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BioActivity Data for Compound Phenformin (CID 8249)

BioActivity Outcomes:
Active(3)
 
 
Inactive(194)
 
 
Inconclusive(13)
 
 
Unspecified(100)
 
 
Top Targets:
p450(14)
 
 
 
 
MFS(7)
 
 
HSD10-like SD..(4)
 
 
ePHD KMT2A(3)
 
 
KAZAL SLC21(3)
 
 
BioAssay Types:
Literature(162)
 
 
 
 
 
Confirmatory(115)
 
 
 
Screening(19)
 
 
BioAssay Categories:
In vitro(6)
 
 
In vivo(1)
 
 
Biochemical(10)
 
 
 
Toxicity(22)
 
 
 
ADME(21)
 
 
 
Cell-based(20)
 
 
 
BioActivity Types:
Potency(89)
 
 
 
IC50(9)
 
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 238    Data Row: 310   Total Pages: 16   Display: Page     
Sort: [Click the result table header to sort]
#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 45.4Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D2 expressed in Saccharomyces cerevisiae [AID54564, Type: Literature]Cytochrome P450 2D26 [gi:117242]
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3
[SID48416408]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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4
[SID103426218]
IC50 10TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes [AID680364, Type: Literature]Solute carrier family 22 member 1 [gi:313104181]
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5
[SID103426218]
Km 15.6TP_TRANSPORTER: uptake in OCT1-expressing CHO cells [AID679316, Type: Literature]Solute carrier family 22 member 1 [gi:81872095]
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6
[SID103426218]
IC50 65TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes [AID680369, Type: Literature]Solute carrier family 22 member 2 [gi:313104182]
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7
[SID103426218]
IC50 180In vitro inhibition of glucose oxidation by the compound in isolated rat fat cells [AID179736, Type: Literature]
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8
[SID103426218]
IC50 833Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D4 expressed in Saccharomyces cerevisiae [AID54566, Type: Literature]Cytochrome P450 2D4 [gi:117244]
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9
[SID103426218]
IC50 1927Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D3 expressed in Saccharomyces cerevisiae [AID54565, Type: Literature]Cytochrome P450 2D3 [gi:3915646]
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10
[SID103426218]
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting [AID699539, Type: Literature]Solute carrier organic anion transporter family member 1B1 [gi:12643959]
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11
[SID103426218]
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting [AID699540, Type: Literature]Solute carrier organic anion transporter family member 1B3 [gi:27734563]
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12
[SID103426218]
Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] [AID1079937, Type: Literature]
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13
[SID103426218]
Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] [AID1079938, Type: Literature]
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14
[SID103426218]
Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] [AID1079936, Type: Literature]
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15
[SID103426218]
Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] [AID1079934, Type: Literature]
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16
[SID103426218]
Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] [AID1079932, Type: Literature]
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17
[SID103426218]
Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] [AID1079943, Type: Literature]
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18
[SID103426218]
Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] [AID1079939, Type: Literature]
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19
[SID103426218]
Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] [AID1079931, Type: Literature]
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20
[SID103426218]
Presence of at least one case with successful reintroduction. [column 'REINT' in source] [AID1079946, Type: Literature]
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