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CHEMBL1603014 (CID 20969430) - Compound BioActivity Data
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BioActivity Outcomes:
Active(34)
 
 
Inactive(531)
 
 
Inconclusive(6)
 
 
Unspecified(15)
 
 
Top Targets:
GH31 MGAM SI..(25)
 
 
 
7TM GPCR Srx(21)
 
 
7TM GPCR Srsx(15)
 
 
CAP ED(5)
 
 
TRP 2(5)
 
 
BioAssay Types:
Screening(370)
 
 
 
Confirmatory(171)
 
 
 
 
 
Literature(28)
 
 
 
 
BioActivity Types:
Potency(138)
 
 
 
 
 
IC50(29)
 
 
 
EC50(4)
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 527    Data Row: 586   Total Pages: 12   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID49731601]
Potency 0.3275qHTS Assay for Inhibitors and Activators of Human alpha-Glucosidase Cleavage of Glycogen [AID2100, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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2
[SID89650105]
Potency 0.5191qHTS Assay for Inhibitors and Activators of Human alpha-Glucosidase Cleavage of Glycogen [AID2100, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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3
[SID89650104]
Potency 0.52Confirmation of Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate [AID2113, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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4
[SID89650104]
Potency 0.6707qHTS Assay for Inhibitors and Activators of Human alpha-Glucosidase Cleavage of Glycogen [AID2100, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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5
[SID49731601]
Potency 0.73Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase [AID2115, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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6
[SID89650104]
Potency 0.7492Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase [AID2115, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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7
[SID163312420]
IC50 0.75Inhibition of wild type recombinant GAA preincubated for 5 mins measured after 45 mins using blue-shifted dye by fluorescence assay [AID705434, Type: Literature]
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8
[SID89650105]
Potency 0.8191Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase [AID2115, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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9
[SID49731601]
Potency 0.9191Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase Using an Alternate Red Fluorescent Susbtrate [AID2110, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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10
[SID163312420]
IC50 0.94Inhibition of wild type recombinant GAA preincubated for 5 mins measured after 45 mins using red-shifted dye by fluorescence assay [AID705433, Type: Literature]
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11
[SID89650104]
Potency 0.9431Confirmation of Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate Using an Alternate Red Fluorescent Susbtrate [AID2111, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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12
[SID49731601]
Potency 1.0312Confirmation of Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate Using an Alternate Red Fluorescent Susbtrate [AID2111, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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13
[SID49731601]
Potency 1.0312Confirmation of Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate [AID2113, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
14
[SID89650104]
Potency 1.0582Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase Using an Alternate Red Fluorescent Susbtrate [AID2110, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
15
[SID89650105]
Potency 1.2982Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase Using an Alternate Red Fluorescent Susbtrate [AID2110, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
16
[SID89650105]
Potency 2.0575Confirmation of Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate Using an Alternate Red Fluorescent Susbtrate [AID2111, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
17
[SID89650105]
Potency 2.0575Confirmation of Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate [AID2113, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
18
[SID163312420]
Kd 20Binding affinity at wild type recombinant NT-495 labelled GAA incubated for 15 mins by microscale thermophoresis assay [AID705424, Type: Literature]
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19
[SID163312420]
Binding affinity at wild type recombinant GAA assessed as thermostabilization of protein at 50 uM incubated at 66 degC for 60 mins [AID705435, Type: Literature]
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20
[SID163312420]
Aqueous solubility in PBS buffer [AID705415, Type: Literature]
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21
[SID163312420]
Binding affinity at wild type recombinant GAA assessed as rise in melting temperature of protein using SYPRO Orange dye by fluorescence assay [AID705432, Type: Literature]
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22
[SID49731601]
Parallel artificial membrane permeability assay at pH 7.4 [AID624339, Type: other]
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23
[SID163312420]
Inhibition of glucocerebrosidase [AID705437, Type: Literature]
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24
[SID163312420]
