkPPc(10)
 
 
Bcl-2 like(10)
 
 
7TM GPCR Srsx(8)
 
 
Tryp SPc(6)
 
 
BioAssay Types:
Screening(388)
 
 
 
 
Confirmatory(173)
 
 
 
 
 
Literature(5)
 
 
BioActivity Types:
Potency(125)
 
 
 
 
 
IC50(31)
 
 
EC50(12)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 576    Data Row: 576   Total Pages: 12   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID24824580]
Potency 17.7828qHTS Assay for Inhibitors of Human Jumonji Domain Containing 2E (JMJD2E) [AID2147, Type: confirmatory]Chain A, Crystal Structure Of The Human 2-Oxoglutarate Oxygenase Loc390245 [gi:221046486]
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2
[SID24824580]
EC50 23.257Fluorescent Polarization Homogeneous Dose Response HTS to Indentify Inhibitors of Mex-5 Binding to TCR-2 [AID1960, Type: confirmatory]Zinc finger protein mex- [gi:55976631]
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3
[SID24824580]
EC50 23.257Fluorescent Polarization Homogeneous Dose Response HTS to Indentify Inhibitors of Mex-5 Binding to TCR-2 [AID1960, Type: confirmatory]Zinc finger protein mex- [gi:55976631]
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4
[SID24824580]
Potency 35.4813qHTS Assay for Inhibitors of JMJD2A-Tudor Domain [AID504339, Type: confirmatory]Chain A, Jmjd2a Tandem Tudor Domains In Complex With A Trimethylated Histone H4-K20 Peptide [gi:162330054]
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5
[SID24824580]
Potency 56.2341qHTS Assay for Inhibitors of BAZ2B [AID504333, Type: confirmatory]bromodomain adjacent to zinc finger domain 2B [Homo sapiens] [gi:6683500]
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6
[SID24824580]
 Luminescence-based cell-based primary high throughput screening assay to identify activators of the DAF-12 from the parasite H. contortus (hcDAF-12) [AID652067, Type: screening]Protein DAF-12, isoform a [Caenorhabditis elegans] [gi:71987181]
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7
[SID24824580]
 In vivo-based yeast HTS to detect compounds rescuing yeast growth/survival of Plasmodium Falciparum HSP40-mediated toxicity Measured in Whole Organism System Using Plate Reader - 2120-01_Inhibitor_SinglePoint_HTS_Activity [AID504582, Type: screening]HSP40, subfamily A, putative [Plasmodium falciparum 3D7] [gi:124809271]
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8
[SID24824580]
 MLPCN maternal gene expression-MEX-5 TCR-2 binding assay-Primary Screen [AID1832, Type: screening]Zinc finger protein mex- [gi:55976631]
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9
[SID24824580]
 MLPCN maternal gene expression-MEX-5 TCR-2 binding assay-Primary Screen [AID1832, Type: screening]Zinc finger protein mex- [gi:55976631]
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10
[SID24824580]
 Confirmatory screen for compounds that protect hERG from block by proarrhythmic agents [AID1835, Type: screening]putative potassium channel subunit [Homo sapiens] [gi:487738]
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11
[SID24824580]
 Confirmatory screen for compounds that protect hERG from block by proarrhythmic agents [AID1835, Type: screening]putative potassium channel subunit [Homo sapiens] [gi:487738]
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12
[SID24824580]
 Confirmatory screen for compounds that protect hERG from block by proarrhythmic agents [AID1835, Type: screening]putative potassium channel subunit [Homo sapiens] [gi:487738]
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13
[SID24824580]
 Confirmatory screen for compounds that protect hERG from block by proarrhythmic agents [AID1835, Type: screening]putative potassium channel subunit [Homo sapiens] [gi:487738]
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14
[SID24824580]
 Confirmatory screen for compounds that protect hERG from block by proarrhythmic agents [AID1835, Type: screening]putative potassium channel subunit [Homo sapiens] [gi:487738]
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15
[SID24824580]
 Fluorescence-based biochemical primary high throughput assay to identify inhibitors of T-cell receptor (TCR)-CD3 interaction using a TAMRA-labeled TCR probe [AID651800, Type: screening]TCRAV4S1 [Homo sapiens] [gi:2358024]
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16
[SID24824580]
