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Gemfibrozil (CID 3463) - Compound BioActivity Data
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BioActivity Outcomes:
Active(27)
 
 
Inactive(1623)
 
 
Inconclusive(93)
 
 
Unspecified(1762)
 
 
Top Targets:
NR LBD PPAR(53)
 
 
 
 
 
7TM GPCR Srx(42)
 
 
 
7TM GPCR Srsx(39)
 
 
 
NR LBD ER(32)
 
 
 
 
p450(28)
 
 
 
 
 
BioAssay Types:
Confirmatory(810)
 
 
 
 
 
Screening(671)
 
 
 
Literature(294)
 
 
 
 
Summary(72)
 
 
 
BioActivity Types:
Potency(720)
 
 
 
 
 
IC50(169)
 
 
 
 
EC50(16)
 
 
 
Ki(2)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 2844    Data Row: 3505   Total Pages: 71   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103166445]
Ki 1.86Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay [AID407366, Type: Literature]Fatty acid-binding protein, liver [gi:119810]
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2
[SID103166445]
IC50 4.1Inhibition of CYP2C8 [AID705607, Type: Literature]
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3
[SID11112705]
Potency 6.3096qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C9 [AID883, Type: confirmatory]cytochrome P450 2C9 precursor [Homo sapiens] [gi:13699818]
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4
[SID103166445]
IC50 9.6Reversible inhibition of CYP2C9 in human liver microsomes [AID705589, Type: Literature]Cytochrome P450 2C9 [gi:6686268]
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5
[SID855780]
Potency 19.9526VP16 counterscreen qHTS for inhibitors of ROR gamma transcriptional activity [AID2546, Type: confirmatory]nuclear receptor ROR-gamma [Mus musculus] [gi:188536040]
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6
[SID144209195]
Potency-Replicate_1 48.9036qHTS assay to identify small molecule that activate the aryl hydrocarbon receptor (AhR) signaling pathway [AID743085, Type: confirmatory]aryl hydrocarbon receptor [Homo sapiens] [gi:51095037]
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7
[SID11112705]
p450-cyp1a2 [AID410, Type: confirmatory]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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8
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_14, Type: screening]oxysterols receptor LXR-beta isoform 1 [Homo sapiens] [gi:85362735]
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9
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_24, Type: screening]COUP transcription factor 1 [Homo sapiens] [gi:5032173]
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10
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_57, Type: screening]retinoic acid receptor RXR-alpha [Homo sapiens] [gi:4506755]
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11
[SID855780]
High Throughput Screen to Identify Compounds that Inhibit Class II HMG-CoA Reductases - Primary Screen [AID1066, Type: screening]acetyl-CoA acetyltransferase/HMG-CoA reductase [Enterococcus faecalis] [gi:9937384]
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12
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_52, Type: screening]nuclear receptor ROR-alpha isoform c [Homo sapiens] [gi:4506577]
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13
[SID11112705]
Cytochrome panel assay with activity outcomes [AID1851_5, Type: other]cytochrome P450 2C9 precursor [Homo sapiens] [gi:13699818]
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14
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_49, Type: screening]retinoic acid receptor beta isoform 1 [Homo sapiens] [gi:14916494]
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15
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_36, Type: screening]steroidogenic factor 1 [Homo sapiens] [gi:20070193]
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16
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_37, Type: screening]steroidogenic factor 1 [Homo sapiens] [gi:20070193]
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17
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_38, Type: screening]nuclear receptor subfamily 5 group A member 2 isoform 2 [Homo sapiens] [gi:4504343]
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18
[SID103166445]
Peroxisome proliferator-activated receptor alpha agonist [AID742844, Type: other]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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19
[SID103166445]
Agonist activity at PPARalpha in human HepG2 cells assessed as upregulation of CPT1a mRNA expression at 0.1 to 100 uM after 24 hrs by quantitative RT-PCR analysis [AID620231, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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20
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_46, Type: screening]retinoic acid receptor alpha isoform 1 [Homo sapiens] [gi:4506419]
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21
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_47, Type: screening]retinoic acid receptor alpha isoform 1 [Homo sapiens] [gi:4506419]
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22
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277_50, Type: screening]retinoic acid receptor gamma isoform 1 [Homo sapiens] [gi:4506423]
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23
[SID87219219]
Center Based Initiative to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR): luminescence-based high throughput cell-based assay to identify modulators of human nuclear receptors. [AID2277, Type: screening]
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24
[SID48413808]
