Phenformin (CID 8249) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(3)
 
 
Inactive(185)
 
 
Inconclusive(13)
 
 
Unspecified(72)
 
 
Top Targets:
p450(15)
 
 
 
 
P53(3)
 
 
Firefly Luc l..(3)
 
 
HELICc(2)
 
 
HIF-1a CTAD(2)
 
 
BioAssay Types:
Literature(131)
 
 
 
 
 
Confirmatory(105)
 
 
 
Screening(20)
 
 
BioActivity Types:
Potency(81)
 
 
 
IC50(8)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 206    Data Row: 273   Total Pages: 6   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103426218]
IC50 27Inhibition of MAMC O-dealkylation mediated by human Cytochrome P450 2D6 expressed in human lymphoblastoid cell line [AID54570, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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2
[SID103426218]
IC50 27Inhibition of MAMC O-dealkylation mediated by human Cytochrome P450 2D6 expressed in human lymphoblastoid cell line [AID54570, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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3
[SID103426218]
IC50 45.4Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D2 expressed in Saccharomyces cerivisiae [AID54564, Type: Literature]Cytochrome P450 2D26 [gi:117242]
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4
[SID48416408]
 DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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5
[SID103426218]
IC50 10TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes [AID680364, Type: other]Solute carrier family 22 member 1 [gi:313104181]
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6
[SID103426218]
Km 15.6TP_TRANSPORTER: uptake in OCT1-expressing CHO cells [AID679316, Type: other]Solute carrier family 22 member 1 [gi:81872095]
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7
[SID103426218]
IC50 65TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes [AID680369, Type: other]Solute carrier family 22 member 2 [gi:313104182]
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8
[SID103426218]
IC50 180In vitro inhibition of glucose oxidation by the compound in isolated rat fat cells [AID179736, Type: Literature]
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9
[SID103426218]
IC50 833Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D4 expressed in Saccharomyces cerivisiae [AID54566, Type: Literature]Cytochrome P450 2D18 [gi:2493368]
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10
[SID103426218]
IC50 1927Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D3 expressed in Saccharomyces cerivisiae [AID54565, Type: Literature]Cytochrome P450 2D3 [gi:3915646]
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11
[SID103426218]
 Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D1 expressed in Saccharomyces cerivisiae; ND=no data [AID54563, Type: Literature]Cytochrome P450 2D1 [gi:117241]
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12
[SID11112448]
 Cytochrome panel assay with activity outcomes [AID1851, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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13
[SID11112448]
 Cytochrome panel assay with activity outcomes [AID1851, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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14
[SID103426218]
 Rise in the blood glucose level after 0 min following 300 mg/kg oral dose in fasted nondiabetic rats [AID179876, Type: Literature]
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15
[SID103426218]
 Rise in the blood glucose level after 0 min following 50 mg/kg oral dose in fasted nondiabetic rats [AID179877, Type: Literature]
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16
[SID103426218]
 Rise in the blood glucose level after 30 min following 10 mg/kg oral dose in fasted nondiabetic rats [AID179878, Type: Literature]
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17
[SID103426218]
 Rise in the blood glucose level after 30 min following 100 mg/kg oral dose in fasted nondiabetic rats [AID179879, Type: Literature]
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18
[SID103426218]
 Rise in the blood glucose level after 30 min following 150 mg/kg oral dose in fasted nondiabetic rats [AID179880, Type: Literature]
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19
[SID103426218]
 Rise in the blood glucose level after 30 min following 300 mg/kg oral dose in fasted nondiabetic rats [AID179882, Type: Literature]
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20
[SID103426218]
 Rise in the blood glucose level after 30 min following 50 mg/kg oral dose in fasted nondiabetic rats [AID179883, Type: Literature]
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21
[SID103426218]
 Rise in the blood glucose level at 10 mg/kg oral dose in fasted nondiabetic rats [AID179884, Type: Literature]
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22
[SID103426218]
 Rise in the blood glucose level at 100 mg/kg oral dose in fasted nondiabetic rats [AID179885, Type: Literature]
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23
[SID103426218]
 Rise in the blood glucose level at 150 mg/kg oral dose in fasted nondiabetic rats [AID179886, Type: Literature]
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24
[SID103426218]
 Rise in the blood glucose level at 300 mg/kg oral dose in fasted nondiabetic rats [AID179888, Type: Literature]
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25
[SID103426218]
 Rise in the blood glucose level at 50 mg/kg oral dose in fasted nondiabetic rats [AID179889, Type: Literature]
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26
[SID103426218]
 Percent inhibition of glucose rise, following 10 mg/kg oral dose in fasted nondiabetic rats [AID182468, Type: Literature]