 Luminescence-based primary cell-based high throughput screening assay to identify activators of the Aryl Hydrocarbon Receptor (AHR) [AID2796, Type: screening]aryl hydrocarbon receptor precursor [Homo sapiens] [gi:4502003]
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17
[SID24824580]
 Luminescence-based primary cell-based high throughput screening assay to identify activators of the Aryl Hydrocarbon Receptor (AHR) [AID2796, Type: screening]aryl hydrocarbon receptor precursor [Homo sapiens] [gi:4502003]
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18
[SID24824580]
 Luminescence-based primary cell-based high throughput screening assay to identify activators of the Aryl Hydrocarbon Receptor (AHR) [AID2796, Type: screening]aryl hydrocarbon receptor precursor [Homo sapiens] [gi:4502003]
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19
[SID24824580]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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20
[SID24824580]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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21
[SID24824580]
Potency 28.1838qHTS Assay for Inhibitors Targeting the Menin-MLL Interaction in MLL Related Leukemias: Competition With Texas Red Labeled MLL-derived Mutant Peptide [AID1768, Type: confirmatory]MEN1 gene product [Homo sapiens] [gi:18860839]
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22
[SID24824580]
Potency 31.6228qHTS Fluorescence Polarization Assay for Inhibitors of MLL CXXC domain - DNA interaction [AID2662, Type: confirmatory]MLL gene product [Homo sapiens] [gi:56550039]
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23
[SID24824580]
Potency 100qHTS for Inhibitors of Polymerase Iota [AID588590, Type: confirmatory]DNA polymerase iota [Homo sapiens] [gi:154350220]
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24
[SID24824580]
Potency 100qHTS for Inhibitors of Polymerase Iota [AID588590, Type: confirmatory]DNA polymerase iota [Homo sapiens] [gi:154350220]
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25
[SID24824580]
EC50 110Luminescence-based Microorganism Dose Response HTS to Identify Inhibitors of E. Coli Growth [AID1959, Type: confirmatory]
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26
[SID24824580]
EC50 300Fluorescent Polarization Homogeneous Dose Response HTS to Indentify Inhibitors of POS-1 Binding to mex-3-RNA [AID1964, Type: confirmatory]POsterior Segregation family member (pos-1) [Caenorhabditis elegans] [gi:17562800]
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27
[SID24824580]
 Luminescence-based cell-based primary high throughput screening assay to identify activators of the DAF-12 from the parasite S. stercoralis (ssDAF-12) [AID652126, Type: screening]Protein DAF-12, isoform a [Caenorhabditis elegans] [gi:71987181]
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28
[SID24824580]
 High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set [AID588497, Type: Literature]botulinum neurotoxin type F, BoNT/F [Clostridium botulinum Bf] [gi:168184763]
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29
[SID24824580]
Potency qHTS for Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in Human Glioma: qHTS [AID602332, Type: confirmatory]heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) [Homo sapiens] [gi:168984549]
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30
[SID24824580]
Potency qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a [AID504332, Type: confirmatory]euchromatic histone-lysine N-methyltransferase 2 [Homo sapiens] [gi:168985070]
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31
[SID24824580]
Potency qHTS Assay for Inhibitors of Influenza NS1 Protein Function [AID2326, Type: confirmatory]nonstructural protein 1 [Influenza A virus (A/WSN/1933(H1N1))] [gi:194352380]
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32
[SID24824580]
 MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_SinglePoint_HTS_Activity [AID488899, Type: screening]Microphthalmia-associated transcription factor [Homo sapiens] [gi:40807040]
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33
[SID24824580]
 MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_SinglePoint_HTS_Activity [AID488899, Type: screening]Microphthalmia-associated transcription factor [Homo sapiens] [gi:40807040]
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34
[SID24824580]
