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CHEMBL1543343 (CID 3162043) - Compound BioActivity Data
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BioActivity Outcomes:
Active(8)
 
 
Inactive(524)
 
 
Inconclusive(9)
 
 
Unspecified(3)
 
 
Top Targets:
7TM GPCR Srx(21)
 
 
7TM GPCR Srsx(15)
 
 
STKc AGC(10)
 
 
 
STKc PKA(5)
 
 
CAP ED(5)
 
 
BioAssay Types:
Screening(364)
 
 
 
Confirmatory(166)
 
 
 
 
 
Literature(8)
 
 
 
 
BioActivity Types:
Potency(122)
 
 
 
 
 
IC50(30)
 
 
 
 
AC50(9)
 
 
 
EC50(5)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 499    Data Row: 544   Total Pages: 11   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID163319244]
IC50 0.28Inhibition of N-terminal 6His-tagged full length human recombinant STK33 using myelin basic protein as substrate incubated for 15 mins before initiation of kinase reaction measured after 1 hr by ADP-glo assay [AID712545, Type: Literature]Serine/threonine-protein kinase 33 [gi:74761329]
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2
[SID125081988]
AC50_uM 0.285STK-33 Kinase Inhibition Measured in Biochemical System Using Plate Reader - 2052-02_Inhibitor_Dose_DryPowder_Activity_Set2 [AID588480, Type: confirmatory]serine/threonine-protein kinase 33 isoform a [Homo sapiens] [gi:23943882]
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3
[SID99351038]
AC50_uM 0.308STK-33 Kinase Inhibition Measured in Biochemical System Using Plate Reader - 2052-02_Inhibitor_Dose_DryPowder_Activity_Set2 [AID588480, Type: confirmatory]serine/threonine-protein kinase 33 isoform a [Homo sapiens] [gi:23943882]
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4
[SID99351038]
AC50_uM 0.331STK-33 Kinase Inhibition Measured in Biochemical System Using Plate Reader - 2052-02_Inhibitor_Dose_DryPowder_Activity [AID588632, Type: confirmatory]serine/threonine-protein kinase 33 isoform a [Homo sapiens] [gi:23943882]
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5
[SID49680978]
EC50_uM 2.102Luminescence Cell-Free Homogenous Dose Retest to Identify Inhibitors of Serine/Threonine Kinase 33 Activity [AID2821, Type: confirmatory]serine/threonine-protein kinase 33 isoform a [Homo sapiens] [gi:23943882]
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6
[SID49680978]
Potency 9.2qHTS Assay for Lipid Storage Modulators in Drosophila S3 Cells [AID2685, Type: confirmatory]
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7
[SID173334081]
Confirmed inhibitors of Serine Threonine Kinase 33, STK33 [AID743321, Type: other]serine/threonine-protein kinase 33 isoform a [Homo sapiens] [gi:23943882]
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8
[SID49680978]
Luminescence Cell-Free Homogenous Primary HTS to Identify Inhibitors of Serine/Threonine Kinase 33 Activity [AID2661, Type: screening]serine/threonine-protein kinase 33 isoform a [Homo sapiens] [gi:23943882]
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9
[SID163319244]
IC50 10Inhibition of His-tagged recombinant catalytic fragment of PKA assessed as phosphorylation of fluorescent-labeled peptide 21substrate by caliper capillary electrophoresis [AID712541, Type: Literature]
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10
[SID163319244]
Selectivity ratio of IC50 for His-tagged recombinant catalytic fragment of PKA to IC50 for N-terminal 6His-tagged full length human recombinant STK33 [AID712544, Type: Literature]
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11
[SID49680978]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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12
[SID49680978]
Potency 0.0752qHTS 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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13
[SID49680978]
Potency 2.8184qHTS of GLP-1 Receptor Inverse Agonists (Inhibition Mode) [AID624417, Type: confirmatory]glp-1 receptor [Homo sapiens] [gi:1724069]
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14
[SID49680978]
qHTS Assay for Inhibitors of the CtBP/E1A Interaction [AID651724, Type: screening]CtBP interacting protein CtIP [Homo sapiens] [gi:1730321]
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15
[SID49680978]
uHTS identification of SUMO1-mediated protein-protein interactions [AID602429, Type: screening]SUMO-1 [Homo sapiens] [gi:1762973]
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16
[SID49680978]
