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Diphenhydramine (CID 3100) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(103)
 
 
Inactive(754)
 
 
Inconclusive(91)
 
 
Unspecified(223)
 
 
Top Targets:
7TM GPCR Srx(37)
 
 
 
 
p450(34)
 
 
 
 
 
7TM GPCR Srsx(31)
 
 
 
 
B zip1(9)
 
 
 
CAP ED(9)
 
 
 
BioAssay Types:
Confirmatory(506)
 
 
 
 
 
Screening(284)
 
 
 
Literature(184)
 
 
 
 
 
Summary(24)
 
 
 
BioActivity Types:
Potency(417)
 
 
 
 
 
IC50(132)
 
 
 
 
Ki(2)
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 919    Data Row: 1171   Total Pages: 24   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103189265]
IC50 0.001Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum [AID86581, Type: Literature]Histamine H1 receptor [gi:399889]
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2
[SID103189265]
Kd 0.01175Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins [AID626461, Type: Literature]Histamine H1 receptor [gi:399889]
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3
[SID103189265]
Ki 0.01479Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting [AID626411, Type: Literature]Histamine H1 receptor [gi:547645]
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4
[SID103189265]
IC50 0.162DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625155, Type: other]Muscarinic acetylcholine receptor M5 [gi:543761]
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5
[SID103189265]
IC50 0.171DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) [AID625269, Type: other]Histamine H1 receptor [gi:547645]
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6
[SID11111059]
Potency 0.1995qHTS Assay for Antagonists of Acetylcholine Muscarinic M1 Receptor: Kinetic Measurement of Intracellular Calcium Response [AID943, Type: confirmatory]muscarinic acetylcholine receptor M1 [Rattus norvegicus] [gi:18249941]
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7
[SID103189265]
IC50 0.346DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625151, Type: other]Muscarinic acetylcholine receptor M1 [gi:113118]
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8
[SID103189265]
IC50 0.372DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625154, Type: other]Muscarinic acetylcholine receptor M4 [gi:23503039]
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9
[SID103189265]
IC50 0.647DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625153, Type: other]Muscarinic acetylcholine receptor M3 [gi:113125]
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10
[SID103189265]
IC50 0.98DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) [AID625218, Type: other]5-hydroxytryptamine receptor 2C [gi:112816]
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11
[SID103189265]
IC50 1.05DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625152, Type: other]Muscarinic acetylcholine receptor M2 [gi:113122]
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12
[SID103189265]
IC50 1.118DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) [AID625217, Type: other]5-hydroxytryptamine receptor 2B [gi:1168220]
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13
[SID103189265]
IC50 1.295DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) [AID625192, Type: other]5-hydroxytryptamine receptor 2A [gi:543727]
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14
[SID124879863]
Potency 1.495qHTS profiling of Chloroquine Analogs as inhibitors of Plasmodium falciparum (DD2) proliferation [AID743326, Type: confirmatory]
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15
[SID11111059]
Potency 2.5119qHTS Assay for Antagonists of Acetylcholine Muscarinic M1 Receptor: Measurement of IP-One Response [AID944, Type: confirmatory]muscarinic acetylcholine receptor M1 [Rattus norvegicus] [gi:18249941]
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16
[SID103189265]
IC50 2.5704Inhibition of human ERG [AID576612, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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17
[SID103189265]
IC50 3.542DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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18
[SID11111060]
Potency 3.9811qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2D6 [AID891, Type: confirmatory]cytochrome P450 2D6 isoform 1 [Homo sapiens] [gi:40805836]
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19
[SID103189265]
IC50 6Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex [AID205267, Type: Literature]
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20
[SID103189265]
IC50 7.28DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888)) [AID625234, Type: other]
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21
[SID11111059]
Potency 12.5893qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2D6 [AID891, Type: confirmatory]cytochrome P450 2D6 isoform 1 [Homo sapiens] [gi:40805836]
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22
[SID144203678]
Potency-Replicate_1 26.6032qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway [AID743065, Type: confirmatory]thyroid hormone receptor beta isoform 2 [Rattus norvegicus] [gi:399498506]
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23
[SID144203678]
Potency-Replicate_1 26.6032qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway - cell viability counter screen [AID743064, Type: confirmatory]
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24
[SID103189265]
IC50 26.9153Inhibitory concentration against potassium channel HERG [AID243151, Type: Literature]
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25
[SID103189265]
IC50 26.9153Inhibition of human Potassium channel HERG expressed in mammalian cells [AID161281, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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26
[SID103189265]
IC50 26.9153Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique [AID408340, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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27
[SID144203678]
Potency 28.1838qHTS for Inhibitors of binding or entry into cells for Marburg Virus [AID720532, Type: confirmatory]gene 4 small orf - Marburg virus [gi:420597]
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28
[SID144203678]
Potency-Replicate_1 29.8493qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - wild type cell line [AID743012, Type: confirmatory]
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29
[SID144203678]
Potency-Replicate_1 29.8493qHTS 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]
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30
[SID144203678]
Potency-Replicate_1 29.8493qHTS 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]
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31
[SID103189265]
IC50 31.859DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) [AID625171, Type: other]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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32
[SID103189265]
Ki 42.658Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting [AID626460, Type: Literature]Histamine H4 receptor [gi:14194819]
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33
[SID85148365]
Fluorescence-based cell-based primary high throughput screening assay to identify antagonists of the human cholinergic receptor, muscarinic 5 (CHRM5) [AID624040, Type: screening]muscarinic acetylcholine receptor M5 [Homo sapiens] [gi:7108336]
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34
[SID103189265]
Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins [AID678714, Type: Literature]Cytochrome P450 2C19 [gi:60416369]
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35
[SID11111060]
Cytochrome panel assay with activity outcomes [AID1851_2, Type: other]cytochrome P450 2D6 isoform 2 [Homo sapiens] [gi:68509921]
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36
[SID11111059]
Cytochrome panel assay with activity outcomes [AID1851_2, Type: other]cytochrome P450 2D6 isoform 2 [Homo sapiens] [gi:68509921]
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37
[SID11111060]
p450-cyp1a2 [AID410, Type: confirmatory]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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38
[SID11111059]
p450-cyp1a2 [AID410, Type: confirmatory]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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39
[SID103189265]
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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40
[SID85148365]
qHTS of D3 Dopamine Receptor Antagonist: qHTS [AID652054, Type: screening]D(3) dopamine receptor isoform e [Homo sapiens] [gi:89191863]
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41
[SID103189265]
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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42
[SID103189265]
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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43
[SID103189265]
Antiallergic activity in IgE/Ag-induced passive cutaneous anaphylactic ICR mouse model injected with DNP-HSA-Evans blue dye post DNP-IgE challenge at 50 mg/kg, po 1 hr before antigenic challenge measured after 2 hrs post IgE/Ag challenge [AID699844, Type: Literature]
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44
[SID85209057]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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45
[SID26751623]
qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749_19, Type: Literature]
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46
[SID48415909]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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47
[SID103189265]
Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604020, Type: Literature]
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48
[SID104171144]
qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749_3, Type: Literature]
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49
[SID103189265]
Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis [AID678721, Type: Literature]
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50
[SID511392]
NCI human tumor cell line growth inhibition assay. Data for the NCI-H23 Non-Small Cell Lung cell line [AID1, Type: confirmatory]
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