NSC357777 (CID 5477815) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(57)
 
 
Inactive(255)
 
 
Inconclusive(14)
 
 
Unspecified(2)
 
 
Top Targets:
p450(10)
 
 
 
 
7TM GPCR Srx(9)
 
 
7TM GPCR Srsx(6)
 
 
 
Peptidase C54(3)
 
 
BRLZ(3)
 
 
BioAssay Types:
Screening(173)
 
 
 
 
Confirmatory(133)
 
 
 
 
 
Literature(3)
 
 
BioActivity Types:
Potency(93)
 
 
 
 
 
IC50(11)
 
 
 
AC50(4)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 323    Data Row: 328   Total Pages: 7   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID4254263]
Potency 0.81Tau ThS binding assay [AID911, Type: confirmatory]Microtubule-associated protein tau [Homo sapiens] [gi:92096784]
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2
[SID4254263]
Potency 0.81Tau ThS binding assay [AID911, Type: confirmatory]Microtubule-associated protein tau [Homo sapiens] [gi:92096784]
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3
[SID4254263]
Potency 1.03Beta amyloid ThS binding assay [AID956, Type: confirmatory]beta-amyloid peptide, A beta {N-terminal} [human, cerebrospinal fluid, conditioned medium of mixed-b [gi:257056]
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4
[SID4254263]
Potency 1.2589qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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5
[SID4254263]
Potency 1.2589qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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6
[SID92763872]
AC50 1.31MLPCN 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
[SID92763872]
AC50 1.31MLPCN 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
[SID92763872]
AC50 2.15FRET-based HTS for detection of RAD52 Inhibitors Measured in Biochemical System Using Plate Reader - 7018-01_Inhibitor_Dose_CherryPick_Activity [AID652116, Type: confirmatory]RAD52 gene product [Homo sapiens] [gi:109637798]
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9
[SID4254263]
Potency 2.62482Alpha-synuclein ThS binding assay [AID937, Type: confirmatory]alpha synuclein [Homo sapiens] [gi:46242542]
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10
[SID4254263]
Potency 2.62482Alpha-synuclein ThS binding assay [AID937, Type: confirmatory]alpha synuclein [Homo sapiens] [gi:46242542]
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11
[SID92763872]
IC50 5.61Dose response confirmation of the uHTS fluorescent assay for identification of inhibitors of ATG4B. [AID504756, Type: confirmatory]cysteine protease ATG4B isoform a [Homo sapiens] [gi:47132611]
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12
[SID92763872]
IC50 6.649Discovery of Small Molecule Probes for H1N1 Influenza NS1A [AID504329, Type: confirmatory]nonstructural protein 1 [Influenza A virus (A/California/07/2009(H1N1))] [gi:227977143]
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13
[SID92763872]
Potency 7.3078qHTS 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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14
[SID92763872]
Potency 7.3078qHTS 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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15
[SID92763872]
Potency 7.3078qHTS 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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16
[SID92763872]
IC50 8.598Fluorescence-based biochemical high throughput dose response assay for inhibitors of the calcium sensitivity of cardiac Regulated Thin Filaments (RTF) [AID504742, Type: confirmatory]cardiac alpha tropomyosin [Sus scrofa] [gi:1927]
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17
[SID92763872]
IC50 9.6Dose response counterscreen of uHTS hits for ATG4B inhibitors in a Phospholipase A2 assay [AID588400, Type: confirmatory]phospholipase A2 precursor [Homo sapiens] [gi:4505847]
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18
[SID92763872]
IC50 9.6Dose response counterscreen of uHTS hits for ATG4B inhibitors in a Phospholipase A2 assay [AID588400, Type: confirmatory]phospholipase A2 precursor [Homo sapiens] [gi:4505847]
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19
[SID92763872]
Potency 11.2202qHTS for Inhibitors of WRN Helicase [AID651768, Type: confirmatory]WRN [Homo sapiens] [gi:3719421]
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20
[SID92763872]
IC50 12.69Discovery of small molecule inhibitors of the oncogenic and cytokinetic protein MgcRacGAP - Primary and Confirmatory Screens [AID624330, Type: confirmatory]RACGAP1 gene product [Homo sapiens] [gi:21361397]
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21
[SID92763872]
IC50 18.01Discovery of small molecule inhibitors of the oncogenic and cytokinetic protein MgcRacGAP - Counter Screen Coupled Enzyme [AID624351, Type: confirmatory]
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22
[SID92763872]
Potency 20.5962qHTS 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
[SID92763872]
Potency 20.5962qHTS 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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24
[SID92763872]
Potency 20.5962qHTS 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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25
[SID92763872]
Potency 28.1838qHTS Assay for the Inhibitors of Human Flap endonuclease 1 (FEN1). [AID588795, Type: confirmatory]flap endonuclease 1 [Homo sapiens] [gi:4758356]
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26
