MLS001149857 (CID 24237049) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(13)
 
 
Inactive(431)
 
 
Inconclusive(13)
 
 
Unspecified(1)
 
 
Top Targets:
7TM GPCR Srx(14)
 
 
KCNQ channel(9)
 
 
 
7TM GPCR Srsx(6)
 
 
TRP 2(5)
 
 
Pyruvate Kina..(4)
 
 
BioAssay Types:
Screening(315)
 
 
 
 
Confirmatory(132)
 
 
 
 
 
Literature(5)
 
 
BioActivity Types:
Potency(99)
 
 
 
 
 
IC50(25)
 
 
 
EC50(4)
 
 
AC50(2)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 458    Data Row: 458   Total Pages: 10   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID49822915]
AC50 2.639MLPCN Dyrk1A Kinase Measured in Biochemical System Using Plate Reader - 2124-01_Inhibitor_Dose_CherryPick_Activity [AID588345, Type: confirmatory]dual specificity tyrosine-phosphorylation-regulated kinase 1A [Rattus norvegicus] [gi:6978787]
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2
[SID49822915]
AC50 2.639MLPCN Dyrk1A Kinase Measured in Biochemical System Using Plate Reader - 2124-01_Inhibitor_Dose_CherryPick_Activity [AID588345, Type: confirmatory]dual specificity tyrosine-phosphorylation-regulated kinase 1A [Rattus norvegicus] [gi:6978787]
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3
[SID49822915]
Potency 13.4591qHTS profiling assay for firefly luciferase inhibitor/activator using purifed enzyme and Km concentrations of substrates (counterscreen for miR-21 project) [AID588342, Type: confirmatory]Luciferase [Photinus pyralis] [gi:160794]
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4
[SID49822915]
Potency 25.929qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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5
[SID49822915]
Potency 25.929qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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6
[SID49822915]
Potency 25.929qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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7
[SID49822915]
 Dyrk1 A HTS Measured in Biochemical System Using Plate Reader - 2124-01_Inhibitor_SinglePoint_HTS_Activity [AID504441, Type: screening]dual specificity tyrosine-phosphorylation-regulated kinase 1A [Rattus norvegicus] [gi:6978787]
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8
[SID49822915]
 Dyrk1 A HTS Measured in Biochemical System Using Plate Reader - 2124-01_Inhibitor_SinglePoint_HTS_Activity [AID504441, Type: screening]dual specificity tyrosine-phosphorylation-regulated kinase 1A [Rattus norvegicus] [gi:6978787]
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9
[SID49822915]
 Cycloheximide Counterscreen for Small Molecule Inhibitors of Shiga Toxin [AID2314, Type: screening]shiga toxin 1 variant A subunit [Escherichia coli O157:H7] [gi:32400299]
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10
[SID49822915]
 A qHTS for Small Molecule Inhibitors of Shiga Toxin [AID2315, Type: screening]shiga toxin 1 variant A subunit [Escherichia coli O157:H7] [gi:32400299]
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11
[SID49822915]
 HTS-Luminescent assay for inhibitors of ALR by detection of hydrogen peroxide production Measured in Biochemical System Using Plate Reader - 2036-02_Inhibitor_SinglePoint_HTS [AID485317, Type: screening]FAD-linked sulfhydryl oxidase ALR [Homo sapiens] [gi:54112432]
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12
[SID49822915]
 Validation (re-confirmation) assay for identification of compounds that inhibit KCNQ1 potassium channels [AID588353, Type: screening]KCNQ1 gene product [Homo sapiens] [gi:32479527]
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13
[SID49822915]
 Specificity screen against KCNQ1/KCNE1 for identification of compounds that inhibit KCNQ1 potassium channels [AID652147, Type: screening]KCNQ1 gene product [Homo sapiens] [gi:32479527]
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14
[SID49822915]
 Validation for compounds that inhibit KCNQ1 potassium channels on automated electrophysiology assay [AID624120, Type: other]KCNQ1 gene product [Homo sapiens] [gi:32479527]
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15
[SID49822915]
 Primary cell-based high-throughput screening assay for identification of compounds that inhibit KCNQ1 potassium channels [AID2642, Type: screening]KCNQ1 gene product [Homo sapiens] [gi:32479527]
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16
[SID49822915]
 Screen for inhibitors of the SWI/SNF chromatin remodeling complex (esBAF) in mouse embryonic stem cells with Luciferase reporter assay Measured in Cell-Based System Using Plate Reader - 2141-01_Inhibitor_SinglePoint_HTS_Activity [AID602393, Type: screening]transcription activator BRG1 isoform 1 [Mus musculus] [gi:291463269]
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17
[SID49822915]
 Specificity screen against KCNQ2 for identification of compounds that inhibit KCNQ1 potassium channels [AID651746, Type: screening]Kcnq2 gene product [Rattus norvegicus] [gi:18959272]
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18
[SID49822915]
 Specificity screen against KCNQ2 for identification of compounds that inhibit KCNQ1 potassium channels [AID651746, Type: screening]Kcnq2 gene product [Rattus norvegicus] [gi:18959272]
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19
[SID49822915]
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
[SID49822915]
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
[SID49822915]
Potency 35.4813qHTS Inhibitors of AmpC Beta-Lactamase (assay without detergent) [AID485341, Type: confirmatory]Chain A, Ampc Beta-Lactamase In Complex With 4-Methanesulfonylamino Benzoic Acid [gi:119389684]
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22
[SID49822915]
 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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23
[SID49822915]
 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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24
[SID49822915]
 Fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of the HTRA serine peptidase 1 (HTRA1) [AID504803, Type: screening]HTRA1 protein [gi:121945198]
