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4-hydroxy-1-methyl-3-(5-oxo-2,5-dihydro-1H-pyrazol-3-yl)-2(1H)-quinolinone (CID 54687581) - Compound BioActivity Data
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BioActivity Outcomes:
Active(11)
 
 
Inactive(639)
 
 
Inconclusive(12)
 
 
Unspecified(1)
 
 
Top Targets:
7TM GPCR Srx(19)
 
 
7TM GPCR Srsx(17)
 
 
Bcl-2 like(11)
 
 
alkPPc(10)
 
 
G-alpha(8)
 
 
 
BioAssay Types:
Screening(447)
 
 
 
 
Confirmatory(198)
 
 
 
 
 
Literature(5)
 
 
BioActivity Types:
Potency(145)
 
 
 
 
 
IC50(35)
 
 
EC50(12)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 614    Data Row: 663   Total Pages: 14   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-5 [gi:55976631]
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3
[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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4
[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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5
[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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6
[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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7
[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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8
[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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9
[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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10
[SID24824580]
MLPCN maternal gene expression-MEX-5 TCR-2 binding assay-Primary Screen [AID1832, Type: screening]Zinc finger protein mex-5 [gi:55976631]
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11
[SID24824580]
HTS for Bacterial rRNA inhibitors Measured in Microorganism-Based System Using Plate Reader - 7056-01_Inhibitor_SinglePoint_HTS_Activity [AID720706, Type: screening]
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12
[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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13
[SID24824580]
Potency 25.1189qHTS for Inhibitors of AMA1-RON; Towards Development of Antimalarial Drug Lead: Primary Screen [AID720542, Type: confirmatory]apical membrane antigen 1, AMA1 [Plasmodium falciparum 3D7] [gi:23496270]
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14
[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]histone-lysine N-methyltransferase 2A isoform 2 precursor [Homo sapiens] [gi:56550039]
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15
[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]menin isoform 1 [Homo sapiens] [gi:18860839]
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16
[SID24824580]
Potency 31.6228qHTS Fluorescence Polarization Assay for Inhibitors of MLL CXXC domain - DNA interaction [AID2662, Type: confirmatory]histone-lysine N-methyltransferase 2A isoform 2 precursor [Homo sapiens] [gi:56550039]
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17
[SID24824580]
Potency 100qHTS for Inhibitors of Polymerase Iota [AID588590, Type: confirmatory]DNA polymerase iota [Homo sapiens] [gi:154350220]
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18
[SID24824580]
EC50 110Luminescence-based Microorganism Dose Response HTS to Identify Inhibitors of E. Coli Growth [AID1959, Type: confirmatory]
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19
[SID24824580]
EC50 300Fluorescent Polarization Homogeneous Dose Response HTS to Indentify Inhibitors of POS-1 Binding to mex-3-RNA [AID1964, Type: confirmatory]Protein POS-1 [Caenorhabditis elegans] [gi:17562800]
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20
[SID24824580]
Multiplex HTS Screen of TOR pathway GFP-fusion proteins in Saccharomyes cerevisiae_specifically_ LAP4_MLPCN. [AID2023, Type: screening]LAP4 [Saccharomyces cerevisiae] [gi:486173]
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21
[SID24824580]
Primary cell-based high-throughput screening assay for identification of compounds that protect hERG from block by proarrhythmic agents [AID1511, Type: screening]putative potassium channel subunit [Homo sapiens] [gi:487738]
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22
[SID24824580]
HTS to identify specific small molecule inhibitors of Ras and Ras-related GTPases specifically Cdc42 wildtype [AID761, Type: screening]cell division cycle 42 (GTP binding protein, 25kDa) [Homo sapiens] [gi:56202836]
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23
[SID24824580]
Potency qHTS Assay for Inhibitors Targeting the Menin-MLL Interaction in MLL Related Leukemias: Competition With Fluorescein Labeled MLL-derived Peptide [AID1766, Type: confirmatory]histone-lysine N-methyltransferase 2A isoform 2 precursor [Homo sapiens] [gi:56550039]
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24
[SID24824580]
Potency qHTS for Inhibitors of TGF-b [AID588855, Type: confirmatory]Smad3 [Homo sapiens] [gi:18418623]
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25
[SID24824580]
Potency qHTS Assay for Inhibitors Targeting the Menin-MLL Interaction in MLL Related Leukemias: Competition With Fluorescein Labeled MLL-derived Peptide [AID1766, Type: confirmatory]menin isoform 1 [Homo sapiens] [gi:18860839]
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26
[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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27
[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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28
[SID24824580]
Fluorescence-based primary biochemical high throughput screening assay to identify inhibitors of the Hepatitis C Virus non-structural protein 3 helicase (NS3) [AID1800, Type: screening]NS3 [Hepatitis C virus] [gi:125541954]
