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GR 113808 (CID 119376) - Compound BioActivity Data
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BioActivity Outcomes:
Active(34)
 
 
Inactive(720)
 
 
Inconclusive(35)
 
 
Unspecified(19)
 
 
Top Targets:
7TM GPCR Srx(21)
 
 
 
p450(12)
 
 
 
7TM GPCR Srsx(12)
 
 
TAS2R(9)
 
 
 
 
Pyr redox dim(7)
 
 
BioAssay Types:
Confirmatory(366)
 
 
 
 
 
Screening(365)
 
 
 
Literature(52)
 
 
 
 
 
Summary(1)
 
 
BioActivity Types:
Potency(303)
 
 
 
 
 
IC50(23)
 
 
 
 
Ki(15)
 
 
 
AC50(1)
 
 
EC50(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 668    Data Row: 808   Total Pages: 17   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103209519]
Ki 7.41e-05Antagonistic activity at human 5HT4 receptor expressed in HEK293 cells [AID548650, Type: Literature]5-hydroxytryptamine receptor 4 [gi:12644029]
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2
[SID103209519]
Ki 7.8e-05Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells [AID6469, Type: Literature]
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3
[SID103209519]
Ki 0.0001Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808 [AID6472, Type: Literature]
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4
[SID103209519]
Ki 0.00011Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand [AID6175, Type: Literature]5-hydroxytryptamine receptor 4 [gi:6224984]
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5
[SID103209519]
Ki 0.00015Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand [AID6239, Type: Literature]
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6
[SID103209519]
Ki 0.00015Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement. [AID6246, Type: Literature]
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7
[SID103209519]
Ki 0.000158Binding affinity at 5HT4 receptor [AID416400, Type: Literature]
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8
[SID103209519]
IC50 0.00021Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels [AID707290, Type: Literature]5-hydroxytryptamine receptor 4 [gi:12644029]
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9
[SID103209519]
Ki 0.00033Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells [AID6466, Type: Literature]
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10
[SID103209519]
Ki 0.00041Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells [AID6468, Type: Literature]
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11
[SID103209519]
Ki 0.0005Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells [AID297383, Type: Literature]
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12
[SID103209519]
Ki 0.0005Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cells [AID297386, Type: Literature]5-hydroxytryptamine receptor 4 [gi:12644029]
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13
[SID103209519]
Ki 0.00053Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells [AID6467, Type: Literature]
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14
[SID103209519]
Ki 0.0007Binding affinity to YFP fused 5HT4 receptor expressed in CHO cells [AID297387, Type: Literature]5-hydroxytryptamine receptor 4 [gi:12644029]
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15
[SID103209519]
IC50 0.013Antagonist activity was calculated as the concentration which produced a 50% reduction in the submaximal of 5-HT induced contractions guinea pig ileum [AID78004, Type: Literature]
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16
[SID103209519]
IC50 0.0135-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum [AID6152, Type: Literature]5-hydroxytryptamine receptor 4 [gi:6224984]
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17
[SID103209519]
IC50 7.94328Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay [AID524796, Type: Literature]
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18
[SID50104812]
Potency 8.9125qHTS for differential inhibitors of proliferation of Plasmodium falciparum line W2 [AID1883, Type: confirmatory]
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19
[SID103209519]
IC50 10Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay [AID524790, Type: Literature]
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20
[SID103209519]
IC50 10Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay [AID524791, Type: Literature]
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21
[SID103209519]
IC50 10Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay [AID524794, Type: Literature]
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22
[SID50104812]
Potency 10qHTS for differential inhibitors of proliferation of Plasmodium falciparum line 7G8 [AID1815, Type: confirmatory]
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23
[SID103209519]
IC50 12.5892Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay [AID524795, Type: Literature]
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24
[SID46500374]
AC50_uM 50Identification of Small Molecule Correctors of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Delta508 Mutation Function in Human Bronchial Epithelial Cells. Measured in Cell-Based System Using Plate Reader - 7017-01_Other_Dose_CherryPick_Activity [AID743267, Type: confirmatory]cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7 [Homo sapiens] [gi:89348172]
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25
[SID46500374]
