Metformin (CID 4091) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(9)
 
 
Inactive(173)
 
 
Inconclusive(23)
 
 
Unspecified(1695)
 
 
Top Targets:
p450(18)
 
 
 
7TM GPCR Srx(12)
 
 
7TM GPCR Srsx(10)
 
 
MFS(5)
 
 
STKc ERK1 2 l..(4)
 
 
 
BioAssay Types:
Literature(252)
 
 
 
 
 
Confirmatory(115)
 
 
 
Screening(4)
 
 
BioActivity Types:
IC50(119)
 
 
 
Potency(89)
 
 
 
AC50(2)
 
 
EC50(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1832    Data Row: 1900   Total Pages: 38   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103508547]
EC50 0.27Increase in glucose consumption in insulin-resistant human HepG2 cells after 24 hrs [AID619463, Type: Literature]
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2
[SID103508547]
IC50 29Inhibition of DPP4 [AID313842, Type: Literature]
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3
[SID103508547]
 Antidiabetic activity in high fat diet-fed C57BL/6J mouse assessed as decrease in blood glucose level at 250 mg/kg/day, po for 4 weeks measured after 60 mins by intraperitoneal glucose tolerance test [AID615040, Type: Literature]
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4
[SID103508547]
 Antidiabetic activity in high fat diet-fed C57BL/6J mouse assessed as decrease in blood glucose level at 250 mg/kg/day, po for 4 weeks measured after 120 mins by intraperitoneal glucose tolerance test [AID615041, Type: Literature]
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5
[SID103508547]
 Antidiabetic activity in C57BLKS/J-db/db mouse assessed as reduction of fasting blood glucose level at 250 mg/kg/day, po for 5 weeks [AID615133, Type: Literature]
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6
[SID48416229]
 DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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7
[SID103508547]
 Antiproliferative activity against human MDA-MB-231 cells at 1 to 20 mM after 24 hrs by MTT assay [AID658424, Type: Literature]
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8
[SID103508547]
 Antidiabetic activity in STZ-induced ICR mouse T1DM model assessed as reduction in plasma glucose level at 200 mg/kg, ip after 60 mins [AID654703, Type: Literature]
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9
[SID103508547]
 Antidiabetic activity in normal ICR mouse assessed as reduction in plasma glucose level at 200 mg/kg, ip after 60 mins [AID654702, Type: Literature]
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10
[SID103508547]
Km 377TP_TRANSPORTER: uptake in OCT1-expressing CHO cells [AID679316, Type: other]Solute carrier family 22 member 1 [gi:81872095]
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11
[SID103508547]
IC50 1700TP_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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12
[SID103508547]
IC50 2010TP_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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13
[SID103508547]
 Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy [AID386623, Type: Literature]Solute carrier family 22 member 1 [gi:313104181]
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14
[SID103508547]
IC50 DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625198, Type: other]Alpha-1D adrenergic receptor [gi:1168244]
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15
[SID103508547]
 Substrates of transporters of clinical importance in the absorption and dispostion of drugs, MATE1 [AID588972, Type: Literature]Multidrug and toxin extrusion protein 1 [gi:74731723]
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16
[SID103508547]
IC50 DRUGMATRIX: Insulin radioligand binding (ligand: [125I] Insulin) [AID625273, Type: other]Insulin receptor [gi:124531]
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17
[SID103508547]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) [AID625191, Type: other]5-hydroxytryptamine receptor 1B [gi:112815]
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18
[SID103508547]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) [AID625191, Type: other]5-hydroxytryptamine receptor 1B [gi:112815]
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19
[SID103508547]
IC50 DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) [AID625223, Type: other]Sigma non-opioid intracellular receptor 1 [gi:74752153]
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20
[SID103508547]
IC50 DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) [AID625223, Type: other]Sigma non-opioid intracellular receptor 1 [gi:74752153]
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21
[SID103508547]
IC50 DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) [AID625145, Type: other]Cysteinyl leukotriene receptor 1 [gi:20138087]
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22
[SID103508547]
IC50 DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) [AID625145, Type: other]Cysteinyl leukotriene receptor 1 [gi:20138087]
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23
[SID103508547]
 DRUGMATRIX: Nitric Oxide Synthase, Inducible (iNOS) enzyme inhibition (substrate: L-Arginine) [AID625160, Type: other]Nitric oxide synthase, inducible [gi:266649]
