Glycyrrhetinic Acid (CID 10114) - BioAssay Data Summary for Compound
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BioActivity Outcomes:
Active(54)
 
 
Top Targets:
11beta-HSD1 l..(10)
 
 
type2 17beta..(5)
 
 
Aldo ket red(1)
 
 
NR LBD PPAR(1)
 
 
PMP22 Claudin(1)
 
 
BioAssay Types:
Literature(47)
 
 
Confirmatory(4)
 
 
Screening(1)
 
 
BioActivity Types:
IC50(23)
 
 
Potency(4)
 
 
EC50(1)
 
 
Kd(1)
 
 
SAR
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Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 54    Data Row: 54   Total Pages: 2   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103525989]
IC50 0.005Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH [AID352314, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:1706408]
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2
[SID103525989]
IC50 0.0086Inhibition of human 11beta HSD1 expressed in HEK293 cells assessed as assessed as inhibition of [1,2-(n)3H]cortisone to [3H]-cortisol after 60 mins by scintillation proximity assay [AID621453, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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3
[SID103525989]
IC50 0.0086Inhibition of human 11beta HSD1 expressed in HEK293 cells assessed as assessed as inhibition of [1,2-(n)3H]cortisone to [3H]-cortisol after 60 mins by scintillation proximity assay [AID621453, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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4
[SID103525989]
IC50 0.01058Inhibition of mouse 11beta-HSD1 [AID316049, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:1706408]
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5
[SID103525989]
IC50 0.01178Inhibition of human 11beta-HSD1 [AID316048, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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6
[SID103525989]
IC50 0.01178Inhibition of human 11beta-HSD1 [AID316048, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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7
[SID103525989]
IC50 0.013Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH [AID352313, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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8
[SID103525989]
IC50 0.013Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay in presence of NADPH [AID352313, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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9
[SID103525989]
IC50 0.09Inhibition of 11beta-HSD1 in rat liver assessed as cortisone level [AID456093, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:23830928]
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10
[SID103525989]
IC50 0.09Inhibition of rat hepatic 11beta-HSD1 [AID587118, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:23830928]
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11
[SID103525989]
Kd 0.25Binding affinity to recombinant human PKCeta in after 2 hrs by microequilibrium dialysis assay [AID605339, Type: Literature]Protein kinase C eta type [gi:281185512]
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12
[SID103525989]
Kd 0.25Binding affinity to recombinant human PKCeta in after 2 hrs by microequilibrium dialysis assay [AID605339, Type: Literature]Protein kinase C eta type [gi:281185512]
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13
[SID103525989]
IC50 0.257Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2,6,7-3H]-cortisol to cortisone by scintillation counting [AID526982, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 2 [gi:30316367]
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14
[SID103525989]
IC50 0.257Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2,6,7-[3H]cortisol to cortisone after 10 mins by scintillation counting [AID587116, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 2 [gi:30316367]
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15
[SID103525989]
IC50 0.36Inhibition of rat renal 11beta-HSD2 in rat liver assessed as inhibition of cortisone production [AID456094, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 2 [gi:1706412]
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16
[SID103525989]
IC50 0.36Inhibition of rat renal 11beta-HSD2 [AID587119, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 2 [gi:1706412]
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17
[SID103525989]
IC50 0.778Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-3H]-cortisone to cortisol by scintillation counting [AID526983, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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18
[SID103525989]
IC50 0.778Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-[3H]cortisone to cortisol after 10 mins by scintillation counting [AID587113, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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19
[SID103525989]
IC50 0.778Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-3H]-cortisone to cortisol by scintillation counting [AID526983, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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20
[SID103525989]
IC50 0.778Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-[3H]cortisone to cortisol after 10 mins by scintillation counting [AID587113, Type: Literature]Corticosteroid 11-beta-dehydrogenase isozyme 1 [gi:118569]
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21
[SID103525989]
