Loxapine (CID 3964) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(35)
 
 
Inactive(66)
 
 
Inconclusive(5)
 
 
Unspecified(49)
 
 
Top Targets:
7TM GPCR Srx(7)
 
 
 
 
PIKKc TOR(4)
 
 
Pyr redox dim(4)
 
 
BRLZ(2)
 
 
PIN FEN1(2)
 
 
 
BioAssay Types:
Literature(82)
 
 
 
 
 
Confirmatory(56)
 
 
 
 
Screening(15)
 
 
BioActivity Types:
Potency(56)
 
 
 
 
Ki(10)
 
 
IC50(8)
 
 
Kd(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 151    Data Row: 155   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 0.00242Displacement 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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3
[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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4
[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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5
[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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6
[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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7
[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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8
[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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9
[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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10
[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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11
[SID103218455]
Ki 0.015Binding affinity towards human 5-hydroxytryptamine 6 receptor [AID6563, Type: Literature]
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12
[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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13
[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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14
[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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15
[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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16
[SID103218455]
IC50 0.022Binding affinity towards human Dopamine receptor D3 [AID64825, Type: Literature]
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17
[SID103218455]
Ki 0.043Binding affinity towards rat 5-hydroxytryptamine 7 receptor [AID6648, Type: Literature]
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18
[SID103218455]
Ki 0.05Binding affinity for human 5-hydroxytryptamine 6 receptor [AID238747, Type: Literature]5-hydroxytryptamine receptor 6 [gi:1703010]
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19
[SID103218455]
Ki 0.05Binding affinity for human 5-hydroxytryptamine 6 receptor [AID238747, Type: Literature]5-hydroxytryptamine receptor 6 [gi:1703010]
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20
[SID103218455]
Ki 0.05Binding affinity for human 5-hydroxytryptamine 6 receptor [AID238747, Type: Literature]5-hydroxytryptamine receptor 6 [gi:1703010]
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21
[SID103218455]
IC50 0.054Compound was tested in vitro for its binding affinity towards human Dopamine receptor D2 [AID61306, Type: Literature]
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22
[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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23
[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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24
[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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25
[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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26
[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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27
[SID103218455]
IC50 1Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand [AID87514, Type: Literature]
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28
[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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29
[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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30
[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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31
[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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32
[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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33
[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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34
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT6 [AID624192, Type: Literature]HTR6 gene product [Homo sapiens] [gi:4504545]
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35
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT6 [AID624192, Type: Literature]HTR6 gene product [Homo sapiens] [gi:4504545]
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36
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT6 [AID624192, Type: Literature]HTR6 gene product [Homo sapiens] [gi:4504545]
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37
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A [AID624223, Type: Literature]HTR2A gene product [Homo sapiens] [gi:260099679]
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38
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A [AID624223, Type: Literature]HTR2A gene product [Homo sapiens] [gi:260099679]
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39
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A [AID624223, Type: Literature]HTR2A gene product [Homo sapiens] [gi:260099679]
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40
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2C [AID624209, Type: Literature]HTR2C gene product [Homo sapiens] [gi:377520139]
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41
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2C [AID624209, Type: Literature]HTR2C gene product [Homo sapiens] [gi:377520139]
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42
[SID135650533]
 Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2C [AID624209, Type: Literature]HTR2C gene product [Homo sapiens] [gi:377520139]
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43
[SID48416188]
 DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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44
[SID103218455]
 Binding affinity against human UDP Glucuronosyltransferase 1A4 (UGT1A4) [AID214939, Type: Literature]
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45
[SID103218455]
 FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase [AID588216, Type: Literature]
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46
[SID103218455]
 FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase [AID588217, Type: Literature]
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47
[SID85209777]
 Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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48
[SID103218455]
 FDA HLAED, liver enzyme composite activity [AID588214, Type: Literature]
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49
[SID135650533]
 Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT6 [AID624190, Type: Literature]Htr6 gene product [Rattus norvegicus] [gi:13242259]
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50
[SID135650533]
 Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT6 [AID624190, Type: Literature]Htr6 gene product [Rattus norvegicus] [gi:13242259]
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