 Anti-Malarial Hsp90 Inhibitors Measured in Microorganism System Using Plate Reader - 2121-01_Inhibitor_SinglePoint_HTS_Activity_Set2 [AID504621, Type: screening]HSP90 [Plasmodium falciparum 3D7] [gi:124809506]
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35
[SID24824580]
IC50 Inhibitors of Plasmodium falciparum M17- Family Leucine Aminopeptidase (M17LAP) [AID1619, Type: confirmatory]M17 leucyl aminopeptidase [Plasmodium falciparum 3D7] [gi:124809582]
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36
[SID24824580]
IC50 Inhibitors of Plasmodium falciparum M17- Family Leucine Aminopeptidase (M17LAP) [AID1619, Type: confirmatory]M17 leucyl aminopeptidase [Plasmodium falciparum 3D7] [gi:124809582]
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37
[SID24824580]
IC50 Inhibitors of Plasmodium falciparum M17- Family Leucine Aminopeptidase (M17LAP) [AID1619, Type: confirmatory]M17 leucyl aminopeptidase [Plasmodium falciparum 3D7] [gi:124809582]
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38
[SID24824580]
 QFRET-based primary biochemical high throughput screening assay to identify inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PFM18AAP). [AID1822, Type: screening]M18 aspartyl aminopeptidase [Plasmodium falciparum 3D7] [gi:23505220]
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39
[SID24824580]
 QFRET-based primary biochemical high throughput screening assay to identify inhibitors of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PFM18AAP). [AID1822, Type: screening]M18 aspartyl aminopeptidase [Plasmodium falciparum 3D7] [gi:23505220]
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40
[SID24824580]
IC50 Inhibitors of Plasmodium falciparum M1- Family Alanyl Aminopeptidase (M1AAP) [AID1445, Type: confirmatory]m1-family aminopeptidase [Plasmodium falciparum 3D7] [gi:124512980]
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41
[SID24824580]
IC50 Inhibitors of Plasmodium falciparum M1- Family Alanyl Aminopeptidase (M1AAP) [AID1445, Type: confirmatory]m1-family aminopeptidase [Plasmodium falciparum 3D7] [gi:124512980]
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42
[SID24824580]
 Multiplex HTS Screen of TOR pathway GFP-fusion proteins in Saccharomyes cerevisiae_specifically_ AGP1_MLPCN. [AID2066, Type: screening]Agp1p [Saccharomyces cerevisiae S288c] [gi:85666113]
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43
[SID24824580]
 Fluorescence Cell-Free Homogenous Primary HTS to Identify Inhibitors of the Ras-converting Enzyme [AID2563, Type: screening]Rce1p [Saccharomyces cerevisiae S288c] [gi:6323930]
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44
[SID24824580]
 Fluorescence Cell-Free Homogenous Primary HTS to Identify Inhibitors of the Ras-converting Enzyme [AID2563, Type: screening]Rce1p [Saccharomyces cerevisiae S288c] [gi:6323930]
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45
[SID24824580]
 uHTS identification of small molecule inhibitors of tim23-1 yeast via a luminescent assay [AID463212, Type: screening]TPA: Tim23p [Saccharomyces cerevisiae S288c] [gi:285814664]
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46
[SID24824580]
 HTS of Small Molecules that Regulate V-ATPase Proton Transport in Yeast using pHLuorin [AID504577, Type: screening]Vma11p [Saccharomyces cerevisiae S288c] [gi:6325022]
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47
[SID24824580]
 uHTS identification of small molecule inhibitors of tim10 yeast via a luminescent assay [AID463195, Type: screening]TPA: Tim10p [Saccharomyces cerevisiae S288c] [gi:285809906]
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48
[SID24824580]
 uHTS identification of small molecule inhibitors of tim10-1 yeast via a luminescent assay [AID463190, Type: screening]TPA: Tim10p [Saccharomyces cerevisiae S288c] [gi:285809906]
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49
[SID24824580]
 Fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of the membrane-associated serine protease Rv3671c in M.tuberculosis [AID2606, Type: screening]membrane-associated serine protease [Mycobacterium tuberculosis H37Rv] [gi:15610807]
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50
[SID24824580]
IC50 Inhibitors of Mycobacterial Glucosamine-1-phosphate acetyl transferase (GlmU) [AID1376, Type: confirmatory]UDP-N-acetylglucosamine pyrophosphorylase glmU [Mycobacterium tuberculosis H37Rv] [gi:15608158]
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