MLS003124308 (CID 49786875) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(12)
 
 
Inactive(140)
 
 
Inconclusive(5)
 
 
Top Targets:
7TM GPCR Srx(8)
 
 
7TM GPCR Srsx(4)
 
 
NR DBD CAR(3)
 
 
Bromo SNF2L2(3)
 
 
 
APPBP1 RUB(3)
 
 
 
BioAssay Types:
Screening(124)
 
 
 
 
Confirmatory(27)
 
 
 
 
Literature(3)
 
 
BioActivity Types:
Potency(24)
 
 
 
 
EC50(2)
 
 
IC50(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 157    Data Row: 157   Total Pages: 4   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103060846]
Potency 4.6109qHTS 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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2
[SID103060846]
Potency 4.6109qHTS 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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3
[SID103060846]
Potency 4.6109qHTS 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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4
[SID103060846]
Potency 5.1735qHTS 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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5
[SID103060846]
Potency 5.1735qHTS 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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6
[SID103060846]
Potency 5.1735qHTS 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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7
[SID103060846]
Potency 23.1093qHTS 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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8
[SID103060846]
Potency 35.4813qHTS for Inhibitors of ATXN expression [AID651635, Type: confirmatory]ATXN2 gene product [Homo sapiens] [gi:171543895]
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9
[SID103060846]
 Single concentration confirmation of inhibitors of cullin neddylation in a TR-FRET assay [AID652217, Type: screening]NAE1 gene product [Homo sapiens] [gi:4502169]
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10
[SID103060846]
 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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11
[SID103060846]
 Fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of ArfGAP with SH3 domain, ankyrin repeat and PH domain 1 (ASAP1) [AID624431, Type: screening]ASAP1 gene product [Homo sapiens] [gi:351542238]
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12
[SID103060846]
 uHTS identification of CXCR6 Inhibitors in a B-arrestin luminescence assay [AID602244, Type: screening]CXCR6 gene product [Homo sapiens] [gi:5730106]
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13
[SID103060846]
 uHTS identification of CXCR6 Inhibitors in a B-arrestin luminescence assay [AID602244, Type: screening]CXCR6 gene product [Homo sapiens] [gi:5730106]
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14
[SID103060846]
 uHTS identification of inhibitors of cullin neddylation in a TR-FRET assay [AID651699, Type: screening]NAE1 gene product [Homo sapiens] [gi:4502169]
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15
[SID103060846]
 Inhibition of the MLL-AF4-AF9 Interaction in Pediatric Leukemia Measured in Biochemical System Using Plate Reader - 2160-01_Inhibitor_SinglePoint_HTS_Activity [AID651704, Type: screening]MLLT3 gene product [Homo sapiens] [gi:156104889]
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16
[SID103060846]
 Luminescence-based cell-based primary high throughput confirmation assay to identify activators of the function of SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2 (SMARCA2, BRM) [AID652260, Type: screening]SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2, i [gi:119579215]
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17
[SID103060846]
 Luminescence-based cell-based primary high throughput screening assay to identify activators of the function of SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2 (SMARCA2, BRM) [AID652017, Type: screening]SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2, i [gi:119579215]
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18
[SID103060846]
Potency 15.8489qHTS for Inhibitors of TGF-b: Cytotox Counterscreen [AID588856, Type: confirmatory]
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19
[SID103060846]
IC50 49.9Dose-response confirmation of inhibitors of cullin neddylation in a TR-FRET assay [AID652247, Type: confirmatory]NAE1 gene product [Homo sapiens] [gi:4502169]
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20
[SID103060846]
EC50 91.18Luminescence-based cell-based high throughput dose response assay to identify activators of the function of SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2 (SMARCA2, BRM) [AID686991, Type: confirmatory]
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21
[SID103060846]
EC50 91.18Counterscreen for activators of the function of SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2 (SMARCA2, BRM): Luminescence-based cell-based high throughput dose response assay to identify non-selective compounds using the VP16 reporter assay [AID686995, Type: confirmatory]
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22
[SID103060846]
 VEID(2) R110 Enzymatic Primary HTS to identify Inhibitors of Caspase 6 Measured in Biochemical System Using Plate Reader - 7052-01_Inhibitor_SinglePoint_HTS_Activity_Set2 [AID686996, Type: screening]
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23
[SID103060846]
 Luminescence-based cell-based primary high throughput screening assay to identify biased ligands of the melanocortin 4 receptor (MC4R): agonists of MC4R [AID540308, Type: screening]melanocortin receptor 4 [Homo sapiens] [gi:119508433]
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24
[SID103060846]
 Luminescence-based cell-based primary high throughput screening assay to identify biased ligands of the melanocortin 4 receptor (MC4R): agonists of MC4R [AID540308, Type: screening]melanocortin receptor 4 [Homo sapiens] [gi:119508433]
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25
[SID103060846]
 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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26
[SID103060846]
 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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27
[SID103060846]
