Bookmark and Share
Cimetidine (CID 2756) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(46)
 
 
Inactive(1649)
 
 
Inconclusive(97)
 
 
Unspecified(1870)
 
 
Top Targets:
7TM GPCR Srsx(64)
 
 
 
 
MFS(56)
 
 
 
7TM GPCR Srx(47)
 
 
 
 
p450(39)
 
 
 
 
 
NR LBD PPAR(27)
 
 
 
BioAssay Types:
Confirmatory(959)
 
 
 
 
 
Screening(544)
 
 
 
Literature(381)
 
 
 
 
 
Summary(49)
 
 
 
BioActivity Types:
Potency(796)
 
 
 
 
 
IC50(206)
 
 
 
 
 
Ki(12)
 
 
 
Kd(7)
 
 
EC50(7)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 3074    Data Row: 3662   Total Pages: 74   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]
View
2
[SID103165167]
Kd 0.25119Antagonistic activity for inhibition of histamine H2 receptor from anesthetized rats [AID88493, Type: other]
View
3
[SID103165167]
Kd 0.25119Antagonistic activity by inhibition histamine H2 receptor from rats. [AID88494, Type: other]
View
4
[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]
View
5
[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]
View
6
[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]
View
7
[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]
View
8
[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]
View
9
[SID103165167]
IC50 0.781Inhibition of histamine H2 receptor [AID340249, Type: Literature]
View
10
[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]
View
11
[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]
View
12
[SID103165167]
Kd 1Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium [AID88156, Type: Literature]Histamine H2 receptor [gi:1346291]
View
13
[SID103165167]
IC50 1.02Inhibition of guinea pig histamine H2 receptor [AID566261, Type: Literature]Histamine H2 receptor [gi:1346291]
View
14
[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]
View
15
[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]
View
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]
View
17
[SID103165167]
IC50 5.523DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
View
18
[SID103165167]
IC50 5.7Inhibition of human MATE1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692195, Type: Literature]Multidrug and toxin extrusion protein 1 [gi:74731723]
View
19
[SID103165167]
IC50 12.5892Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay [AID524796, Type: Literature]
View
20
[SID104171130]
Potency 13.4591Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation [AID504834, Type: confirmatory]
View
21
[SID144208358]
Potency-Replicate_1 13.5603qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - Rad54/Ku70 mutant cell line [AID743015, Type: confirmatory]
View
22
[SID103165167]
IC50 15Inhibition of human cytochrome P450 3A4 [AID54923, Type: Literature]
View
23
[SID103165167]
IC50 20Inhibition of human OCT2 A270S mutant expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692193, Type: Literature]
View
24
[SID103165167]
IC50 23Inhibition of human OCT2 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692192, Type: Literature]Solute carrier family 22 member 2 [gi:313104182]
View
25
[SID26747359]
Potency 28.1838qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
View
26
[SID11113773]
Potency 31.6228qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450 2C19 precursor [Homo sapiens] [gi:4503219]
View
27
[SID103165167]
IC50 39Inhibition of human MATE2-K expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692196, Type: Literature]Multidrug and toxin extrusion protein 2 [gi:74727585]
View
28
[SID144208358]
Potency-Replicate_1 53.9844qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - Rev3 mutant cell line [AID743014, Type: confirmatory]
View
29
[SID103165167]
Antagonism of the positive chronotropic action of histamine in the isolated guinea pig atrium [AID77616, Type: Literature]
View
30
[SID103165167]
Elevation in glycogen level in fasting BALB/c mouse at 11.40 mg/kg, ip after 3 hrs [AID318592, Type: Literature]
View
31
[SID85209024]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
View
32
[SID85211953]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
View
33
[SID85220244]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
View
34
[SID103165167]
Histamine H2 receptor antagonist [AID742852, Type: other]Histamine H2 receptor [gi:123120]
View
35
[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]
View
36
[SID11113773]
Cytochrome panel assay with activity outcomes [AID1851_1, Type: other]cytochrome P450 2C19 precursor [Homo sapiens] [gi:4503219]
View
37
[SID103165167]
Antagonistic activity against histamine H2 receptor from guinea pig atrium [AID88010, Type: Literature]Histamine H2 receptor [gi:1346291]
View
38
[SID103165167]
Histamine H2 receptor antagonistic activity was evaluated in guinea pig atrium. [AID88019, Type: Literature]Histamine H2 receptor [gi:1346291]
View
39
[SID103165167]
Evaluated in vitro for histamine H2 receptor antagonist activity by using histamine-stimulated chronotropic response of the guinea pig atrium [AID88013, Type: Literature]Histamine H2 receptor [gi:1346291]
View
40
[SID103165167]
Cmax in human [AID692185, Type: Literature]
View
41
[SID48415780]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
View
42
[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]
View
43
[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]
View
44
[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]
View
45
[SID103165167]
Partial inhibition of human OCT2 expressed in HEK-293-Flp-In cells at 20 uM incubated for 3 mins by ASP+ substrate uptake assay [AID692190, Type: Literature]Solute carrier family 22 member 2 [gi:313104182]
View
46
[SID103165167]
Inhibition of human OCT2 expressed in HEK-293-Flp-In cells at 500 uM incubated for 3 mins by ASP+ substrate uptake assay [AID692191, Type: Literature]Solute carrier family 22 member 2 [gi:313104182]
View
47
[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]
View
48
[SID103165167]
Ki 5.7TP_TRANSPORTER: inhibition of TEA uptake (basolateral to cell) in OCT1-expressing MDCK cells [AID681574, Type: other]Solute carrier family 22 member 1 [gi:81872095]
View
49
[SID103165167]
IC50 8TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes [AID678785, Type: other]Solute carrier family 22 member 2 [gi:81882176]
View
50
[SID103165167]
Ki 9.4TP_TRANSPORTER: inhibition of TEA uptake (basolateral to cell) in OCT2-expressing MDCK cells [AID681590, Type: other]Solute carrier family 22 member 2 [gi:81872789]
View