Cimetidine (CID 2756) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(35)
 
 
Inactive(1342)
 
 
Inconclusive(79)
 
 
Unspecified(1831)
 
 
Top Targets:
p450(36)
 
 
 
 
 
7TM GPCR Srx(35)
 
 
 
MFS(27)
 
 
7TM GPCR Srsx(23)
 
 
 
 
ABC MTABC3 MD..(21)
 
 
 
BioAssay Types:
Confirmatory(758)
 
 
 
 
 
Screening(478)
 
 
 
Literature(358)
 
 
 
 
 
Summary(1)
 
 
BioActivity Types:
Potency(571)
 
 
 
 
 
IC50(195)
 
 
 
 
 
Ki(12)
 
 
 
EC50(7)
 
 
Kd(7)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 2886    Data Row: 3287   Total Pages: 66   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103165167]
IC50 0.18Displacement of radiolabeled cimetidine from human histamine H2 receptor [AID346426, Type: Literature]Histamine H2 receptor [gi:123120]
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2
[SID103165167]
IC50 0.18Displacement of radiolabeled cimetidine from human histamine H2 receptor [AID346426, 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: other]
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5
[SID103165167]
Kd 0.25119Antagonistic activity by inhibition histamine H2 receptor from rats. [AID88494, Type: other]
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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]
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7
[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]
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8
[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]
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9
[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]
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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]
IC50 0.781Inhibition of histamine H2 receptor [AID340249, Type: Literature]
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12
[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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13
[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]
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14
[SID103165167]
Kd 1Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium [AID88156, Type: Literature]
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15
[SID103165167]
IC50 1.02Inhibition of guinea pig histamine H2 receptor [AID566261, Type: Literature]Histamine H2 receptor [gi:1346291]
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16
[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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17
[SID103165167]
ED50 2.7Histamine H2 receptor antagonist activity (chronotropic response to histamine) in guinea pig right atrium [AID87867, Type: Literature]
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18
[SID103165167]
IC50 5.523DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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19
[SID103165167]
IC50 5.523DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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20
[SID103165167]
IC50 5.523DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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21
[SID103165167]
IC50 12.5892Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay [AID524796, Type: Literature]
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22
[SID104171130]
Potency 13.4591Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation [AID504834, Type: confirmatory]
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23
[SID103165167]
IC50 15Inhibition of human cytochrome P450 3A4 [AID54923, Type: Literature]
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24
[SID26747359]
Potency 28.1838qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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25
[SID26747359]
Potency 28.1838qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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26
[SID11113773]
Potency 31.6228qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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27
[SID11113773]
Potency 31.6228qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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28
[SID11113773]
 Cytochrome panel assay with activity outcomes [AID1851_1, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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29
[SID11113773]
 Cytochrome panel assay with activity outcomes [AID1851_1, Type: other]cytochrome P450, family 2, subfamily C, polypeptide 19 [Homo sapiens] [gi:4503219]
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30
[SID103165167]
 Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins [AID678712, Type: Literature]Cytochrome P450 1A2 [gi:117144]
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31
[SID103165167]
 Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins [AID678712, Type: Literature]Cytochrome P450 1A2 [gi:117144]
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32
[SID103165167]
 Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins [AID678712, Type: Literature]Cytochrome P450 1A2 [gi:117144]
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33
[SID103165167]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins [AID678716, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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34
[SID103165167]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins [AID678716, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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35
[SID103165167]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins [AID678716, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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36
[SID103165167]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins [AID678717, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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37
[SID103165167]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins [AID678717, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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38
[SID103165167]
 Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins [AID678717, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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39
[SID85220244]
 Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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40
[SID48415780]
 DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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41
[SID103165167]
 Antagonism of the positive chronotropic action of histamine in the isolated guinea pig atrium [AID77616, Type: Literature]
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42
[SID103165167]
 Antagonistic activity against histamine H2 receptor from guinea pig atrium [AID88010, Type: Literature]
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43
[SID103165167]
 Evaluated in vitro for histamine H2 receptor antagonist activity by using histamine-stimulated chronotropic response of the guinea pig atrium [AID88013, Type: Literature]
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44
[SID103165167]
 Histamine H2 receptor antagonistic activity was evaluated in guinea pig atrium. [AID88019, Type: Literature]
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45
[SID103165167]
 Elevation in glycogen level in fasting BALB/c mouse at 11.40 mg/kg, ip after 3 hrs [AID318592, Type: Literature]
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46
[SID85209024]
 Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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47
[SID85211953]
 Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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48
[SID103165167]
 Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins [AID678715, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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49
[SID103165167]
 Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins [AID678715, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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50
[SID103165167]
IC50 0.59TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes [AID678794, Type: other]Solute carrier family 22 member 1 [gi:189046191]
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