3-amino-6-benzyl-N-(2-fluorophenyl)-4-(trifluoromethyl)thieno[2,3-b]pyridine-2-carboxamide (CID 1006298) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(23)
 
 
Inactive(604)
 
 
Inconclusive(26)
 
 
Unspecified(2)
 
 
Top Targets:
7TM GPCR Srx(19)
 
 
alkPPc(12)
 
 
Bcl-2 like(10)
 
 
7TM GPCR Srsx(9)
 
 
 
G-alpha(6)
 
 
 
BioAssay Types:
Screening(445)
 
 
 
 
 
Confirmatory(192)
 
 
 
 
 
Literature(5)
 
 
BioActivity Types:
Potency(129)
 
 
 
 
 
IC50(37)
 
 
 
EC50(11)
 
 
 
AC50(8)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 655    Data Row: 655   Total Pages: 14   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID17386900]
EC50 1.904Inhibitors of T-Type Calcium Channels [AID493021, Type: confirmatory]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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2
[SID17386900]
EC50 1.904Inhibitors of T-Type Calcium Channels [AID493021, Type: confirmatory]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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3
[SID17386900]
EC50 1.904Inhibitors of T-Type Calcium Channels [AID493021, Type: confirmatory]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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4
[SID17386900]
EC50 2.71Inhibitors of T-Type Calcium Channel [AID489005, Type: confirmatory]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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5
[SID17386900]
EC50 2.71Inhibitors of T-Type Calcium Channel [AID489005, Type: confirmatory]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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6
[SID17386900]
EC50 2.71Inhibitors of T-Type Calcium Channel [AID489005, Type: confirmatory]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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7
[SID17386900]
Potency 10qHTS Assay for Identifying the Cell-Membrane Permeable IMPase Inhibitors: Potentiation with Lithium [AID1457, Type: confirmatory]Inositol monophosphatase [gi:44888968]
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8
[SID17386900]
Potency 10qHTS Assay for Identifying the Cell-Membrane Permeable IMPase Inhibitors: Potentiation with Lithium [AID1457, Type: confirmatory]Inositol monophosphatase [gi:44888968]
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9
[SID17386900]
Potency 12.5893Quantitative High-Throughput Screen for Regulators of Epigenetic Control [AID1865, Type: confirmatory]
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10
[SID17386900]
AC50 16.118C-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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11
[SID17386900]
EC50 17.4Dose response confirmation uHTS hits for MazEF TA System activators via a fluorescence-based single-stranded RNase assay [AID588481, Type: confirmatory]mRNA interferase toxin, antitoxin is MazE [Escherichia coli str. K-12 substr. MG1655] [gi:16130689]
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12
[SID124360081]
AC50 19.4C-LANA Counter Screen: DNA intercalators Measured in Biochemical System Using Plate Reader - 2117-02_Inhibitor_Dose_DryPowder_Activity [AID588364, Type: confirmatory]
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13
[SID17386900]
AC50 20.177C-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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14
[SID124360081]
AC50 23.05C-LANA FP assay Measured in Biochemical System Using Plate Reader - 2117-01_Inhibitor_Dose_DryPowder_Activity [AID588363, Type: confirmatory]LANA [Human herpesvirus 8] [gi:312275222]
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15
[SID17386900]
AC50 95.92724 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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16
[SID17386900]
AC50 98.56Inhibitors of Mycobacterium tuberculosis UDP-galactopyranose mutase (UGM) enzyme Measured in Biochemical System Using Plate Reader - 2105-02_Inhibitor_Dose_CherryPick_Activity [AID540359, Type: confirmatory]glf gene product [Mycobacterium tuberculosis H37Rv] [gi:15610945]
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17
[SID17386900]
 Inhibitors of Mycobacterium tuberculosis UDP-galactopyranose mutase (UGM) enzyme - High throughput screening using Fluorescent polarization assay Measured in Biochemical System Using Plate Reader - 2105-01_Inhibitor_SinglePoint_HTS_Activity_Set6 [AID504406, Type: screening]glf gene product [Mycobacterium tuberculosis H37Rv] [gi:15610945]
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18
[SID17386900]
 Fluorescence-based biochemical primary high throughput screening assay to identify activators of the calcium sensitivity of cardiac Regulated Thin Filaments (RTF) [AID493008, Type: screening]cardiac alpha tropomyosin [Sus scrofa] [gi:1927]
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19
[SID17386900]
 uHTS identification of MazEF TA System activators via a fluorescence-based single-stranded RNase assay [AID504720, Type: screening]mRNA interferase toxin, antitoxin is MazE [Escherichia coli str. K-12 substr. MG1655] [gi:16130689]
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20
[SID17386900]
 High-content cell-based screening for modulators of autophagy [AID463193, Type: screening]microtubule-associated proteins 1A/1B light chain 3A isoform b [Homo sapiens] [gi:31563518]
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21
[SID17386900]
 Inhibitors of Cav3 T-type Calcium Channels: Primary Screen [AID449739, Type: screening]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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22
[SID17386900]
 Inhibitors of Cav3 T-type Calcium Channels: Primary Screen [AID449739, Type: screening]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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23
[SID17386900]
 Inhibitors of Cav3 T-type Calcium Channels: Primary Screen [AID449739, Type: screening]voltage-dependent T-type calcium channel subunit alpha-1H isoform a [Homo sapiens] [gi:53832009]
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24
[SID17386900]
Potency qHTS of IL-2 Activators [AID652025, Type: confirmatory]Il2 gene product [Mus musculus] [gi:7110653]
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25
