AK-968/41025379 (CID 6874905) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(72)
 
 
Inactive(567)
 
 
Inconclusive(37)
 
 
Unspecified(2)
 
 
Top Targets:
7TM GPCR Srx(19)
 
 
Bcl-2 like(15)
 
 
 
alkPPc(12)
 
 
7TM GPCR Srsx(8)
 
 
UBCc(8)
 
 
 
BioAssay Types:
Screening(448)
 
 
 
 
 
Confirmatory(214)
 
 
 
 
 
Literature(5)
 
 
BioActivity Types:
Potency(138)
 
 
 
 
 
IC50(62)
 
 
 
EC50(8)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 673    Data Row: 678   Total Pages: 14   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID17409043]
Potency 0.5358qHTS 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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2
[SID56373716]
IC50 1.38SAR analysis of the MOA of E2 SUMOylation inhibitors in an HTRF format [AID485393, Type: confirmatory]SUMO-conjugating enzyme UBC9 [Homo sapiens] [gi:4507785]
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3
[SID17409043]
IC50 1.66718Dose Response Confirmation for Mcl-1/Noxa Interaction Inhibitors [AID1417, Type: confirmatory]Mcl-1 [Homo sapiens] [gi:7582271]
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4
[SID17409043]
IC50 1.66718Dose Response Confirmation for Mcl-1/Noxa Interaction Inhibitors [AID1417, Type: confirmatory]Mcl-1 [Homo sapiens] [gi:7582271]
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5
[SID17409043]
IC50 1.66718Dose Response Confirmation for Mcl-1/Noxa Interaction Inhibitors [AID1417, Type: confirmatory]Mcl-1 [Homo sapiens] [gi:7582271]
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6
[SID85256229]
IC50 1.83SAR analysis of the MOA of E2 SUMOylation inhibitors in an HTRF format [AID485393, Type: confirmatory]SUMO-conjugating enzyme UBC9 [Homo sapiens] [gi:4507785]
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7
[SID17409043]
Potency 2.2387qHTS for Inhibitors of Polymerase Eta [AID588591, Type: confirmatory]DNA polymerase eta [Homo sapiens] [gi:5729982]
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8
[SID17409043]
Potency 2.2387qHTS for Inhibitors of Polymerase Eta [AID588591, Type: confirmatory]DNA polymerase eta [Homo sapiens] [gi:5729982]
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9
[SID17409043]
IC50 2.253TR-FRET counterscreen for FAK inhibitors: dose-response biochemical high throughput screening assay to identify inhibitors of Proline-rich tyrosine kinase 2 (Pyk2) [AID1641, Type: confirmatory]PTK2B protein tyrosine kinase 2 beta [Homo sapiens] [gi:34784998]
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10
[SID17409043]
IC50 2.253TR-FRET counterscreen for FAK inhibitors: dose-response biochemical high throughput screening assay to identify inhibitors of Proline-rich tyrosine kinase 2 (Pyk2) [AID1641, Type: confirmatory]PTK2B protein tyrosine kinase 2 beta [Homo sapiens] [gi:34784998]
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11
[SID17409043]
IC50 2.253TR-FRET counterscreen for FAK inhibitors: dose-response biochemical high throughput screening assay to identify inhibitors of Proline-rich tyrosine kinase 2 (Pyk2) [AID1641, Type: confirmatory]PTK2B protein tyrosine kinase 2 beta [Homo sapiens] [gi:34784998]
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12
[SID17409043]
IC50 3.18Homogeneous Time-Resolved Fluorescence Resonance Energy Transfer (HTRF) Assay [AID2073, Type: confirmatory]Mint1 [Rattus norvegicus] [gi:2625023]
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13
[SID17409043]
IC50 3.61Dose Response Confirmation for Small Molecule Inhibitors of Epstein-Barr Virus [AID1419, Type: confirmatory]BZLF2 [Human herpesvirus 4 type 2] [gi:139424501]
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14
[SID17409043]
Potency 4.4668qHTS 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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15
[SID85256229]
IC50 4.79SAR analysis of small molecule inhibitors of Mint-PDZ and N-type Ca2+ channel carboxyl-terminal peptide association using HTRF - Set 2 [AID434980, Type: confirmatory]Mint1 [Rattus norvegicus] [gi:2625023]
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16
[SID17409043]
IC50 4.81Dose response confirmation of DNMT1 inhibitors in a Fluorescent Molecular Beacon assay [AID602386, Type: confirmatory]DNA (cytosine-5)-methyltransferase 1 isoform b [Homo sapiens] [gi:4503351]
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17
[SID17409043]
IC50 4.81Dose response confirmation of DNMT1 inhibitors in a Fluorescent Molecular Beacon assay [AID602386, Type: confirmatory]DNA (cytosine-5)-methyltransferase 1 isoform b [Homo sapiens] [gi:4503351]
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18
[SID17409043]
Potency 5.6234qHTS Assay for the Inhibitors of L3MBTL1 [AID485360, Type: confirmatory]lethal(3)malignant brain tumor-like protein 1 isoform I [Homo sapiens] [gi:117938328]
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19
[SID17409043]
Potency 5.6234qHTS Assay for the Inhibitors of L3MBTL1 [AID485360, Type: confirmatory]lethal(3)malignant brain tumor-like protein 1 isoform I [Homo sapiens] [gi:117938328]
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20
[SID17409043]
Potency 5.7591qHTS Confirmation Assay for Inhibitors of Bloom's syndrome helicase (BLM) [AID2585, Type: confirmatory]Bloom syndrome protein [Homo sapiens] [gi:4557365]
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21
[SID17409043]
Potency 5.7988qHTS for inhibitors of Phosphogylcerate Kinase: Hit Validation Screen [AID686980, Type: confirmatory]phosphoglycerate kinase [Trypanosoma brucei] [gi:115503961]
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22
[SID17409043]
Potency 6.3096qHTS Assay for Inhibitors of BAZ2B [AID504333, Type: confirmatory]bromodomain adjacent to zinc finger domain 2B [Homo sapiens] [gi:6683500]
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23
[SID56373716]
IC50 7.16SAR analysis of SUMOylation using HTRF in an in-Vitro dose response assay [AID2614, Type: confirmatory]SUMO-conjugating enzyme UBC9 [Homo sapiens] [gi:4507785]