[SID92763872]
Potency 39.8107qHTS for Inhibitors of Polymerase Eta [AID588591, Type: confirmatory]DNA polymerase eta [Homo sapiens] [gi:5729982]
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27
[SID92763872]
Potency 39.8107qHTS for Inhibitors of Polymerase Eta [AID588591, Type: confirmatory]DNA polymerase eta [Homo sapiens] [gi:5729982]
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28
[SID92763872]
Potency 56.2341qHTS 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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29
[SID92763872]
Potency 58.0479qHTS Assay for Inhibitors of Rango (Ran-regulated importin-beta cargo) - Importin beta complex formation [AID540263, Type: confirmatory]snurportin-1 [Homo sapiens] [gi:5031833]
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30
[SID92763872]
CC50 67.444Discovery of small molecule inhibitors of the oncogenic and cytokinetic protein MgcRacGAP - HeLa Cytotoxicity [AID624300, Type: confirmatory]
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31
[SID92763872]
Potency 70.7946HTS 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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32
[SID92763872]
Potency 79.4328qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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33
[SID92763872]
Potency 79.4328qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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34
[SID92763872]
 Fluorescence polarization-based biochemical primary high throughput screening assay to identify inhibitors of ArfGAP with SH3 domain, ankyrin repeat and PH domain 1 (ASAP1) [AID624377, Type: screening]ASAP1 gene product [Homo sapiens] [gi:351542238]
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35
[SID26653182]
 Inhibitors of the EP2 Prostaglandin E2 Receptor - Primary Screen [AID1422, Type: screening]prostaglandin E receptor 2 (subtype EP2), 53kDa [Homo sapiens] [gi:31881630]
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36
[SID26653182]
 Inhibitors of the EP2 Prostaglandin E2 Receptor - Primary Screen [AID1422, Type: screening]prostaglandin E receptor 2 (subtype EP2), 53kDa [Homo sapiens] [gi:31881630]
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37
[SID92763872]
 FRET-based HTS for detection of RAD52 Inhibitors Measured in Biochemical System Using Plate Reader - 7018-01_Inhibitor_SinglePoint_HTS_Activity_Set2 [AID651710, Type: screening]RAD52 gene product [Homo sapiens] [gi:109637798]
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38
[SID92763872]
 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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39
[SID92763872]
 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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40
[SID92763872]
 Single concentration confirmation of inhibitors of ATG4B via a fluorescent assay [AID504757, Type: screening]cysteine protease ATG4B isoform a [Homo sapiens] [gi:47132611]
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41
[SID92763872]
 uHTS fluorescent assay for identification of inhibitors of ATG4B [AID504462, Type: screening]cysteine protease ATG4B isoform a [Homo sapiens] [gi:47132611]
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42
[SID92763872]
 qHTS Assay for Inhibitors of the CtBP/E1A Interaction [AID651724, Type: screening]CtBP interacting protein CtIP [Homo sapiens] [gi:1730321]
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43
[SID92763872]
 uHTS identification of SUMO1-mediated protein-protein interactions [AID602429, Type: screening]SUMO-1 [Homo sapiens] [gi:1762973]
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44
[SID92763872]
 Fluorescence-based biochemical primary high throughput screening assay to identify inhibitors of the calcium sensitivity of cardiac Regulated Thin Filaments (RTF) [AID493244, Type: screening]cardiac alpha tropomyosin [Sus scrofa] [gi:1927]
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45
[SID92763872]
 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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46
[SID92763872]
 uHTS identification of inhibitors of NadD in a Colorimetric assay [AID602399, Type: screening]hypothetical protein SA1422 [Staphylococcus aureus subsp. aureus N315] [gi:15927174]
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47
[SID92763872]
Potency qHTS for Inhibitors of phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) [AID652105, Type: confirmatory]Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha [gi:18266879]
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48
[SID92763872]
 Fluorescence-based biochemical high throughput confirmation assay for inhibitors of the calcium sensitivity of cardiac Regulated Thin Filaments (RTF) [AID504635, Type: screening]cardiac alpha tropomyosin [Sus scrofa] [gi:1927]
View
49
[SID92763872]
 Fluorescence polarization-based biochemical primary high throughput screening assay to identify inhibitors of ADP-ribosylation factor GTPase activating protein 1 (ARFGAP1) [AID651572, Type: screening]Arfgap1 gene product [Rattus norvegicus] [gi:21489979]
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50
[SID92763872]
 HTS Assay for Peg3 Promoter Inhibitors [AID588405, Type: screening]Ppp1r15a gene product [Rattus norvegicus] [gi:78486550]
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