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Chlorpheniramine (CID 2725) - Compound BioActivity Data
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BioActivity Outcomes:
Active(23)
 
 
Inactive(94)
 
 
Inconclusive(6)
 
 
Unspecified(1491)
 
 
Top Targets:
ABC MTABC3 MD..(5)
 
 
CAP ED(4)
 
 
 
Pyr redox dim(4)
 
 
7TM GPCR Srx(4)
 
 
PIKKc TOR(4)
 
 
BioAssay Types:
Literature(128)
 
 
 
 
Confirmatory(76)
 
 
 
Screening(17)
 
 
BioActivity Types:
Potency(75)
 
 
 
IC50(20)
 
 
 
 
Ki(4)
 
 
Kd(2)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1606    Data Row: 1614   Total Pages: 33   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103173276]
Ki 0.002Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes [AID87525, Type: Literature]
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2
[SID103173276]
Kd 0.0037Dissociation constant (KD) of the compound [AID17268, Type: Literature]
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3
[SID103173276]
Kd 0.00398pA2 value is determined compared to standard H1-antagonists [AID24863, Type: Literature]
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4
[SID103173276]
Ki 0.0055Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes [AID87519, Type: Literature]
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5
[SID103173276]
Ki 0.0055Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand [AID87521, Type: Literature]
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6
[SID103173276]
Ki 0.007Binding affinity to histamine H1 receptor [AID591511, Type: Literature]
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7
[SID103173276]
IC50 0.0088Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex [AID86586, Type: Literature]Histamine H1 receptor [gi:399889]
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8
[SID103173276]
IC50 0.066Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells [AID351895, Type: Literature]Histamine H1 receptor [gi:547645]
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9
[SID103173276]
IC50 1.1Inhibitory concentration against IKr potassium channel [AID240820, Type: Literature]
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10
[SID103173276]
IC50 3.9Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes by SYBR green assay [AID351890, Type: Literature]
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11
[SID103173276]
IC50 10Inhibition 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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12
[SID103173276]
IC50 20.893Inhibitory concentration against potassium channel HERG [AID243151, Type: Literature]
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13
[SID103173276]
IC50 20.893Inhibition 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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14
[SID103173276]
IC50 20.893Inhibition 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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15
[SID103173276]
IC50 20.893Inhibition of human ERG [AID576612, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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16
[SID103173276]
IC50 33.4Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay [AID351891, Type: Literature]
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17
[SID103173276]
IC50 34Inhibition of MBTD1 by alpha-screening [AID537070, Type: Literature]
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18
[SID103173276]
IC50 41Inhibition of L3MBTL1 by alpha-screening [AID537067, Type: Literature]
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19
[SID103173276]
IC50 42Inhibition of L3MBTL3 by alpha-screening [AID537068, Type: Literature]
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20
[SID103173276]
Displacement of [3H](-)-trans-H2-PAT from Guinea pig histamine H2 receptors. [AID88008, Type: Literature]Histamine H2 receptor [gi:1346291]
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21
[SID48415764]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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22
[SID85208874]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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23
[SID103173276]
Compound was tested for the displacement of [3H]mepyramine from Histamine H1 receptor by competition binding assay [AID88625, Type: Literature]Histamine H1 receptor [gi:399889]
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24
[SID103173276]
IC50 14TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells [AID681348, Type: other]Solute carrier family 22 member 1 [gi:81872095]
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25
[SID103173276]
IC50 26TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells [AID681345, Type: other]Solute carrier family 22 member 2 [gi:81872789]
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26
[SID103173276]
IC50 50In vitro antagonist activity, determined by 50% inhibition of PAF-induced platelet aggregation of human platelet rich plasma when challenged with PAF [AID92393, Type: Literature]
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27
[SID103173276]
IC50 50Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF. [AID89260, Type: Literature]
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28
[SID103173276]
IC50 61.2Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes by SYBR green assay [AID351893, Type: Literature]
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29
[SID103173276]
IC50 100Inhibition of L3MBTL4 by alpha-screening [AID537069, Type: Literature]
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30
[SID103173276]
Specific activity of expressed human recombinant UGT1A4 [AID624608, Type: Literature]UDP-glucuronosyltransferase 1-4 [gi:136731]
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31
[SID103173276]
Evaluated for antagonist activity against histamine H1 receptor and represented as KB. [AID86607, Type: Literature]Histamine H1 receptor [gi:399889]
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32
[SID103173276]
Compound is evaluated for the inhibition of H1-receptor antagonists of histamine-induced skin wheal formation in the guinea pig with a pretreatment interval prior to histamine challenge at 1 h [AID74208, Type: Literature]Histamine H1 receptor [gi:399889]
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33
[SID103173276]
Compound is evaluated for the inhibition of H1-receptor antagonists of histamine-induced skin wheal formation in the guinea pig with a pretreatment interval prior to histamine challenge at 18 h [AID74209, Type: Literature]Histamine H1 receptor [gi:399889]
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34
[SID103173276]
Evaluated for antagonist activity against histamine H3 receptor and represented as KB [AID89555, Type: Literature]
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35
[SID103173276]
Evaluated for antagonist activity against histamine H3 receptor and represented as KB. [AID89556, Type: Literature]
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36
[SID103173276]
Evaluated for antagonist activity against histamine H1 receptor and represented as KB [AID87677, Type: Literature]
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37
[SID103173276]
Dissociation constant, pKa of the compound [AID467611, Type: Literature]
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38
[SID103173276]
Fraction unbound in human plasma [AID467612, Type: Literature]
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39
[SID103173276]
Volume of distribution at steady state in human [AID467613, Type: Literature]
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40
[SID103173276]
Absolute bioavailability in human [AID481439, Type: Literature]
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41
[SID103173276]
Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells [AID481442, Type: Literature]
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42
[SID103173276]
Intrinsic solubility of the compound in water [AID515780, Type: Literature]
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43
[SID103173276]
Activity at L3MBTL1 at 100 uM [AID537066, Type: Literature]
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44
[SID103173276]
Volume of distribution at steady state in human after iv administration [AID540209, Type: Literature]
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45
[SID103173276]
Clearance in human after iv administration [AID540210, Type: Literature]
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46
[SID103173276]
Fraction unbound in human after iv administration [AID540211, Type: Literature]
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47
[SID103173276]
Mean residence time in human after iv administration [AID540212, Type: Literature]
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48
[SID103173276]
Half life in human after iv administration [AID540213, Type: Literature]
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49
[SID103173276]
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans [AID588211, Type: Literature]
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50
[SID103173276]
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents [AID588212, Type: Literature]
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