MLS000103371 (CID 1789058) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(134)
 
 
Inactive(540)
 
 
Inconclusive(42)
 
 
Unspecified(2)
 
 
Top Targets:
7TM GPCR Srx(20)
 
 
 
alkPPc(14)
 
 
Bcl-2 like(13)
 
 
 
Tryp SPc(12)
 
 
 
7TM GPCR Srsx(8)
 
 
 
BioAssay Types:
Screening(468)
 
 
 
 
 
Confirmatory(223)
 
 
 
 
 
Literature(5)
 
 
BioActivity Types:
Potency(136)
 
 
 
 
 
IC50(50)
 
 
 
 
EC50(17)
 
 
 
AC50(7)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 718    Data Row: 718   Total Pages: 15   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID7971429]
EC50 0.1101Fluorescence Polarization Cell-Free Homogeneous Dose Retest to Confirm Inhibitors of the LANA Histone H2A/H2B Interaction [AID435023, Type: confirmatory]LANA [Human herpesvirus 8] [gi:139472804]
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2
[SID7971429]
AC50 0.526C-LANA FP assay Measured in Biochemical System Using Plate Reader - 2117-01_Inhibitor_Dose_CherryPick_Activity [AID504725, Type: confirmatory]LANA [Human herpesvirus 8] [gi:312275222]
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3
[SID7971429]
Potency 0.5645qHTS Fluorescence Polarization (FP) Assay for Inhibitors of MLL CXXC domain - DNA interaction: Fluorescein FP [AID624160, Type: confirmatory]
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4
[SID7971429]
AC50 0.63C-LANA Counter Screen: DNA intercalators Measured in Biochemical System Using Plate Reader - 2117-02_Inhibitor_Dose_CherryPick_Activity_Set2 [AID504727, Type: confirmatory]LANA [Human herpesvirus 8] [gi:312275222]
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5
[SID7971429]
IC50 0.88994Epi-absorbance-based dose response assay for common IMP-1 and VIM-2 inhibitors: biochemical high throughput counterscreen to identify inhibitors of TEM-1 metallo-beta-lactamase [AID2755, Type: confirmatory]Beta lactamase [Pseudomonas aeruginosa] [gi:114881106]
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6
[SID7971429]
AC50 1.575MLPCN 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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7
[SID7971429]
AC50 1.575MLPCN 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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8
[SID7971429]
IC50 1.84Epi-absorbance-based dose response assay for common IMP-1 and VIM-2 inhibitors: biochemical high throughput screening assay to identify inhibitors of VIM-2 metallo-beta-lactamase [AID2754, Type: confirmatory]metallo beta-lactamase [Pseudomonas aeruginosa] [gi:7381449]
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9
[SID7971429]
IC50 1.84Epi-absorbance-based dose response assay for common IMP-1 and VIM-2 inhibitors: biochemical high throughput screening assay to identify inhibitors of VIM-2 metallo-beta-lactamase [AID2754, Type: confirmatory]metallo beta-lactamase [Pseudomonas aeruginosa] [gi:7381449]
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10
[SID7971429]
IC50 2.115Epi-absorbance-based dose response assay for common IMP-1 and VIM-2 inhibitors: biochemical high throughput screening assay to identify inhibitors of IMP-1metallo-beta-lactamase [AID2756, Type: confirmatory]metallo-beta-lactamase IMP-1 [Pseudomonas aeruginosa] [gi:27368096]
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11
[SID7971429]
Potency 3.9811qHTS FP-Based Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) [AID2573, Type: confirmatory]Chain A, Human Ape1 Endonuclease With Bound Abasic Dna And Mn2+ Ion [gi:6980812]
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12
[SID7971429]
EC50 4.03HCS for Compounds that Up-Regulate Insulin Promoter Activity in MIN6 Cells [AID1625, Type: confirmatory]
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13
[SID7971429]
Potency 7.0795qHTS for Small Molecule Inhibitors of the ERG Ets/DNA interaction [AID624246, Type: confirmatory]ERG gene product [Homo sapiens] [gi:343478176]
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14
[SID7971429]
Potency 7.0795qHTS for Small Molecule Inhibitors of the ERG Ets/DNA interaction [AID624246, Type: confirmatory]ERG gene product [Homo sapiens] [gi:343478176]
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15
[SID7971429]
Potency 10qHTS Multiplex Assay to Identify Dual Action Probes in a Cell Model of Huntington: Aggregate Formation (GFP) [AID1688, Type: confirmatory]huntingtin [Homo sapiens] [gi:90903231]
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16
[SID7971429]
Potency 10qHTS Multiplex Assay to Identify Dual Action Probes in a Cell Model of Huntington: Aggregate Formation (GFP) [AID1688, Type: confirmatory]huntingtin [Homo sapiens] [gi:90903231]
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17
[SID7971429]
Potency 11.5821qHTS screen for small molecules that inhibit ELG1-dependent DNA repair in human embryonic kidney (HEK293T) cells expressing luciferase-tagged ELG1 [AID504467, Type: confirmatory]ATAD5 protein [Homo sapiens] [gi:116283940]
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18
[SID7971429]
Potency 12.5893Counterscreen for APE1 Inhibitors: qHTS Assay for Inhibitors of Endonuclease IV [AID2565, Type: confirmatory]endonuclease IV [Escherichia coli] [gi:405898]
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19
[SID7971429]
Potency 14.581A quantitative high throughput screen for small molecules that induce DNA re-replication in MCF 10a normal breast cells. [AID624296, Type: confirmatory]GMNN gene product [Homo sapiens] [gi:7705682]
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20
[SID7971429]
Potency 14.581qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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21
[SID7971429]
Potency 14.581qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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22
[SID7971429]
Potency 14.581qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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23
[SID7971429]
Potency 16.3601qHTS 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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24
[SID7971429]
Potency 16.3601qHTS 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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25
