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Maprotiline (CID 4011) - Compound BioActivity Data
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BioActivity Outcomes:
Active(99)
 
 
Inactive(925)
 
 
Inconclusive(130)
 
 
Unspecified(176)
 
 
Top Targets:
7TM GPCR Srx(46)
 
 
 
 
p450(43)
 
 
 
 
 
7TM GPCR Srsx(37)
 
 
 
 
HSD10-like SD..(12)
 
 
NR LBD GR(11)
 
 
 
 
BioAssay Types:
Confirmatory(577)
 
 
 
 
 
Screening(388)
 
 
 
 
Literature(160)
 
 
 
 
 
Summary(24)
 
 
 
 
BioActivity Types:
Potency(488)
 
 
 
 
 
IC50(167)
 
 
 
 
 
Ki(7)
 
 
 
EC50(4)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 977    Data Row: 1330   Total Pages: 27   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103189345]
Ki 0.00167Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells [AID392464, Type: Literature]Histamine H1 receptor [gi:547645]
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2
[SID103189345]
IC50 0.00879DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) [AID625269, Type: other]Histamine H1 receptor [gi:547645]
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3
[SID103189345]
Ki 0.012Inhibition of norepinephrine reuptake at NET [AID452389, Type: Literature]
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4
[SID103189345]
IC50 0.03DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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5
[SID103189345]
IC50 0.064DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) [AID625192, Type: other]5-hydroxytryptamine receptor 2A [gi:543727]
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6
[SID103189345]
IC50 0.078DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) [AID625218, Type: other]5-hydroxytryptamine receptor 2C [gi:112816]
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7
[SID103189345]
IC50 0.16DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625155, Type: other]Muscarinic acetylcholine receptor M5 [gi:543761]
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8
[SID103189345]
IC50 0.163DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) [AID625199, Type: other]Alpha-1B adrenergic receptor [gi:543734]
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9
[SID103189345]
IC50 0.292DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) [AID625202, Type: other]Alpha-2B adrenergic receptor [gi:27151763]
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10
[SID103189345]
IC50 0.336DRUGMATRIX: 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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11
[SID103189345]
IC50 0.373DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) [AID625252, Type: other]D(1A) dopamine receptor [gi:118228]
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12
[SID103189345]
IC50 0.397DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625200, Type: other]Alpha-1D adrenergic receptor [gi:1168243]
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13
[SID103189345]
IC50 0.4DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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14
[SID103189345]
Ki 0.402Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells [AID392465, Type: Literature]D(1A) dopamine receptor [gi:118228]
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15
[SID103189345]
IC50 0.413DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625154, Type: other]Muscarinic acetylcholine receptor M4 [gi:23503039]
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16
[SID103189345]
Ki 0.429Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells [AID392466, Type: Literature]D(1B) dopamine receptor [gi:118214]
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17
[SID103189345]
IC50 0.446DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888)) [AID625234, Type: other]
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18
[SID103189345]
IC50 0.473DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625153, Type: other]Muscarinic acetylcholine receptor M3 [gi:113125]
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19
[SID103189345]
Ki 0.504Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells [AID392468, Type: Literature]D(3) dopamine receptor [gi:1169206]
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20
[SID90341780]
Potency 0.5212High 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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21
[SID103189345]
IC50 0.567DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) [AID625198, Type: other]Alpha-1D adrenergic receptor [gi:1168244]
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22
[SID103189345]
IC50 0.593DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625151, Type: other]Muscarinic acetylcholine receptor M1 [gi:113118]
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23
[SID103189345]
IC50 0.645DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) [AID625254, Type: other]D(3) dopamine receptor [gi:1169206]
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24
[SID103189345]
Ki 0.665Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells [AID392467, Type: Literature]D(2) dopamine receptor [gi:118206]
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25
[SID103189345]
IC50 0.892DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) [AID625221, Type: other]5-hydroxytryptamine receptor 6 [gi:1703010]
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26
[SID103189345]
IC50 1.824DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) [AID625201, Type: other]Alpha-2A adrenergic receptor [gi:1351829]
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27
[SID103189345]
IC50 1.927DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625152, Type: other]Muscarinic acetylcholine receptor M2 [gi:113122]
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28
[SID90341780]
Potency 2.2387HTS Assay for Allosteric Agonists of the Human D1 Dopamine Receptor: Primary Screen for Antagonists [AID488983, Type: confirmatory]D(1A) dopamine receptor [Homo sapiens] [gi:4503383]
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29
[SID11111502]
Potency 2.2387qHTS 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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30
[SID11113802]
Potency 2.5119qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450 3A4 isoform 1 [Homo sapiens] [gi:13435386]
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31
[SID11112599]
Potency 2.5119qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450 3A4 isoform 1 [Homo sapiens] [gi:13435386]
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32
[SID103189345]
IC50 2.572DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin) [AID625225, Type: other]
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33
[SID124880790]
Potency 2.8184qHTS 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
[SID103189345]
IC50 2.91DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
View
35
[SID103189345]
IC50 3.044DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) [AID625203, Type: other]Alpha-2C adrenergic receptor [gi:20141211]
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36
[SID11111502]
Potency 3.1623qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450 3A4 isoform 1 [Homo sapiens] [gi:13435386]
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37
[SID103189345]
IC50 3.286DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem) [AID625215, Type: other]
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38
[SID103189345]
IC50 3.463DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) [AID625253, Type: other]D(2) dopamine receptor [gi:118206]
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39
[SID124880792]
Potency 3.5481qHTS 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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40
[SID11112599]
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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41
[SID50085871]
IC50_Mean 4.28Dose response confirmation of uHTS inhibitor hits of the mitochondrial permeability transition pore via an absorbance assay [AID651561, Type: confirmatory]
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42
[SID103189345]
IC50 4.322DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) [AID625251, Type: other]Cytochrome P450 3A4 [gi:116241312]
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43
[SID11111502]
Potency 4.4668qHTS 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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44
[SID11113802]
Potency 5.0119qHTS Assay for Anthrax Lethal Toxin Internalization [AID912, Type: confirmatory]lethal factor [Bacillus anthracis str. A2012] [gi:21392848]
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45
[SID144203751]
Potency 5.0119qHTS 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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46
[SID144203751]
Potency-Replicate_1 7.4978qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway - cell viability counter screen [AID743064, Type: confirmatory]
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47
[SID144203751]
Potency-Replicate_1 9.4392qHTS 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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48
[SID124880790]
Potency 9.4411qHTS 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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49
[SID11113802]
Potency 10qHTS for inhibitors of ROR gamma transcriptional activity [AID2551, Type: confirmatory]nuclear receptor ROR-gamma [Mus musculus] [gi:188536040]
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50
[SID144203751]
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 - wild type cell line [AID743012, Type: confirmatory]
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