 TRFRET-based biochemical primary high throughput screening assay to identify inhibitors of 5-meCpG-binding domain protein 2 (MBD2)-DBD binding to methylated oligonucleotide [AID686964, Type: screening]Methyl-CpG binding domain protein 2 [Homo sapiens] [gi:21595776]
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28
[SID103060846]
 uHTS identification of small molecule activators of alpha dystroglycan glycosylation [AID624168, Type: screening]LARGE [Homo sapiens] [gi:47678551]
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29
[SID103060846]
 Luminescence-based cell-based high throughput primary screening assay to identify agonists of nuclear receptor subfamily 2, group E, member 3 (NR2E3) [AID602229, Type: screening]photoreceptor-specific nuclear receptor [Homo sapiens] [gi:216409728]
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30
[SID103060846]
 Luminescence-based cell-based high throughput primary screening assay to identify agonists of nuclear receptor subfamily 2, group E, member 3 (NR2E3) [AID602229, Type: screening]photoreceptor-specific nuclear receptor [Homo sapiens] [gi:216409728]
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31
[SID103060846]
 Luminescence-based cell-based high throughput primary screening assay to identify agonists of nuclear receptor subfamily 2, group E, member 3 (NR2E3) [AID602229, Type: screening]photoreceptor-specific nuclear receptor [Homo sapiens] [gi:216409728]
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32
[SID103060846]
 Flow Cytometric HTS Screen for inhibitors of the ABC transporter ABCB6 for MLPCN Compound Set [AID602162, Type: screening]ABCB6 gene product [Homo sapiens] [gi:9955963]
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33
[SID103060846]
 Turbidometric Biochemical Primary HTS to identify inhibitors of ERp5 Measured in Biochemical System Using Plate Reader - 7002-01_Inhibitor_SinglePoint_HTS_Activity [AID651711, Type: screening]Protein disulfide-isomerase A6 [gi:2501205]
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34
[SID103060846]
 uHTS identification of inhibitors of Rpn11 in a Fluorescent Polarization assay [AID588493, Type: screening]PSMD14 protein [Homo sapiens] [gi:16306916]
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35
[SID103060846]
 Luminescence-based cell-based primary high throughput screening assay to identify inhibitors of the Steroid Receptor Coactivator 2 (SRC2; NCOA2) [AID651957, Type: screening]NCOA2 gene product [Homo sapiens] [gi:5729858]
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36
[SID103060846]
 Luminescence-based cell-based primary high throughput screening assay to identify inhibitors of the Steroid Receptor Coactivator 2 (SRC2; NCOA2) [AID651957, Type: screening]NCOA2 gene product [Homo sapiens] [gi:5729858]
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37
[SID103060846]
 Single concentration confirmation of uHTS hits from a small molecule antagonists of the CXCR6 receptor via a luminescent beta-arrestin assay [AID602409, Type: screening]CXCR6 gene product [Homo sapiens] [gi:5730106]
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38
[SID103060846]
 Single concentration confirmation of uHTS hits from a small molecule antagonists of the CXCR6 receptor via a luminescent beta-arrestin assay [AID602409, Type: screening]CXCR6 gene product [Homo sapiens] [gi:5730106]
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39
[SID103060846]
 qHTS Assay for Inhibitors of the Six1/Eya2 Interaction [AID651725, Type: screening]six1 [Homo sapiens] [gi:1246761]
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40
[SID103060846]
 Luminescence-based biochemical primary high throughput screening assay to identify inhibitors of the interaction of the lipase co-activator protein, abhydrolase domain containing 5 (ABHD5) with perilipin-5 (MLDP; PLIN5) [AID602281, Type: screening]ABHD5 gene product [Homo sapiens] [gi:31542303]
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41
[SID103060846]
 MLPCN ERAP1 Measured in Biochemical System Using Plate Reader - 7016-01_Inhibitor_SinglePoint_HTS_Activity [AID652197, Type: screening]ERAP1 protein [Homo sapiens] [gi:21315078]
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42
[SID103060846]
 MLPCN ERAP1 Measured in Biochemical System Using Plate Reader - 7016-01_Inhibitor_SinglePoint_HTS_Activity [AID652197, Type: screening]ERAP1 protein [Homo sapiens] [gi:21315078]
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43
[SID103060846]
 uHTS identification of small molecule inhibitors of Csn-mediated Deneddylation of Cullin-Ring Ligases, vis a fluorescence polarization assay [AID651999, Type: screening]COPS5 gene product [Homo sapiens] [gi:38027923]
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44
[SID103060846]
 Luminescence-based cell-based primary high throughput screening assay to identify agonists of the mouse 5-hydroxytryptamine (serotonin) receptor 2A (HTR2A) [AID624169, Type: screening]Htr2a gene product [Mus musculus] [gi:27753985]
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45
[SID103060846]
 Luminescence-based cell-based primary high throughput screening assay to identify agonists of the mouse 5-hydroxytryptamine (serotonin) receptor 2A (HTR2A) [AID624169, Type: screening]Htr2a gene product [Mus musculus] [gi:27753985]
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46
[SID103060846]
Potency qHTS of IL-2 Activators [AID652025, Type: confirmatory]Il2 gene product [Mus musculus] [gi:7110653]
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47
[SID103060846]
 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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48
[SID103060846]
Potency qHTS of TDP-43 Inhibitors [AID652104, Type: confirmatory]TAR DNA-binding protein 43 [gi:20140568]
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49
[SID103060846]
 uHTS identification of microRNA-mediated mRNA deadenylation inhibitors by fluoresence polarization assay [AID588489, Type: screening]polyadenylate-binding protein 1 [Homo sapiens] [gi:46367787]
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50
[SID103060846]
 Small Molecule Inhibitors of FGF22-Mediated Excitatory Synaptogenesis & Epilepsy Measured in Biochemical System Using RT-PCR - 7012-01_Inhibitor_SinglePoint_HTS_Activity [AID651658, Type: screening]FGF22 gene product [Homo sapiens] [gi:10190672]
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