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29
[SID24824580]
Fluorescence-based counterscreen assay for HCV NS3 helicase inhibitors: biochemical high-throughput screening assay to identify compounds that cause fluorescent intercalator displacement (FID) [AID1845, Type: screening]NS3 [Hepatitis C virus] [gi:125541954]
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30
[SID24824580]
C. difficile toxins: HTS for inhibitors of TcdB glycohydrolase activity Measured in Biochemical System Using Plate Reader - 7074-01_Inhibitor_SinglePoint_HTS_Activity [AID652162, Type: screening]toxin B [Clostridium difficile 630] [gi:126698238]
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31
[SID24824580]
Primary cell-based high-throughput screening assay to measure PERK inhibition [AID1416, Type: screening]eukaryotic translation initiation factor 2-alpha kinase 3 precursor [Homo sapiens] [gi:134304838]
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32
[SID24824580]
uHTS for Small Molecule Inhibitiors of Epstein-Barr Virus Inhibitors [AID1085, Type: screening]BZLF2 [Human herpesvirus 4 type 2] [gi:139424501]
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33
[SID24824580]
Fluorescence Polarization Cell-Free Homogeneous Primary HTS to Identify Inhibitors of the LANA Histone H2A/H2B Interaction [AID2629, Type: screening]LANA [Human herpesvirus 8] [gi:139472804]
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34
[SID24824580]
High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set [AID588499, Type: Literature]botulinum neurotoxin type A [Clostridium botulinum A str. ATCC 3502] [gi:148378801]
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35
[SID24824580]
RNA aptamer-based HTS for inhibitors of GRK2 [AID488847, Type: screening]beta-adrenergic receptor kinase 1 [Homo sapiens] [gi:148539876]
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36
[SID24824580]
Fluorescence-based biochemical high throughput primary assay to identify inhibitors of phospholipase C isozymes (PLC-beta3). [AID720704, Type: screening]Phospholipase C, beta 3 (phosphatidylinositol-specific) [Homo sapiens] [gi:148745659]
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37
[SID24824580]
Fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of the prolyl oligopeptidase-like enzyme (PREPL) [AID2751, Type: screening]Prolyl endopeptidase-like [Homo sapiens] [gi:153217451]
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38
[SID24824580]
Potency qHTS Assay for Inhibitors of GCN5L2 [AID504327, Type: confirmatory]histone acetyltransferase KAT2A [Homo sapiens] [gi:153791535]
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39
[SID24824580]
Plate Read Microorganism-Based Primary HTS to Identify Modulators of the AI-2 Quorum Sensing System [AID2094, Type: screening]LuxS [Vibrio harveyi] [gi:166202459]
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40
[SID24824580]
uHTS Fluorescent assay for identification of inhibitors of Apaf-1 [AID489030, Type: screening]Apoptotic peptidase activating factor 1 [Homo sapiens] [gi:187952397]
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41
[SID24824580]
uHTS Fluorescent assay for identification of activators of Apaf-1 [AID489031, Type: screening]Apoptotic peptidase activating factor 1 [Homo sapiens] [gi:187952397]
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42
[SID24824580]
Potency HTS for Inhibitors of HP1-beta Chromodomain Interactions with Methylated Histone Tails [AID540317, Type: confirmatory]chromobox protein homolog 1 [Homo sapiens] [gi:187960037]
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43
[SID24824580]
Identification of agents that induce E-selectin on human endothelial cells Measured in Cell-Based System Using Imaging - 2152-01_Activator_SinglePoint_HTS_Activity [AID686992, Type: screening]E-selectin precursor [Homo sapiens] [gi:187960042]
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44
[SID24824580]
Potency qHTS Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2 as the Reporter [AID463254, Type: confirmatory]ubiquitin carboxyl-terminal hydrolase 2 isoform a [Homo sapiens] [gi:188528692]
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45
[SID24824580]
Potency VP16 counterscreen qHTS for inhibitors of ROR gamma transcriptional activity [AID2546, Type: confirmatory]nuclear receptor ROR-gamma [Mus musculus] [gi:188536040]
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46
[SID24824580]
Potency qHTS for inhibitors of ROR gamma transcriptional activity [AID2551, Type: confirmatory]nuclear receptor ROR-gamma [Mus musculus] [gi:188536040]
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47
[SID24824580]
Potency qHTS for Inhibitors of the Interaction of Thyroid Hormone Receptor and Steroid Receptor Coregulator 2 [AID1469, Type: confirmatory]thyroid hormone receptor beta [Homo sapiens] [gi:189491771]
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48
[SID24824580]
Potency Total Fluorescence Counterscreen for Inhibitors of the Interaction of Thyroid Hormone Receptor and Steroid Receptor Coregulator 2 [AID1479, Type: confirmatory]thyroid hormone receptor beta [Homo sapiens] [gi:189491771]
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49
[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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50
[SID24824580]
Primary cell-based high-throughput screening for identification of compounds that activate MrgX1 receptor signaling [AID588627, Type: screening]MAS-related GPR member X1 [Homo sapiens] [gi:195969650]
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