IC50 1.3Inhibition of LPS-induced TNFalpha release in mouse RAW264.7 cells pretreated 1 hr before LPS challenge by enyme immunoassay [AID418484, Type: Literature]
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22
[SID144204355]
Potency 2.3715qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]
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23
[SID103525989]
IC50 7.3Antiproliferative activity against mouse r/m HM-SFME-1 cells after 24 hrs by MTT assay [AID490287, Type: Literature]
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24
[SID144204355]
Potency 7.4993qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]
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25
[SID104171338]
Potency 8.0875S16 Schwann cell PMP22 intronic element firefly luciferase assay [AID624032, Type: confirmatory]Pmp22 gene product [Rattus norvegicus] [gi:8393992]
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26
[SID103525989]
IC50 9.6Inhibition of recombinant SHP2 [AID551432, Type: Literature]
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27
[SID103525989]
EC50 16Reduction in surface tension in 0.1 M PBS after 10 mins by Wilhelmy plate method using tensitometer [AID658065, Type: Literature]
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28
[SID103525989]
IC50 18Antiproliferative activity against mouse SFME cells after 24 hrs by MTT assay [AID490286, Type: Literature]
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29
[SID103525989]
IC50 18.52Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay [AID528069, Type: Literature]
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30
[SID103525989]
ED50 19.5Cytotoxicity against human HCT8 cells [AID300499, Type: Literature]
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31
[SID103525989]
IC50 20.86Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in hepatitis B surface antigen release [AID659364, Type: Literature]
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32
[SID103525989]
IC50 22.3Inhibition of chymotrypsin-like activity of human 20S proteasome [AID343737, Type: Literature]
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33
[SID103525989]
IC50 27.31Cytotoxicity against human NTUB1 cells after 72 hrs by MTT assay [AID608127, Type: Literature]
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34
[SID104171338]
Potency 33.5875qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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35
[SID104171338]
Potency 33.5875qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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36
[SID103525989]
GI50 37Growth inhibition in mouse B16F10 after 3 days by MTT assay [AID623268, Type: Literature]
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37
[SID103525989]
IC50 39.28Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in viral DNA replication [AID659368, Type: Literature]
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38
[SID103525989]
IC50 45.8Inhibition of recombinant PTP1B [AID551434, Type: Literature]
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39
[SID103525989]
 Drug uptake in human HeLa cells assessed as subcellular localization in endoplasmic reticulum at 25 uM after 6 hrs by live cell microscopic analysis [AID605337, Type: Literature]
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40
[SID103525989]
 Cytostatic activity against human U373 cells assessed as absence of induction of apoptosis at 80 uM after 48 to 72 hrs by TUNEL-based flow cytometric analysis [AID623273, Type: Literature]
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41
[SID103525989]
 Cytostatic activity against human A549 cells assessed as absence of induction of apoptosis at 100 uM after 48 to 72 hrs by TUNEL-based flow cytometric analysis [AID623274, Type: Literature]
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42
[SID103525989]
 Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis [AID678721, Type: Literature]
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43
[SID103525989]
 Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins [AID678713, Type: Literature]
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44
[SID103525989]
 Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins [AID678714, Type: Literature]
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45
[SID103525989]
 Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins [AID678715, Type: Literature]
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46
[SID103525989]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins [AID678716, Type: Literature]
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47
[SID103525989]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins [AID678717, Type: Literature]
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48
[SID103525989]
 Activation of caspase-like activity of 20S proteasome in human U373 cells at 90 uM after 2 days by bioluminescence assay [AID622024, Type: Literature]
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49
[SID103525989]
 Activation of chymotrypsin-like activity of 20S proteasome in human U373 cells at 90 uM after 2 days by bioluminescence assay [AID621960, Type: Literature]
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50
[SID103525989]
 Inhibition of trypsin-like activity of 20S proteasome in human U373 cells at 90 uM after 2 days by bioluminescence assay [AID621961, Type: Literature]
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