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CHEMBL2181103 (CID 36649951) - Compound BioActivity Data
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BioActivity Outcomes:
Active(22)
 
 
Inactive(3)
 
 
Unspecified(8)
 
 
Top Targets:
GH31 MGAM SI..(21)
 
 
 
 
BioAssay Types:
Literature(24)
 
 
 
 
Confirmatory(8)
 
 
BioActivity Types:
Potency(8)
 
 
IC50(2)
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 29    Data Row: 33   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID163335587]
IC50 1.63Inhibition 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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2
[SID163335587]
IC50 1.63Inhibition 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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3
[SID89650120]
Potency 1.6343Confirmation 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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4
[SID89650120]
Potency 1.6343Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase [AID2115, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
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5
[SID89650120]
Potency 1.8338Confirmation 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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6
[SID89650121]
Potency 3.6588Confirmation 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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7
[SID89650120]
Potency 4.6062Confirmation 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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8
[SID89650121]
Potency 4.6062Confirmation of Inhibitors and Activators of Purified Human alpha-Glucosidase [AID2115, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
9
[SID89650121]
Potency 5.1682Confirmation of Inhibitors and Activators of Human alpha-Glucosidase From Spleen Homogenate [AID2113, Type: confirmatory]lysosomal alpha-glucosidase preproprotein [Homo sapiens] [gi:119393891]
View
10
[SID89650121]
Potency 5.1682Confirmation 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
11
[SID163335587]
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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12
[SID163335587]
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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13
[SID163335587]
Aqueous solubility in PBS buffer [AID705415, Type: Literature]
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14
[SID163335587]
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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15
[SID163335587]
Increase in translocation of GAA to lysosome in human F3248 cells at 5 uM after 5 days by confocal laser-scanning microscopic analysis [AID705419, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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16
[SID163335587]
Increase in translocation of GAA to lysosome in human F0833 cells at 5 uM after 5 days by confocal laser-scanning microscopic analysis [AID705420, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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17
[SID163335587]
Increase in translocation of GAA to lysosome in human F2845 cells at 5 uM after 5 days by confocal laser-scanning microscopic analysis [AID705421, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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18
[SID89650120]
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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19
[SID163335587]
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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20
[SID163335587]
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]
View
21
[SID163335587]
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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22
[SID163335587]
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]
View
23
[SID163335587]
Increase in translocation of GAA to lysosomes in human wild type skin fibrobalsts at 5 uM after 6 days by confocal laser-scanning microscopic analysis [AID705423, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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24
[SID163335587]
Increase in translocation of GAA to lysosomes in human wild type fibroblasts at 15 uM after 6 days confocal laser-scanning microscopic analysis [AID705425, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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25
[SID163335587]
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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26
[SID163335587]
Efflux ratio from basolateral to apical side to apical to basolateral side of human Caco2 cells [AID705408, Type: Literature]
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27
[SID163335587]
Permeability from basolateral to apical side of human Caco2 cells [AID705412, Type: Literature]
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28
[SID163335587]
Permeability from apical to basolateral side of human Caco2 cells [AID705413, Type: Literature]
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29
[SID163335587]
Half life in mouse liver microsomes [AID705414, Type: Literature]
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30
[SID163335587]
Cytotoxicity in human F2845 cells at 5 uM after 6 days by confocal laser-scanning microscopic analysis [AID705422, Type: Literature]
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31
[SID163335587]
Increase in translocation of GAA to lysosome in human F2845 cells at 1 uM after 5 days by confocal laser-scanning microscopic analysis [AID705418, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
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32
[SID163335587]
Increase in translocation of GAA to lysosome in human F3248 cells at 1 uM after 5 days by confocal laser-scanning microscopic analysis [AID705409, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
View
33
[SID163335587]
Increase in translocation of GAA to lysosome in human F0833 cells at 1 uM after 5 days by confocal laser-scanning microscopic analysis [AID705410, Type: Literature]Lysosomal alpha-glucosidase [gi:317373572]
View