[SID7971429]
Potency 16.3601qHTS 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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26
[SID7971429]
Potency 18.3564A quantitative high throughput screen for small molecules that induce DNA re-replication in SW480 colon adenocarcinoma cells. [AID624297, Type: confirmatory]GMNN gene product [Homo sapiens] [gi:7705682]
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27
[SID7971429]
Potency 25.1189qHTS Assay for Inhibitors of DNA Polymerase Beta [AID485314, Type: confirmatory]DNA polymerase beta [Homo sapiens] [gi:4505931]
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28
[SID7971429]
Potency 25.1189qHTS Assay for Inhibitors of DNA Polymerase Beta [AID485314, Type: confirmatory]DNA polymerase beta [Homo sapiens] [gi:4505931]
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29
[SID7971429]
Potency 25.1189qHTS 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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30
[SID7971429]
Potency 28.1838qHTS 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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31
[SID7971429]
Potency 28.1838qHTS for Inhibitors of WRN Helicase [AID651768, Type: confirmatory]WRN [Homo sapiens] [gi:3719421]
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32
[SID7971429]
Potency 31.6228qHTS 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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33
[SID7971429]
Potency 56.2341Confirmation qHTS Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) - Round 2 Cherry Picks [AID504841, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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34
[SID7971429]
Potency 63.3428qHTS Fluorescence Polarization (FP) Assay for Inhibitors of MLL CXXC domain - DNA interaction: Texas Red FP [AID624161, Type: confirmatory]
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35
[SID7971429]
AC50 66.07424 hour HeLa Cytotox assay Measured in Cell-Based System Using Plate Reader - 2117-03_Inhibitor_Dose_CherryPick_Activity [AID504726, Type: confirmatory]LANA [Human herpesvirus 8] [gi:312275222]
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36
[SID7971429]
Potency 79.4328qHTS Assay for Inhibitors of Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase) [AID1490, Type: confirmatory]phosphopantetheinyl transferase [Bacillus subtilis] [gi:10954339]
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37
[SID7971429]
Potency 79.4328qHTS Assay for the Inhibitors of Human Flap endonuclease 1 (FEN1). [AID588795, Type: confirmatory]flap endonuclease 1 [Homo sapiens] [gi:4758356]
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38
[SID7971429]
AC50 270.5Luminescence Cell-Free Homogeneous Dose Retest to Confirm Inhibitors of GSK-3 alpha [AID463203, Type: confirmatory]GSK3A gene product [Homo sapiens] [gi:49574532]
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39
[SID7971429]
AC50 270.5Luminescence Cell-Free Homogeneous Dose Retest to Confirm Inhibitors of GSK-3 alpha [AID463203, Type: confirmatory]GSK3A gene product [Homo sapiens] [gi:49574532]
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40
[SID7971429]
 Fluorescence-based cell-based primary high throughput screening assay to identify antagonists of the orexin 1 receptor (OX1R; HCRTR1) [AID434989, Type: screening]orexin receptor type 1 [Homo sapiens] [gi:222080095]
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41
[SID7971429]
 Fluorescence-based cell-based primary high throughput screening assay to identify antagonists of the orexin 1 receptor (OX1R; HCRTR1) [AID434989, Type: screening]orexin receptor type 1 [Homo sapiens] [gi:222080095]
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42
[SID7971429]
 FRET-based cell-based primary high throughput screening assay to identify antagonists of the orexin 1 receptor (OX1R; HCRTR1) [AID485270, Type: screening]orexin receptor type 1 [Homo sapiens] [gi:222080095]
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43
[SID7971429]
 FRET-based cell-based primary high throughput screening assay to identify antagonists of the orexin 1 receptor (OX1R; HCRTR1) [AID485270, Type: screening]orexin receptor type 1 [Homo sapiens] [gi:222080095]
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44
[SID7971429]
 Primary biochemical fluorescence polarization-based high throughput screening assay to identify inhibitors of protein arginine methyltransferase 1 (PRMT1) [AID652257, Type: screening]PRMT1 protein [Homo sapiens] [gi:32425330]
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45
[SID7971429]
 Primary biochemical fluorescence polarization-based high throughput screening assay to identify inhibitors of protein arginine methyltransferase 1 (PRMT1) [AID652257, Type: screening]PRMT1 protein [Homo sapiens] [gi:32425330]
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46
[SID7971429]
 Fluorescence polarization-based cell-based primary high throughput screening assay to identify activators of insulin-degrading enzyme (IDE) [AID493087, Type: screening]IDE gene product [Homo sapiens] [gi:155969707]
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47
[SID7971429]
 uHTS for identification of Inhibitors of Mdm2/MdmX interaction in luminescent format. [AID485346, Type: screening]protein Mdm4 isoform 1 [Homo sapiens] [gi:88702791]
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48
[SID7971429]
 uHTS for identification of Inhibitors of Mdm2/MdmX interaction in luminescent format. [AID485346, Type: screening]protein Mdm4 isoform 1 [Homo sapiens] [gi:88702791]
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49
[SID7971429]
 Single concentration confirmation of uHTS for Inhibitors of Mdm2/MdmX interaction in luminescent format. [AID489028, Type: screening]protein Mdm4 isoform 1 [Homo sapiens] [gi:88702791]
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50
[SID7971429]
 Single concentration confirmation of uHTS for Inhibitors of Mdm2/MdmX interaction in luminescent format. [AID489028, Type: screening]protein Mdm4 isoform 1 [Homo sapiens] [gi:88702791]
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