Fluorescence polarization to screen for inhibitor that competite the binding of FadD28 to bisubstrate Measured in Biochemical System Using Plate Reader - 2147-01_Inhibitor_SinglePoint_HTS_Activity [AID588549, Type: screening]FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) (FATTY-ACID-CoA SYNTHASE) [Mycobacterium tuberculosis H37Rv] [gi:1781172]
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17
[SID49680978]
Fluorescence-based biochemical primary high throughput assay to identify inhibitors of T-cell receptor (TCR)-CD3 interaction using a TAMRA-labeled TCR probe [AID651800, Type: screening]TCRAV4S1 [Homo sapiens] [gi:2358024]
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18
[SID49680978]
QFRET-based biochemical primary high throughput screening assay to identify exosite inhibitors of ADAM10. [AID720582, Type: screening]ADAM10 [Homo sapiens] [gi:2393947]
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19
[SID49680978]
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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20
[SID49680978]
IC50 Homogeneous Time-Resolved Fluorescence Resonance Energy Transfer (HTRF) Assay [AID2073, Type: confirmatory]Mint1 [Rattus norvegicus] [gi:2625023]
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21
[SID49680978]
TRFRET-based biochemical primary high throughput screening assay to identify inhibitors of HIV-1 LEDGF/p75 DNA Integration [AID743269, Type: screening]integrase [Human immunodeficiency virus 1] [gi:2853980]
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22
[SID49680978]
Primary cell-based high-throughput screening assay for identification of compounds that allosterically potentiate transient receptor potential cation channel C4 (TRPC4) [AID2227, Type: screening]alternatively spliced Trp4 [Mus musculus] [gi:2935630]
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23
[SID49680978]
Primary cell-based screen for identification of compounds that inhibit transient receptor potential cation channel C4 (TRPC4). [AID2247, Type: screening]alternatively spliced Trp4 [Mus musculus] [gi:2935630]
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24
[SID49680978]
Primary cell-based screen for identification of compounds that activate transient receptor potential cation channel C4 (TRPC4). [AID2237, Type: screening]alternatively spliced Trp4 [Mus musculus] [gi:2935630]
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25
[SID49680978]
Potency A Quantitative High throughput Screen to Identify Chemical Modulators of PINK1 Expression [AID624263, Type: confirmatory]Parkin [Homo sapiens] [gi:3063388]
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26
[SID49680978]
Potency qHTS for Inhibitors of WRN Helicase [AID651768, Type: confirmatory]WRN [Homo sapiens] [gi:3719421]
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27
[SID49680978]
Potency Inhibitors of TCP-1 ring complex (TRiC) of Methanococcus maripaludis (MmCpn): qHTS [AID504842, Type: confirmatory]chaperonin-containing TCP-1 beta subunit homolog [Homo sapiens] [gi:4090929]
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28
[SID49680978]
HTS for Beta-2AR agonists via FAP method [AID504454, Type: screening]beta-2 adrenergic receptor [Homo sapiens] [gi:4501969]
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29
[SID49680978]
Potency qHTS assay of beta-arrestin-biased ligands of beta2-adrenergic receptor [AID492947, Type: confirmatory]beta-2 adrenergic receptor [Homo sapiens] [gi:4501969]
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30
[SID49680978]
Luminescence-based primary cell-based high throughput screening assay to identify activators of the Aryl Hydrocarbon Receptor (AHR) [AID2796, Type: screening]aryl hydrocarbon receptor precursor [Homo sapiens] [gi:4502003]
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31
[SID49680978]
uHTS identification of inhibitors of cullin neddylation in a TR-FRET assay [AID651699, Type: screening]NEDD8-activating enzyme E1 regulatory subunit isoform a [Homo sapiens] [gi:4502169]
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32
[SID49680978]
Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based primary cell-based high throughput assay to identify agonists of the vasopressin 1 receptor (V1R) [AID2797, Type: screening]vasopressin V1a receptor [Homo sapiens] [gi:4502331]
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33
[SID49680978]
IC50 Homogeneous Time-Resolved Fluorescence Resonance Energy Transfer (HTRF) Assay [AID2073, Type: confirmatory]voltage-dependent N-type calcium channel subunit alpha-1B isoform 1 [Homo sapiens] [gi:4502523]
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34