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25
[SID49822915]
 uHTS identification of modulators of interaction between CendR and NRP-1 using Fluorescence Polarization assay [AID602438, Type: screening]Chain A, Crystal Structure Of The B1b2 Domains From Human Neuropilin- 1 [gi:160877737]
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26
[SID49822915]
Potency qHTS 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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27
[SID49822915]
 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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28
[SID49822915]
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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29
[SID49822915]
Potency qHTS of GLP-1 Receptor Agonists [AID624172, Type: confirmatory]glp-1 receptor [Homo sapiens] [gi:1724069]
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30
[SID49822915]
Potency qHTS of GLP-1 Receptor Agonists [AID624172, Type: confirmatory]glp-1 receptor [Homo sapiens] [gi:1724069]
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31
[SID49822915]
 Heat Shock Factor-1 (HSF-1) Measured in Cell-Based System Using Plate Reader - 2038-01_Activator_SinglePoint_HTS_Activity [AID504408, Type: screening]
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32
[SID49822915]
Potency Nrf2 qHTS screen for inhibitors: counterscreen for cytotoxicity [AID504648, Type: confirmatory]
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33
[SID49822915]
Potency Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 48 hour incubation [AID504832, Type: confirmatory]
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34
[SID49822915]
Potency Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation [AID504834, Type: confirmatory]
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35
[SID49822915]
IC50 uHTS fluorescence assay for the identification of Human Immunodeficiency Virus Fusion Inhibitors. [AID1986, Type: confirmatory]envelope glycoprotein [Human immunodeficiency virus 1] [gi:45357394]
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36
[SID49822915]
 QFRET-based counterscreen for PFM18AAP inhibitors: biochemical high throughput screening assay to identify inhibitors of the Cathepsin L proteinase (CTSL1). [AID1906, Type: screening]cathepsin L1 [Homo sapiens] [gi:55958172]
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37
[SID49822915]
 Counterscreen for procaspase-3 activators: absorbance-based primary biochemical high throughput screening assay to identify activators of procaspase-7 [AID463210, Type: screening]caspase 7, apoptosis-related cysteine peptidase [Homo sapiens] [gi:55960760]
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38
[SID49822915]
Potency qHTS of Trypanosoma Brucei Inhibitors [AID624173, Type: confirmatory]hypothetical protein, conserved [Trypanosoma brucei] [gi:62359610]
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39
[SID49822915]
 Plate Read Microorganism-Based Primary HTS to Identify Modulators of the AI-2 Quorum Sensing System [AID2094, Type: screening]Chain A, Crystal Structure Of The Apo Form Of Vibrio Harveyi Luxp Complexed With The Periplasmic Dom [gi:67463988]
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40
[SID49822915]
 QFRET-based primary biochemical high throughput screening assay to identify inhibitors of the SARS coronavirus 3C-like Protease (3CLPro) [AID1706, Type: screening]3C-like protease [Infectious bronchitis virus] [gi:73745819]
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41
[SID49822915]
 PgID: DNTB colorimetric HTS to detect inhibitor of PgID Measured in Biochemical System Using Plate Reader - 2164-01_Inhibitor_SinglePoint_HTS_Activity [AID602405, Type: screening]WlaI protein (PglD) [gi:75495260]
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42
[SID49822915]
 TR-FRET-based primary biochemical high-throughput screening assay to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization [AID1899, Type: screening]core protein [Hepatitis C virus] [gi:83779224]
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43
[SID49822915]
 Counterscreen for inhibitors of 5-meCpG-binding domain protein 2 (MBD2): TRFRET-based biochemical primary high throughput screening assay to identify inhibitors of binding of ubiquitin-like with PHD and ring finger domains 1 (UHRF1) to methylated oligonucleotide [AID687016, Type: screening]UHRF1 gene product [Homo sapiens] [gi:115430235]
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44
[SID49822915]
Potency qHTS Inhibitors of AmpC Beta-Lactamase (assay with detergent) [AID485294, Type: confirmatory]Chain A, Ampc Beta-Lactamase In Complex With 4-Methanesulfonylamino Benzoic Acid [gi:119389684]
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45
[SID49822915]
 uHTS identification of small molecule activators of the apoptotic arm of the Unfolded Protein response via a luminescent-based reporter assay [AID449763, Type: screening]
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46
[SID49822915]
 Phenotypic HTS multiplex for antifungal efflux pump inhibitors [AID485275, Type: screening]
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47
[SID49822915]
 uHTS identification of small molecule activators of the adaptive arm of the Unfolded Protein response via a luminescent-based reporter assay [AID463104, Type: screening]
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48
[SID49822915]
 Fluorescence-based counterscreen for orexin 1 receptor (OX1R) antagonists: cell-based assay to identify antagonists of the parental CHO cell line [AID463079, Type: screening]
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49
[SID49822915]
Potency qHTS Assay for Small Molecule Inhibitors of Mitochondrial Division or Activators of Mitochondrial Fusion [AID485298, Type: confirmatory]
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50
[SID49822915]
 Inhibitors of Prion Protein 5' UTR mRNA Measured in Cell-Based System Using Plate Reader - 2078-01_Inhibitor_SinglePoint_HTS_Activity [AID488862, Type: screening]
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