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27
[SID103426218]
 Percent inhibition of glucose rise, following 100 mg/kg oral dose in fasted nondiabetic rats [AID182469, Type: Literature]
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28
[SID103426218]
 Percent inhibition of glucose rise, following 150 mg/kg oral dose in fasted nondiabetic rats [AID182470, Type: Literature]
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29
[SID103426218]
 Percent inhibition of glucose rise, following 300 mg/kg oral dose in fasted nondiabetic rats [AID182472, Type: Literature]
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30
[SID103426218]
 Percent inhibition of glucose rise, following 50 mg/kg oral dose in fasted nondiabetic rats [AID182473, Type: Literature]
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31
[SID103426218]
 Lethal dose required to produce 50% lethality in male and female carworth farms CF-1 strain mice weighing 16-25 g administered intraperitoneally [AID184645, Type: Literature]
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32
[SID103426218]
 Lethal dose required to produce 50% lethality in male and female carworth farms CF-1 strain mice weighing 16-25 g administered orally [AID184646, Type: Literature]
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33
[SID103426218]
 Evaluated in alloxanized, diabetic rat for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 100 mg of free base / kg body weight administered orally [AID188229, Type: Literature]
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34
[SID103426218]
 Evaluated in glucose-primed, fasted rat for the percentage reduction in blood glucose level after 2 hr as compared to control groups at a dose of 100 mg of free base / kg body weight administered orally [AID188241, Type: Literature]
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35
[SID103426218]
 Percent reduction in blood glucose after perorally administration of compound at 100 mg/kg in glucose-primed rat [AID188896, Type: Literature]
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36
[SID103426218]
 Percent reduction in blood glucose after perorally administration of compound at 100 mg/kg in in alloxanized rat [AID188897, Type: Literature]
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37
[SID103426218]
 Percent reduction in blood glucose after perorally administration of compound at 120 mg/kg in non-glucose-primed rat [AID188899, Type: Literature]
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38
[SID103426218]
 Percent reduction in blood glucose after perorally administration of compound at 80 mg/kg in non-glucose-primed rat [AID189025, Type: Literature]
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39
[SID103426218]
 In vitro inhibition of glucose oxidation determined in normal rats at a hypoglycemic dose of 2.0 mmol/kg [AID193166, Type: Literature]
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40
[SID103426218]
 In vivo increase of plasma insulin in normal rats at a hypoglycemic dose of 2.0 mmol/kg [AID197698, Type: Literature]
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41
[SID103426218]
 Evaluated for the blood lactate level in 24 hr fasted Sprague-Dawley rats at a dose of 200 mg/kg/day in four divided doses administered intraperitoneally [AID204498, Type: Literature]
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42
[SID103426218]
 Evaluated for the plasma glucose level in 24 hr fasted Sprauge-Dawley rats at a dose of 200 mg/kg/day in four divided doses administered intraperitoneally [AID204499, Type: Literature]
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43
[SID103426218]
 Toxicity in lean normal BALB/c mouse assessed as overt signs of behavioural changes at equimolar dose of 0.5 mmol/kg galegine administered daily through diet for 7 days [AID352936, Type: Literature]
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44
[SID103426218]
 Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.51 mmol/kg/day administered through diet for 7 days relative to time-matched control [AID352937, Type: Literature]
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45
[SID103426218]
 Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.57 mmol/kg/day administered through diet for 7 days relative to time-matched control [AID352938, Type: Literature]
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46
[SID103426218]
 Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.70 mmol/kg/day administered through diet for 7 days relative to time-matched control [AID352939, Type: Literature]
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47
[SID103426218]
 Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.59 mmol/kg/day administered through diet for 7 days relative to time-matched control [AID352940, Type: Literature]
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48
[SID103426218]
 Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.52 mmol/kg/day administered through diet for 7 days relative to time-matched control [AID352941, Type: Literature]
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49
[SID103426218]
 Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.40 mmol/kg/day administered through diet for 7 days relative to time-matched control [AID352948, Type: Literature]
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50
[SID103426218]
 Hypoglycemic activity in lean normal BALB/c mouse assessed as blood glucose level at 0.62 mmol/kg/day administered through diet for 7 days relative to time-matched control [AID352957, Type: Literature]
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