[SID17386900]
 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_SinglePoint_HTS_Activity [AID504523, Type: screening]KEAP1 gene product [Homo sapiens] [gi:45269145]
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26
[SID17386900]
 Fluorescence polarization to screen for inhibitors that disrupt the protein-protein interaction between Keap1 and Nrf2 Measured in Biochemical System Using Plate Reader - 2119-01_Inhibitor_SinglePoint_HTS_Activity [AID504523, Type: screening]KEAP1 gene product [Homo sapiens] [gi:45269145]
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27
[SID17386900]
 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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28
[SID17386900]
 Primary biochemical high-throughput screening assay for inhibitors of the HIV Rev RRE RNA interaction (disruption of protein-RNA interaction) [AID704, Type: screening]Chain B, Rna Aptamer Complexed With Hiv-1 Rev Peptide, Nmr, 7 Structures [gi:253722402]
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29
[SID17386900]
 HTS Assay for Inhibitors of Akt Phophorylation: Primary Screen [AID651550, Type: screening]RAC-alpha serine/threonine-protein kinase [gi:60391226]
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30
[SID17386900]
 HTS Assay for Inhibitors of Akt Phophorylation: Primary Screen [AID651550, Type: screening]RAC-alpha serine/threonine-protein kinase [gi:60391226]
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31
[SID17386900]
 HTS Assay for Inhibitors of Akt Phophorylation: Primary Screen [AID651550, Type: screening]RAC-alpha serine/threonine-protein kinase [gi:60391226]
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32
[SID17386900]
 TRFRET-based cell-based primary high throughput screening assay to identify biased ligands of the melanocortin 4 receptor (MC4R): antagonists of MC4R [AID540295, Type: screening]melanocortin receptor 4 [Homo sapiens] [gi:119508433]
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33
[SID17386900]
 TRFRET-based cell-based primary high throughput screening assay to identify biased ligands of the melanocortin 4 receptor (MC4R): antagonists of MC4R [AID540295, Type: screening]melanocortin receptor 4 [Homo sapiens] [gi:119508433]
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34
[SID17386900]
 Modulators of the EP2 prostaglandin E2 receptor - Primary Screening [AID940, Type: screening]prostaglandin E receptor 2 (subtype EP2), 53kDa [Homo sapiens] [gi:31881630]
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35
[SID17386900]
 Modulators of the EP2 prostaglandin E2 receptor - Primary Screening [AID940, Type: screening]prostaglandin E receptor 2 (subtype EP2), 53kDa [Homo sapiens] [gi:31881630]
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36
[SID17386900]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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37
[SID17386900]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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38
[SID17386900]
 Assay for HTS of Gi/Go-linked GPCRs using mGluR8: Primary Screening [AID488969, Type: screening]metabotropic glutamate receptor 8 [Rattus norvegicus] [gi:1575471]
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39
[SID17386900]
 Assay for HTS of Gi/Go-linked GPCRs using mGluR8: Primary Screening [AID488969, Type: screening]metabotropic glutamate receptor 8 [Rattus norvegicus] [gi:1575471]
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40
[SID17386900]
 Assay for HTS of Gi/Go-linked GPCRs using mGluR8: Primary Screening [AID488969, Type: screening]metabotropic glutamate receptor 8 [Rattus norvegicus] [gi:1575471]
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41
[SID17386900]
Potency 1.8526Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation [AID504834, Type: confirmatory]
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42
[SID17386900]
Potency 4.4668qHTS of GLP-1 Receptor Inverse Agonists: Cytotox Screen [AID624418, Type: confirmatory]
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43
[SID17386900]
Max_Activity_Concentration_uM 12Thermal shift assay to identify compound binding to Kelch domain of Keap1 protein Measured in Biochemical System Using RT-PCR - 2119-02_Inhibitor_Dose_CherryPick_Activity [AID651823, Type: confirmatory]KEAP1 gene product [Homo sapiens] [gi:45269145]
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44
[SID17386900]
Max_Activity_Concentration_uM 12Thermal shift assay to identify compound binding to Kelch domain of Keap1 protein Measured in Biochemical System Using RT-PCR - 2119-02_Inhibitor_Dose_CherryPick_Activity [AID651823, Type: confirmatory]KEAP1 gene product [Homo sapiens] [gi:45269145]
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45
[SID17386900]
Potency 25.1189qHTS for Inhibitors of ATXN expression [AID651635, Type: confirmatory]ATXN2 gene product [Homo sapiens] [gi:171543895]
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46
[SID17386900]
EC50 99Dose response confirmation uHTS hits for MazEF TA System activators via a fluorescence-based single-stranded RNase assay counterscreen [AID588502, Type: confirmatory]mRNA interferase toxin, antitoxin is MazE [Escherichia coli str. K-12 substr. MG1655] [gi:16130689]
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47
[SID17386900]
Potency 112.202qHTS for Inhibitors of Polymerase Iota [AID588590, Type: confirmatory]DNA polymerase iota [Homo sapiens] [gi:154350220]
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48
[SID17386900]
Potency 112.202qHTS for Inhibitors of Polymerase Iota [AID588590, Type: confirmatory]DNA polymerase iota [Homo sapiens] [gi:154350220]
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49
[SID17386900]
 HTS for small molecule inhibitors of CHOP to regulate the unfolded protein response to ER stress [AID2732, Type: screening]Ddit3 gene product [Mus musculus] [gi:160707929]
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50
[SID17386900]
 uHTS for Small Molecule Inhibitors of Eukaryotic Translation Initiation [AID782, Type: screening]eukaryotic translation initiation factor 4E [Mus musculus] [gi:83627717]
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