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Loxapine (CID 3964) - Compound BioActivity Data
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BioActivity Outcomes:
Active(40)
 
 
Inactive(79)
 
 
Inconclusive(5)
 
 
Unspecified(49)
 
 
Top Targets:
7TM GPCR Srx(8)
 
 
 
 
7TM GPCR Srsx(6)
 
 
 
Pyr redox dim(4)
 
 
PIKKc TOR(4)
 
 
Hexokinase 2(3)
 
 
BioAssay Types:
Literature(82)
 
 
 
 
 
Confirmatory(70)
 
 
 
 
Screening(14)
 
 
BioActivity Types:
Potency(69)
 
 
 
 
Ki(10)
 
 
IC50(9)
 
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 161    Data Row: 173   Total Pages: 4   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103218455]
Ki 0.00242Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting [AID659850, Type: Literature]5-hydroxytryptamine receptor 2A [gi:543727]
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2
[SID103218455]
Ki 0.0049Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor [AID64202, Type: Literature]
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3
[SID103218455]
Ki 0.0049Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells [AID65954, Type: Literature]
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4
[SID103218455]
IC50 0.006Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand [AID5483, Type: Literature]
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5
[SID103218455]
Ki 0.009Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting [AID659851, Type: Literature]D(4) dopamine receptor [gi:1345939]
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6
[SID103218455]
IC50 0.014Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2 [AID63865, Type: Literature]
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7
[SID103218455]
Ki 0.015Binding affinity towards human 5-hydroxytryptamine 6 receptor [AID6563, Type: Literature]
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8
[SID103218455]
IC50 0.018In vitro binding affinity towards Alpha-1 adrenergic receptor by the displacement of [3H]prazosin radioligand in rat cortical homogenates [AID36855, Type: Literature]
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9
[SID103218455]
Ki 0.021Affinity was evaluated by inhibition of [3H]spiperone binding to COS cells transfected with human dopamine D-2(long) receptor [AID64197, Type: Literature]
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10
[SID103218455]
Ki 0.021Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells [AID64327, Type: Literature]
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11
[SID103218455]
Ki 0.021In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand [AID65733, Type: Literature]
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12
[SID103218455]
IC50 0.022Binding affinity towards human Dopamine receptor D3 [AID64825, Type: Literature]
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13
[SID103218455]
Ki 0.043Binding affinity towards rat 5-hydroxytryptamine 7 receptor [AID6648, Type: Literature]
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14
[SID103218455]
Ki 0.05Binding affinity for human 5-hydroxytryptamine 6 receptor [AID238747, Type: Literature]5-hydroxytryptamine receptor 6 [gi:1703010]
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15
[SID103218455]
IC50 0.054Compound was tested in vitro for its binding affinity towards human Dopamine receptor D2 [AID61306, Type: Literature]
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16
[SID90341467]
Potency 0.3981HTS 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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17
[SID103218455]
IC50 1Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand [AID87514, Type: Literature]
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18
[SID103218455]
IC50 1Compound was tested in vitro for its binding affinity towards 5-hydroxytryptamine 2C receptor from rat using [3H]mesulergine as radioligand [AID5704, Type: Literature]
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19
[SID103218455]
IC50 5.5Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells [AID141053, Type: Literature]
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20
[SID90341467]
Potency 11.5774qHTS 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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21
[SID50103874]
Potency 16.3601qHTS 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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22
[SID50104024]
Potency 16.3601qHTS 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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23
[SID50104025]
Potency 16.3601qHTS 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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24
[SID50104026]
Potency 16.3601qHTS 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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25
[SID103218455]
Km 27Binding affinity against human UDP Glucuronosyltransferase 1A4 (UGT1A4) [AID214939, Type: Literature]
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26
[SID85209777]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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27
[SID103218455]
FDA HLAED, liver enzyme composite activity [AID588214, Type: Literature]
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28
[SID103218455]
FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase [AID588216, Type: Literature]
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29
[SID103218455]
FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase [AID588217, Type: Literature]
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30
[SID103218455]
Serotonin 2a (5-HT2a) receptor antagonist [AID742882, Type: other]5-hydroxytryptamine receptor 2A [gi:543727]
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31
[SID48416188]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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32
[SID103218455]
Serotonin 2c (5-HT2c) receptor antagonist [AID742885, Type: other]5-hydroxytryptamine receptor 2C [gi:112816]
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33
[SID103218455]
D2-like dopamine receptor antagonist [AID742743, Type: other]D(2) dopamine receptor [gi:118206]
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34
[SID103218455]
D2-like dopamine receptor antagonist [AID742743, Type: other]D(4) dopamine receptor [gi:1345939]
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35
[SID103218455]
D2-like dopamine receptor antagonist [AID742743, Type: other]D(3) dopamine receptor [gi:1169206]
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36
[SID135650533]
Antagonists at Human 5-Hydroxytryptamine receptor 5-HT6 [AID624192, Type: Literature]5-hydroxytryptamine receptor 6 [Homo sapiens] [gi:4504545]
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37
[SID135650533]
Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT7 [AID624180, Type: Literature]5-hydroxytryptamine receptor 7 [Rattus norvegicus] [gi:12621102]
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38
[SID135650533]
Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT6 [AID624190, Type: Literature]5-hydroxytryptamine receptor 6 [Rattus norvegicus] [gi:13242259]
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39
[SID135650533]
Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A [AID624223, Type: Literature]5-hydroxytryptamine receptor 2A isoform 2 [Homo sapiens] [gi:260099679]
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40
[SID135650533]
Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2C [AID624209, Type: Literature]5-hydroxytryptamine receptor 2C isoform b precursor [Homo sapiens] [gi:377520139]
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41
[SID103218455]
Kd Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells [AID266654, Type: Literature]Histamine H4 receptor [gi:14194819]
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42
[SID103218455]
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay [AID266655, Type: Literature]Histamine H4 receptor [gi:14194819]
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43
[SID103218455]
Agonist activity at human histamine H4 receptor transfected in SK-N-MC cells [AID266668, Type: Literature]Histamine H4 receptor [gi:14194819]
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44
[SID103218455]
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 cells at 10'-6 M after 60 mins by liquid scintillation counting [AID659857, Type: Literature]Alpha-2A adrenergic receptor [gi:1351829]
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45
[SID103218455]
Specific activity of expressed human recombinant UGT1A3 [AID624607, Type: Literature]UDP-glucuronosyltransferase 1-4 [gi:136731]
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46
[SID103218455]
Specific activity of expressed human recombinant UGT1A4 [AID624608, Type: Literature]UDP-glucuronosyltransferase 1-4 [gi:136731]
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47
[SID103218455]
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells at 10'-6 M after 60 mins by liquid scintillation counting [AID659855, Type: Literature]5-hydroxytryptamine receptor 1A [gi:231454]
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48
[SID103218455]
FDA HLAED, lactate dehydrogenase (LDH) increase [AID588218, Type: Literature]
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49
[SID103218455]
FDA HLAED, gamma-glutamyl transferase (GGT) increase [AID588219, Type: Literature]
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50
[SID103218455]
Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset [AID588220, Type: Literature]
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