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24
[SID103508547]
 Substrates of transporters of clinical importance in the absorption and dispostion of drugs, OCT2 [AID588966, Type: Literature]Solute carrier family 22 member 2 [gi:313104182]
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25
[SID103508547]
 DRUGMATRIX: Vasoactive Intestinal Peptide VIP1 radioligand binding (ligand: [125I] VIP) [AID625232, Type: other]Vasoactive intestinal polypeptide receptor 1 [gi:418253]
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26
[SID103508547]
IC50 DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP) [AID625167, Type: other]cGMP-specific 3',5'-cyclic phosphodiesterase [gi:317373261]
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27
[SID103508547]
 TP_TRANSPORTER: decrease in small intestine concentration in Oct1 -/- mouse [AID682013, Type: other]Solute carrier family 22 member 1 [gi:189046191]
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28
[SID103508547]
 TP_TRANSPORTER: decrease in liver concentration in Oct1 -/- mouse [AID682014, Type: other]Solute carrier family 22 member 1 [gi:189046191]
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29
[SID103508547]
IC50 DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) [AID625199, Type: other]Alpha-1B adrenergic receptor [gi:543734]
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30
[SID103508547]
IC50 DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) [AID625199, Type: other]Alpha-1B adrenergic receptor [gi:543734]
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31
[SID103508547]
IC50 DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) [AID625208, Type: other]Aldose reductase [gi:1168407]
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32
[SID103508547]
IC50 DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) [AID625228, Type: other]Androgen receptor [gi:113832]
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33
[SID103508547]
IC50 DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) [AID625228, Type: other]Androgen receptor [gi:113832]
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34
[SID103508547]
IC50 DRUGMATRIX: Nitric Oxide Synthase, Neuronal (nNOS) radioligand binding (ligand: [3H]L-Arginine) [AID625159, Type: other]Nitric oxide synthase, brain [gi:266646]
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35
[SID103508547]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein) [AID625180, Type: other]Mitogen-activated protein kinase 3 [gi:232066]
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36
[SID103508547]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein) [AID625180, Type: other]Mitogen-activated protein kinase 3 [gi:232066]
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37
[SID103508547]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein) [AID625180, Type: other]Mitogen-activated protein kinase 3 [gi:232066]
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38
[SID103508547]
IC50 DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF) [AID625168, Type: other]Platelet-activating factor receptor [gi:129557]
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39
[SID103508547]
IC50 DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) [AID625243, Type: other]Prostaglandin G/H synthase 1 [gi:317373262]
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40
[SID103508547]
IC50 DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) [AID625244, Type: other]Prostaglandin G/H synthase 2 [gi:3915797]
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41
[SID103508547]
 DRUGMATRIX: Protein Tyrosine Phosphatase, PTPRC (CD45) enzyme inhibition (substrate: DiFMUP) [AID625188, Type: other]Receptor-type tyrosine-protein phosphatase C [gi:33112650]
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42
[SID103508547]
IC50 DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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43
[SID103508547]
IC50 DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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44
[SID103508547]
IC50 DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
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45
[SID103508547]
IC50 DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
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46
[SID103508547]
IC50 DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
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47
[SID103508547]
IC50 DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
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48
[SID103508547]
IC50 DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: other]Sodium-dependent serotonin transporter [gi:400630]
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49
[SID103508547]
IC50 DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: other]Sodium-dependent serotonin transporter [gi:400630]
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50
[SID103508547]
IC50 DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: other]Sodium-dependent serotonin transporter [gi:400630]
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