[SID49680978]
uHTS identification of DNMT1 inhibitors in a Fluorescent Molecular Beacon assay [AID588458, Type: screening]DNA (cytosine-5)-methyltransferase 1 isoform b [Homo sapiens] [gi:4503351]
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35
[SID49680978]
Potentiators of Human D1 Dopamine Receptor: qHTS [AID504651, Type: screening]D(1A) dopamine receptor [Homo sapiens] [gi:4503383]
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36
[SID49680978]
Antagonist of Human D 1 Dopamine Receptor: qHTS [AID504652, Type: screening]D(1A) dopamine receptor [Homo sapiens] [gi:4503383]
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37
[SID49680978]
Allosteric Agonists of the Human D1 Dopamine Receptor: qHTS [AID504660, Type: screening]D(1A) dopamine receptor [Homo sapiens] [gi:4503383]
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38
[SID49680978]
HTS Assay for Positive Allosteric Modulators of the Human D2 Dopamine Receptor: Primary Screen for Potentiators [AID485347, Type: screening]D(2) dopamine receptor isoform long [Homo sapiens] [gi:4503385]
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39
[SID49680978]
HTS Assay for Allosteric Agonists of the Human D2 Dopamine Receptor: Primary Screen for Agonists [AID485358, Type: screening]D(2) dopamine receptor isoform long [Homo sapiens] [gi:4503385]
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40
[SID49680978]
HTS Assay for Allosteric Antagonists of the Human D2 Dopamine Receptor: Primary Screen for Antagonists [AID485344, Type: screening]D(2) dopamine receptor isoform long [Homo sapiens] [gi:4503385]
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41
[SID49680978]
Beta-Arrestin HTS for Positive Allosteric Modulators of the Human D2 Dopamine Receptor: Antagonists [AID624463, Type: other]D(2) dopamine receptor isoform long [Homo sapiens] [gi:4503385]
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42
[SID49680978]
Beta-Arrestin HTS for Positive Allosteric Modulators of the Human D2 Dopamine Receptor: Potentiators [AID624464, Type: other]D(2) dopamine receptor isoform long [Homo sapiens] [gi:4503385]
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43
[SID49680978]
Beta-Arrestin HTS for Positive Allosteric Modulators of the Human D2 Dopamine Receptor: Agonists [AID624465, Type: other]D(2) dopamine receptor isoform long [Homo sapiens] [gi:4503385]
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44
[SID49680978]
Potency qHTS Assay for Inhibitors of Human Galactokinase (GALK) [AID1868, Type: confirmatory]galactokinase [Homo sapiens] [gi:4503895]
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45
[SID49680978]
Fluorescence-based cell-based primary high throughput screening assay to identify antagonists of the Galanin Receptor 3 (GalR3) [AID651719, Type: screening]galanin receptor type 3 [Homo sapiens] [gi:4503907]
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46
[SID49680978]
Luminescence-based cell-based primary high throughput screening assay to identify inverse agonists of the liver receptor homolog-1 (LRH-1; NR5A2) [AID602396, Type: screening]nuclear receptor subfamily 5 group A member 2 isoform 2 [Homo sapiens] [gi:4504343]
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47
[SID99351038]
AC50_uM Protein Kinase A Activity Assay Measured in Biochemical System Using Plate Reader - 2052-04_Inhibitor_Dose_DryPowder_Activity_Set2 [AID588629, Type: confirmatory]cAMP-dependent protein kinase catalytic subunit alpha isoform 1 [Homo sapiens] [gi:4506055]
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48
[SID99351038]
AC50_uM Protein Kinase A Activity Assay Measured in Biochemical System Using Plate Reader - 2052-04_Inhibitor_Dose_DryPowder_Activity [AID504583, Type: confirmatory]cAMP-dependent protein kinase catalytic subunit alpha isoform 1 [Homo sapiens] [gi:4506055]
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49
[SID125081988]
AC50_uM Protein Kinase A Activity Assay Measured in Biochemical System Using Plate Reader - 2052-04_Inhibitor_Dose_DryPowder_Activity_Set2 [AID588629, Type: confirmatory]cAMP-dependent protein kinase catalytic subunit alpha isoform 1 [Homo sapiens] [gi:4506055]
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50
[SID49680978]
TRFRET-based cell-based primary high throughput screening assay to identify inhibitors of cell surface Prion Protein (PRPC) [AID720596, Type: screening]major prion protein preproprotein [Homo sapiens] [gi:4506113]
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