Inhibition of alpha-galactosidase [AID705438, Type: Literature]
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25
[SID49731601]
qHTS Assay for Inhibitors of Human alpha-Glucosidase as a Potential Chaperone Treatment of Pompe Disease: Stabilizers of Alpha-Glucosidase Under Thermal Denaturation Conditions [AID2641, Type: other]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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26
[SID89650104]
qHTS Assay for Inhibitors of Human alpha-Glucosidase as a Potential Chaperone Treatment of Pompe Disease: Stabilizers of Alpha-Glucosidase Under Thermal Denaturation Conditions [AID2641, Type: other]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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27
[SID49731601]
Inhibitors of Human alpha-Glucosidase: PBS Stability Profiling [AID504681, Type: other]
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28
[SID49731601]
Inhibitors of Human alpha-Glucosidase: Caco-2 Cell Permeability Profiling [AID504686, Type: other]
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29
[SID89650105]
qHTS Assay for Inhibitors of Human alpha-Glucosidase as a Potential Chaperone Treatment of Pompe Disease: Stabilizers of Alpha-Glucosidase Under Thermal Denaturation Conditions [AID2641, Type: other]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
30
[SID163312420]
Increase in GAA activity in human F2845 cells incubated for 5 days by fluorescence assay relative to vehicle-treated control [AID705411, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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31
[SID163312420]
Inhibition of human recombinant GAA assessed as hydrolysis of bovine liver glycogen by Amplex red oxidase assay [AID705436, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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32
[SID163312420]
Increase in GAA activity in human F2845 cells incubated for 5 days followed by 18 to 40 hrs wash out by fluorescence assay relative to vehicle-treated control [AID705416, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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33
[SID163312420]
Increase in GAA activity in human wild type skin fibroblasts incubated for 5 days followed by 18 to 40 hrs wash out by fluorescence assay relative to vehicle-treated control [AID705417, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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34
[SID163312420]
Increase in GAA activity in human wild type skin fibroblasts incubated for 5 days by fluorescence assay relative to vehicle-treated control [AID705407, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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35
[SID49731601]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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36
[SID163312420]
Ratio of Kd for wild type recombinant NT-495 labelled GAA to IC50 for wild type recombinant GAA (unknown origin [AID705406, Type: Literature]
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37
[SID163312420]
Permeability from basolateral to apical side of human Caco2 cells [AID705412, Type: Literature]
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38
[SID163312420]
Permeability from apical to basolateral side of human Caco2 cells [AID705413, Type: Literature]
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39
[SID163312420]
Half life in mouse liver microsomes [AID705414, Type: Literature]
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40
[SID163312420]
Efflux ratio from basolateral to apical side to apical to basolateral side of human Caco2 cells [AID705408, Type: Literature]
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41
[SID163312420]
Cytotoxicity in human F2845 cells assessed as cell viability at 1 to 5 uM after 5 days confocal laser-scanning microscopic analysis [AID705426, Type: other]
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42
[SID163312420]
Cytotoxicity in human wild type skin fibroblasts assessed as cell viability at 1 to 5 uM after 5 days by confocal laser-scanning microscopic analysis [AID705427, Type: Literature]
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43
[SID163312420]
Cytotoxicity in human F2845 cells at 10 to 20 uM after 6 days by confocal laser-scanning microscopic analysis [AID705430, Type: Literature]
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44
[SID163312420]
Cytotoxicity in human wild type skin fibroblasts at 10 to 20 uM after 6 days by confocal laser-scanning microscopic analysis [AID705431, Type: Literature]
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45
[SID49731601]
Plasma Stability Mouse - Set 2 [AID624419, Type: other]
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46
[SID49731601]
Plasma Stability Human - 2 [AID624420, Type: other]
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47
[SID49731601]
Mouse hepatic microsome stability - Set 2 [AID624451, Type: screening]
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48
[SID49731601]
Human hepatic microsome stability-Set 2 [AID624452, Type: screening]
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49
[SID49731601]
Early assessment of compound stability in 1x PBS - Set 2 [AID624456, Type: other]
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50
[SID49731601]
Potency 18.526Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation [AID504834, Type: confirmatory]
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