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24
[SID17409043]
IC50 7.186Fluorescence polarization-based biochemical high throughput dose response assay for inhibitors of myeloid cell leukemia sequence 1 (MCL1) interactions with BIM-BH3 peptide. [AID2217, Type: confirmatory]Myeloid cell leukemia sequence 1 (BCL2-related) [Homo sapiens] [gi:78070770]
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25
[SID17409043]
IC50 7.186Fluorescence polarization-based biochemical high throughput dose response assay for inhibitors of myeloid cell leukemia sequence 1 (MCL1) interactions with BIM-BH3 peptide. [AID2217, Type: confirmatory]Myeloid cell leukemia sequence 1 (BCL2-related) [Homo sapiens] [gi:78070770]
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26
[SID17409043]
IC50 7.186Fluorescence polarization-based biochemical high throughput dose response assay for inhibitors of myeloid cell leukemia sequence 1 (MCL1) interactions with BIM-BH3 peptide. [AID2217, Type: confirmatory]Myeloid cell leukemia sequence 1 (BCL2-related) [Homo sapiens] [gi:78070770]
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27
[SID17409043]
IC50 7.33Dose response confirmation of uHTS inhibitor hits from NadD in a Colorimetric assay [AID624317, Type: confirmatory]hypothetical protein SA1422 [Staphylococcus aureus subsp. aureus N315] [gi:15927174]
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28
[SID17409043]
IC50 8.21uHTS Homogeneous Terbium Time-Resolved Fluorescence Resonance Energy Transfer (HTRF) Assay [AID2091, Type: confirmatory]Mint1 [Rattus norvegicus] [gi:2625023]
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29
[SID85256229]
IC50 8.96SAR analysis of small molecule inhibitors of Mint-PDZ and N-type Ca2+ channel carboxyl-terminal peptide association using HTRF [AID2489, Type: confirmatory]Mint1 [Rattus norvegicus] [gi:2625023]
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30
[SID85256229]
IC50 9.07SAR analysis of SUMOylation using HTRF in an in-Vitro dose response assay [AID2614, Type: confirmatory]SUMO-conjugating enzyme UBC9 [Homo sapiens] [gi:4507785]
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31
[SID17409043]
Potency 10.3225qHTS 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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32
[SID17409043]
Potency 10.3225qHTS 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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33
[SID17409043]
Potency 10.3225qHTS 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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34
[SID17409043]
Potency 11.2202qHTS Assay for Inhibitors of Bloom's syndrome helicase (BLM) [AID2528, Type: confirmatory]Bloom syndrome protein [Homo sapiens] [gi:4557365]
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35
[SID17409043]
Potency 12.5893qHTS for Inhibitors of Glutaminase (GLS) [AID624170, Type: confirmatory]GLS protein [Homo sapiens] [gi:71051501]
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36
[SID56373716]
IC50 12.9SAR analysis of small molecule inhibitors of Mint-PDZ and N-type Ca2+ channel carboxyl-terminal peptide association using HTRF - Set 2 [AID434980, Type: confirmatory]Mint1 [Rattus norvegicus] [gi:2625023]
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37
[SID17409043]
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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38
[SID17409043]
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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39
[SID17409043]
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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40
[SID17409043]
Potency 16.3601qHTS for induction of synthetic lethality in tumor cells producing 2HG: qHTS for the HT-1080-IDH1KD cell line [AID686971, Type: confirmatory]
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41
[SID17409043]
Potency 17.7828qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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42
[SID17409043]
Potency 17.7828qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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43
[SID17409043]
IC50 21.1Dose response confirmation of uHTS inhibitor hits from NadD in a Colorimetric assay - Set 2 [AID651709, Type: confirmatory]hypothetical protein SA1422 [Staphylococcus aureus subsp. aureus N315] [gi:15927174]
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44
[SID17409043]
Potency 22.3872qHTS 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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45
[SID85256229]
IC50 23.3SAR analysis of Ubc13-Ubiquitination selectivity in a TR-FRET assay for In Vitro dose response studies [AID2658, Type: confirmatory]UBE2N gene product [Homo sapiens] [gi:4507793]
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46
[SID85256229]
IC50 23.3SAR analysis of Ubc13-Ubiquitination selectivity in a TR-FRET assay for In Vitro dose response studies [AID2658, Type: confirmatory]UBE2N gene product [Homo sapiens] [gi:4507793]
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47
[SID56373716]
IC50 25.8SAR analysis of Ubc13-Ubiquitination selectivity in a TR-FRET assay for In Vitro dose response studies [AID2658, Type: confirmatory]UBE2N gene product [Homo sapiens] [gi:4507793]
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48
[SID56373716]
IC50 25.8SAR analysis of Ubc13-Ubiquitination selectivity in a TR-FRET assay for In Vitro dose response studies [AID2658, Type: confirmatory]UBE2N gene product [Homo sapiens] [gi:4507793]
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49
[SID17409043]
Potency 28.1838HTS 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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50
[SID17409043]
Potency 28.1838Confirmation qHTS Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) [AID2708, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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