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Cimetidine (CID 2756) - Compound BioActivity Data
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BioActivity Outcomes:
Active(49)
 
 
Inactive(1676)
 
 
Inconclusive(88)
 
 
Unspecified(1904)
 
 
Top Targets:
7tm 4(111)
 
 
 
 
 
MFS(61)
 
 
 
p450(39)
 
 
 
 
 
NR LBD PPAR(27)
 
 
 
NR LBD TR(22)
 
 
BioAssay Types:
Confirmatory(1079)
 
 
 
 
 
Screening(548)
 
 
 
Literature(494)
 
 
 
 
 
Summary(49)
 
 
 
BioActivity Types:
Potency(800)
 
 
 
 
 
IC50(208)
 
 
 
 
 
Ki(13)
 
 
 
Kd(7)
 
 
EC50(7)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 3114    Data Row: 3717   Total Pages: 186   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103165167]
Ki 0.07079Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin) [AID1063783, Type: Literature]Histamine H2 receptor [gi:123120]
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2
[SID103165167]
IC50 0.14Binding affinity to human histamine H2 receptor by radioligand displacement assay [AID751879, Type: Literature]Histamine H2 receptor [gi:123120]
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3
[SID103165167]
IC50 0.18Displacement of radiolabeled cimetidine from human histamine H2 receptor [AID346426, Type: Literature]Histamine H2 receptor [gi:123120]
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4
[SID103165167]
Kd 0.25119Antagonistic activity for inhibition of histamine H2 receptor from anesthetized rats [AID88493, Type: confirmatory]
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5
[SID103165167]
Kd 0.25119Antagonistic activity by inhibition histamine H2 receptor from rats. [AID88494, Type: confirmatory]
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6
[SID103165167]
Kd 0.26303In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria. [AID88151, Type: Literature]Histamine H2 receptor [gi:1346291]
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7
[SID103165167]
IC50 0.27Binding affinity to human histamine H2 receptor by radioligand displacement assay [AID752241, Type: Literature]Histamine H2 receptor [gi:123120]
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8
[SID103165167]
Kd 0.37154Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8 [AID88142, Type: Literature]Histamine H2 receptor [gi:1346291]
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9
[SID103165167]
Kd 0.39811Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4 [AID88141, Type: Literature]Histamine H2 receptor [gi:1346291]
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10
[SID103165167]
Ki 0.50119Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium [AID87707, Type: Literature]Histamine H2 receptor [gi:1346291]
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11
[SID103165167]
Ki 0.50119In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate [AID87709, Type: Literature]Histamine H2 receptor [gi:1346291]
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12
[SID103165167]
IC50 0.781Inhibition of histamine H2 receptor [AID340249, Type: Literature]
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13
[SID103165167]
IC50 0.82Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by exogenous histamine [AID167652, Type: Literature]
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14
[SID103165167]
Kd 0.95499Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0 [AID88140, Type: Literature]Histamine H2 receptor [gi:1346291]
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15
[SID103165167]
Kd 1Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium [AID88156, Type: Literature]Histamine H2 receptor [gi:1346291]
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16
[SID103165167]
IC50 1.02Inhibition of guinea pig histamine H2 receptor [AID566261, Type: Literature]Histamine H2 receptor [gi:1346291]
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17
[SID103165167]
IC50 1.2Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay [AID721754, Type: Literature]Multidrug and toxin extrusion protein 1 [gi:74731723]
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18
[SID103165167]
ED50 2.7Dose representing 50% inhibition of positive chronotropic response to histamine in guinea pig atrium (5 x 10e -6M) [AID78484, Type: Literature]
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19
[SID103165167]
ED50 2.7Histamine H2 receptor antagonist activity (chronotropic response to histamine) in guinea pig right atrium [AID87867, Type: Literature]Histamine H2 receptor [gi:1346291]
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20
[SID103165167]
IC50 5.523DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: confirmatory]Histamine H2 receptor [gi:123120]
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