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Loperamide (CID 3955) - Compound BioActivity Data
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BioActivity Outcomes:
Active(141)
 
 
Inactive(406)
 
 
Inconclusive(104)
 
 
Unspecified(204)
 
 
Top Targets:
p450(39)
 
 
 
 
 
7TM GPCR Srx(28)
 
 
 
 
 
7TM GPCR Srsx(19)
 
 
 
 
ABC MTABC3 MD..(13)
 
 
HSD10-like SD..(12)
 
 
BioAssay Types:
Confirmatory(461)
 
 
 
 
Literature(159)
 
 
 
 
 
Screening(27)
 
 
 
Summary(24)
 
 
 
BioActivity Types:
Potency(406)
 
 
 
 
IC50(120)
 
 
 
 
EC50(5)
 
 
Ki(4)
 
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 539    Data Row: 855   Total Pages: 18   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103220983]
Ki 0.00016Binding affinity for Mu opioid receptor of rat brain [AID238656, Type: Literature]
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2
[SID103220983]
Ki 0.00053Binding affinity for recombinant human mu-opioid receptor was determined by using [3H]- diprenophine radioligand [AID239449, Type: Literature]Mu-type opioid receptor [gi:2851402]
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3
[SID103220983]
IC50 0.00145DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625163, Type: other]Mu-type opioid receptor [gi:2851402]
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4
[SID11113732]
Potency 0.0158qHTS 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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5
[SID103220983]
Ki 0.0501Binding affinity for delta opioid receptor of rat brain [AID238717, Type: Literature]
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6
[SID103220983]
EC50 0.058Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes [AID246293, Type: Literature]Mu-type opioid receptor [gi:3024265]
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7
[SID103220983]
IC50 0.093DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin) [AID625225, Type: other]
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8
[SID103220983]
EC50 0.156Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes [AID246309, Type: Literature]
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9
[SID103220983]
IC50 0.221DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem) [AID625215, Type: other]
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10
[SID103220983]
IC50 0.27Inhibition 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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11
[SID103220983]
EC50 0.4889Inhibition of isolated guinea pig ileum contraction induced by electrical stimulation [AID246131, Type: Literature]
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12
[SID103220983]
IC50 0.589DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888)) [AID625234, Type: other]
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13
[SID103220983]
IC50 0.628DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) [AID625223, Type: other]Sigma non-opioid intracellular receptor 1 [gi:74752153]
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14
[SID103220983]
IC50 0.896DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) [AID625161, Type: other]Delta-type opioid receptor [gi:311033488]
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15
[SID103220983]
IC50 0.965DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) [AID625199, Type: other]Alpha-1B adrenergic receptor [gi:543734]
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16
[SID11111380]
Potency 1.2589qHTS Assay for Agonists of the Thyroid Stimulating Hormone Receptor: Activators of Intracellular cAMP Concentrations in Parental HEK 293 [AID938, Type: confirmatory]thyroid stimulating hormone receptor [Homo sapiens] [gi:38016895]
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17
[SID103220983]
IC50 1.337DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) [AID625254, Type: other]D(3) dopamine receptor [gi:1169206]
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18
[SID103220983]
IC50 1.379DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil) [AID625224, Type: other]
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19
[SID103220983]
IC50 2DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625249, Type: other]Cytochrome P450 2D6 [gi:84028191]
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20
[SID103220983]
IC50 2.202DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: other]Sodium-dependent serotonin transporter [gi:400630]
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21
[SID104171181]
Potency 2.3934Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 48 hour incubation [AID504832, Type: confirmatory]
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22
[SID103220983]
EC50 3Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay [AID547622, Type: Literature]
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23
[SID103220983]
IC50 3.005DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) [AID625205, Type: other]Beta-2 adrenergic receptor [gi:296439450]
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24
[SID103220983]
IC50 3.081DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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25
[SID103220983]
IC50 3.125DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625162, Type: other]Kappa-type opioid receptor [gi:116242691]
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26
[SID103220983]
IC50 4.105DRUGMATRIX: 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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27
[SID90340730]
Potency 4.1078qHTS for inhibitors of binding or entry into cells for Marburg Virus [AID540276, Type: confirmatory]gene 4 small orf - Marburg virus [gi:420597]
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28
[SID90340730]
Potency 4.1078qHTS for Inhibitors of binding or entry into cells for Lassa Virus [AID540256, Type: confirmatory]
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29
[SID11111380]
Potency 5.0119qHTS Assay for Activators of Cytochrome P450 3A4 [AID885, Type: confirmatory]cytochrome P450 3A4 isoform 1 [Homo sapiens] [gi:13435386]
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30
[SID103220983]
Kd 5.9Binding affinity to human recombinant Tie2 by SPR assay [AID653693, Type: Literature]Angiopoietin-1 receptor [gi:218511853]
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31
[SID144203731]
Potency-Replicate_1 5.9557qHTS 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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32
[SID103220983]
IC50 6.219DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625198, Type: other]Alpha-1D adrenergic receptor [gi:1168244]
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33
[SID144203731]
Potency 6.3096qHTS 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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34
[SID144203731]
Potency 6.6838qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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35
[SID144203731]
Potency-Replicate_1 8.4127qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway - cell viability counter screen [AID743064, Type: confirmatory]
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36
[SID144203731]
Potency-Replicate_1 8.4127qHTS 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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37
[SID144203731]
Potency 8.4144qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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38
[SID124880551]
Potency 8.9125qHTS 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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39
[SID124880551]
Potency 9.7264qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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40
[SID124880551]
Potency 9.7264qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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41
[SID11112740]
Potency 10qHTS 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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42
[SID124880553]
Potency 10qHTS 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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43
[SID144203731]
Potency-Replicate_1 10.5909qHTS 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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44
[SID144203731]
Potency-Replicate_1 10.5909qHTS 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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45
[SID170464852]
Potency-Replicate_1 11.8823qHTS assay to identify small molecule antagonists of the peroxisome proliferator-activated receptor delta (PPARd) signaling pathway - cell viability counter screen [AID743213, Type: confirmatory]
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46
[SID170464852]
Potency-Replicate_1 11.8823qHTS assay to identify small molecule agonists of the farnesoid-X-receptor (FXR) signaling pathway - cell viability counter screen [AID743218, Type: confirmatory]
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47
[SID103220983]
EC50 12Cytotoxicity against BESM cells after 88 hrs by HTS assay [AID547621, Type: Literature]
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48
[SID90340730]
Potency 13.0918Cytometry Cell-Based qHTS for Inhibitors of the mTORC1 Signaling Pathway in MEF cells [AID2668, Type: confirmatory]serine/threonine-protein kinase mTOR [Homo sapiens] [gi:4826730]
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49
[SID144203731]
Potency-Replicate_1 13.3332qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathway using the MDA cell line [AID743042, Type: confirmatory]AR protein [Homo sapiens] [gi:124375976]
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50
[SID90340730]
Potency 18.4927High Content Imaging Cell-Based qHTS for Inhibitors of the mTORC1 Signaling Pathway in MEF Cells [AID2667, Type: confirmatory]serine/threonine-protein kinase mTOR [Homo sapiens] [gi:4826730]
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