Identification of Small Molecule Correctors of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Delta508 Mutation Function in Human Bronchial Epithelial Cells. Measured in Cell-Based System Using Plate Reader - 7017-01_Other_SinglePoint_HTS_Activity [AID720511, Type: screening]cystic fibrosis transmembrane conductance regulator ATP-binding cassette sub-family C member 7 [Homo sapiens] [gi:89348172]
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26
[SID135651154]
Antagonists at Human 5-Hydroxytryptamine receptor 5-HT4 [AID624238, Type: Literature]5-hydroxytryptamine receptor 4 isoform d [Homo sapiens] [gi:297206833]
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27
[SID135650309]
Antagonists at Human 5-Hydroxytryptamine receptor 5-HT4 [AID624238, Type: Literature]5-hydroxytryptamine receptor 4 isoform d [Homo sapiens] [gi:297206833]
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28
[SID85209373]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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29
[SID135650309]
Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT4 [AID624200, Type: Literature]5-hydroxytryptamine receptor 4 [Rattus norvegicus] [gi:6981060]
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30
[SID135651154]
Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT4 [AID624200, Type: Literature]5-hydroxytryptamine receptor 4 [Rattus norvegicus] [gi:6981060]
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31
[SID135650309]
Antagonists at Mouse 5-Hydroxytryptamine receptor 5-HT4 [AID624197, Type: Literature]5-hydroxytryptamine receptor 4 [Mus musculus] [gi:84370240]
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32
[SID11114029]
Cytochrome panel assay with activity outcomes [AID1851_4, Type: other]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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33
[SID11114029]
p450-cyp1a2 [AID410, Type: confirmatory]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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34
[SID11111231]
p450-cyp1a2 [AID410, Type: confirmatory]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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35
[SID103209519]
Ki 5.01e-05GRAC: human 5-HT4 selective antagonist [AID540477, Type: other]5-hydroxytryptamine receptor 4 [gi:12644029]
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36
[SID103209519]
IC50 1Inhibitory concentration against 5-hydroxytryptamine 3 receptor in rat enthorinal cortex using [3H]-LY 278584 as radioligand [AID6073, Type: Literature]
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37
[SID103209519]
Ki 10Binding affinity at 5HT3 receptor [AID416399, Type: Literature]
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38
[SID103209519]
Agonist activity at human 5HT4e receptor expressed in C6 cells assessed as cAMP accumulation relative to 5HT [AID297384, Type: Literature]
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39
[SID46500374]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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40
[SID103209519]
Antagonist activity against 5-HT4 receptor mediated relaxation of rat carbachol contracted esophageal muscularis mucosae [AID3203, Type: other]5-hydroxytryptamine receptor 4 [gi:2494928]
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41
[SID103209519]
Antinociceptive activity in the mouse writhing test after intraperitoneal dose of 0.01 mg/kg [AID137940, Type: Literature]
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42
[SID103209519]
Antinociceptive activity in the mouse writhing test after intraperitoneal dose of 0.1 mg/kg [AID137941, Type: Literature]
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43
[SID103209519]
Antinociceptive activity in the mouse writhing test after intraperitoneal dose of 1 mg/kg [AID137943, Type: Literature]
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44
[SID103209519]
Antinociceptive activity in the mouse writhing test before administration of the compound [AID137947, Type: Literature]
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45
[SID103209519]
Compound was tested against 5-HT4 receptor through antagonism of 5-HT mediated relaxation of rat, carbachol contracted esophageal muscularis mucosae [AID203912, Type: other]
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46
[SID103209519]
Antinociceptive activity against acetic acid-induced writhing in NMRI mouse assessed as number of stretches at 0.01 mg/kg, ip by writhing test [AID416538, Type: Literature]
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47
[SID103209519]
Antinociceptive activity against acetic acid-induced writhing in NMRI mouse assessed as number of stretches at 0.1 mg/kg, ip by writhing test [AID416539, Type: Literature]
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48
[SID103209519]
Antinociceptive activity against acetic acid-induced writhing in NMRI mouse assessed as number of stretches at 1 mg/kg, ip by writhing test [AID416540, Type: Literature]
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49
[SID11114029]
Cytochrome panel assay with activity outcomes [AID1851, Type: other]
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50
[SID103209519]
Antagonistic activity at human 5HT4 receptor expressed in HEK293 cells assessed as inhibition of 5-HT stimulated ADCY activity after 20 mins [AID548649, Type: Literature]5-hydroxytryptamine receptor 4 [gi:12644029]
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