DSSTox (CPDBAS) Carcinogenic Potency Database Summary SingleCellCall Results [AID1189, Type: other]
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25
[SID103166445]
Activation of c-Jun expressed in HEK293 cells assessed as induction of protein interaction with Pin1 by EYFP based reporter gene assay [AID503325, Type: Literature]
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26
[SID48413808]
DSSTox (CPDBAS) Carcinogenic Potency Database Summary Rat Bioassay Results [AID1208, Type: other]
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27
[SID48416049]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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28
[SID103166445]
EC50 59Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay [AID620228, Type: Literature]
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29
[SID103166445]
IC50 69Antagonist activity at human T1R2/T1R3 receptor expressed in HEK293E cells assessed as inhibition of sucralose-induced intracellular calcium mobilization [AID439612, Type: Literature]
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30
[SID103166445]
IC50 95Reversible inhibition of CYP2C8 in human liver microsomes [AID705588, Type: Literature]Cytochrome P450 2C8 [gi:117225]
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31
[SID103166445]
EC50 147.8Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs [AID299412, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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32
[SID103166445]
EC50 147.8Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay [AID391553, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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33
[SID103166445]
Ki 179Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay [AID407369, Type: Literature]Fatty acid-binding protein, liver [gi:119810]
View
34
[SID103166445]
EC50 193.3Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay [AID391555, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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35
[SID103166445]
EC50 193.3Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs [AID299410, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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36
[SID103166445]
IC50 2670Compound concentration that cause 50% inhibition of human platelet aggregation by COL/EPI cartridges [AID92093, Type: Literature]
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37
[SID103166445]
Compound was evaluated for the inhibitory activity against human platelet aggregation by COL/ADP cartridges at a concentration of 1 x 10 e-3 M [AID92255, Type: Literature]
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38
[SID103166445]
Compound was evaluated for the inhibitory activity against human platelet aggregation by COL/ADP cartridges at a concentration of 2 x 10 e-3 M [AID92256, Type: Literature]
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39
[SID103166445]
Compound was evaluated for the inhibitory activity against human platelet aggregation by COL/ADP cartridges at a concentration of 3 x 10 e-3 M [AID92257, Type: Literature]
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40
[SID103166445]
Compound was evaluated for the inhibitory activity against human platelet aggregation by COL/ADP cartridges at a concentration of 4 x 10 e-3 M [AID92258, Type: Literature]
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41
[SID103166445]
Compound was evaluated for the inhibitory activity against human platelet aggregation by COL/ADP cartridges at a concentration of 5 x 10 e-3 M [AID92259, Type: Literature]
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42
[SID103166445]
Compound was tested for the inhibition of malate dehydrogenase (MDH) at 200 uM [AID106805, Type: Literature]
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43
[SID103166445]
Hypotriglyceridemic activity of KK-mice in 12 animals [AID111620, Type: Literature]
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44
[SID103166445]
In vivo activity against hypocholesterol (CHOL) by using Alloxan-induced hyperlipoperoxidemia method in BALB/c mice after peroral administration at 100 mg/kg dose [AID111629, Type: Literature]
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45
[SID103166445]
In vivo activity against serum lipid peroxidation level (s-LPO) by using Alloxan-induced hyperlipoperoxidemia method in BALB/c mice after peroral administration at 100 mg/kg dose [AID111634, Type: Literature]
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46
[SID103166445]
In vivo activity against serum lipid peroxidation level (s-LPO) by using Alloxan-induced hyperlipoperoxidemia method in BALB/c mice after peroral administration at 300 mg/kg dose [AID111637, Type: Literature]
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47
[SID103166445]
In vivo activity against triglycerides (TG) by using Alloxan-induced hyperlipoperoxidemia method in BALB/c mice after peroral administration at 300 mg/kg dose [AID111645, Type: Literature]
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48
[SID103166445]
liver weight in Wistar-Imamichi rats at 300 mg/kg dose in 12 rats [AID111649, Type: Literature]
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49
[SID103166445]
In vivo biological activity against Apo A-I relative to gemfibrozil in male Sprague-Dawley rats [AID169209, Type: Literature]
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50
[SID103166445]
In vivo biological activity against HDL relative to gemfibrozil in male Sprague-Dawley rats [AID169210, Type: Literature]
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