1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (CID 1388) - BioAssay Data Summary for Compound
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BioActivity Outcomes:
Active(3)
 
 
Inactive(1)
 
 
Unspecified(95)
 
 
Top Targets:
NAD binding 8(22)
 
 
 
NOS oxygenase..(4)
 
 
MFS(3)
 
 
SLC6sbd DAT1(2)
 
 
BioAssay Types:
Literature(90)
 
 
 
BioActivity Types:
IC50(4)
 
 
Ki(4)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 99    Data Row: 99   Total Pages: 2   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103192001]
Km 0.39Kinetic parameter KM (nM) for the MAO-B catalyzed oxidation of the compound. [AID17444, Type: Literature]
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2
[SID103192001]
 Inhibition of human recombinant MAOA expressed in insect cells assessed as oxidation of kynuramine substrate at 50 uM measured after additional enzyme added after 120 mins incubation [AID641928, Type: Literature]Amine oxidase [flavin-containing] A [gi:113978]
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3
[SID103192001]
 Inhibition of human recombinant MAOA expressed in insect cells assessed as oxidation of kynuramine substrate at 50 uM measured after additional substrate added after 90 mins incubation [AID641842, Type: Literature]Amine oxidase [flavin-containing] A [gi:113978]
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4
[SID103192001]
Km 81.8Activity at baboon liver mitochondrial MAO-B assessed as initial rate of H2O2 production after 12.5 mins [AID488092, Type: Literature]
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5
[SID103192001]
Km 90separate experiments , n=5) [AID27333, Type: Literature]
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6
[SID103192001]
Ki 100Binding affinity against monoamine oxidase-B (MAO-B) [AID126505, Type: Literature]
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7
[SID103192001]
Km 134Kinetic constant (Km) determined in rat brain mitochondria [AID195852, Type: Literature]
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8
[SID103192001]
Km 140Oxidation by human mono-amine oxidase MAO-A [AID102736, Type: Literature]Amine oxidase [flavin-containing] A [gi:113978]
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9
[SID103192001]
Km 140Michaelis Menten constant against MAO A. [AID102566, Type: Literature]
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10
[SID103192001]
Km 191Michalis Menton constant for Monoamine oxidase B catalyzed oxidation (KM). [AID126380, Type: Literature]Amine oxidase [flavin-containing] B [gi:124028638]
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11
[SID103192001]
Km 200Km against bovine liver Monoamine oxidase B [AID126515, Type: Literature]Amine oxidase [flavin-containing] B [gi:124028638]
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12
[SID103192001]
Ki 280Inhibition of human liver monoamine oxidase was determined [AID127329, Type: Literature]
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13
[SID103192001]
Km 390Michaelis-Menten constant was measured against monoamine oxidase B (MAO-B) from beef liver [AID126381, Type: Literature]
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14
[SID103192001]
Km 390Tested against Monoamine oxidase B enzyme from bovine liver mitochondria [AID126383, Type: Literature]
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15
[SID103192001]
Km 390Michaelis Menten constant against MAO B. [AID102575, Type: Literature]Amine oxidase [flavin-containing] B [gi:124028638]
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16
[SID103192001]
Km 390Oxidation by bovine mono-amine oxidase B MAO-B [AID102891, Type: Literature]Amine oxidase [flavin-containing] B [gi:124028638]
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17
[SID103192001]
Ki 500Inactivation of monoamine oxidase measured as kinetic constant, KI at 1-5 conc range [AID127323, Type: Literature]
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18
[SID103192001]
Km 654Michaelis Menton constant for Monoamine oxidase A catalyzed oxidation (Km) [AID125559, Type: Literature]Amine oxidase [flavin-containing] A [gi:113978]
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19
[SID103192001]
IC50 3000Inhibitory activity against human liver Dihydrodipicolinate reductase (DHPR) [AID56917, Type: Literature]
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20
[SID103192001]
IC50 4600Inhibitory activity against rat striatal synaptosomes Dihydrodipicolinate reductase (DHPR) [AID56920, Type: Literature]
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21
[SID103192001]
Ki 5000Inhibitory constant against monoamine Oxidase(MAO-B). [AID126378, Type: Literature]
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22
[SID103192001]
IC50 7200Inhibitory activity against human liver Dihydropteridine reductase enzyme using 10 uM qBH2 and 50 uM NADH assays [AID56918, Type: Literature]
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23
[SID103192001]
IC50 8400Inhibitory activity against rat striatal synaptosomes Dihydrodipicolinate reductase using 10 uM qBH2 and 50 uM NADH assays [AID56921, Type: Literature]
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24
[SID103192001]
 Partition coefficient (logP) [AID19439, Type: Literature]
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25
[SID103192001]
 Maximal rate (Vmax) for oxidation by rat liver MAO (results are means of number of separate experiments , n=5) [AID30129, Type: Literature]
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26
[SID103192001]
 Kinetic parameter Vmax (nm/min/unit of MAO-B) for the MAO-B catalyzed oxidation of the compound. [AID22611, Type: Literature]
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27
[SID103192001]
 Kinetic parameter Vmax/K (Litres/min/unit of MAO-B) for the MAO-B catalyzed oxidation of the compound. [AID22832, Type: Literature]
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28
[SID103192001]
 Cytotoxicity measured as % loss of cells after 120 min [AID86880, Type: Literature]
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29
[SID103192001]
 Turnover number against MAO A (umol of substrate/min per umol of enzyme). [AID102567, Type: Literature]
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30
[SID103192001]
 Compound was tested for inhibition of monoclonal antibody complex (MAO B - MAO B 1C2) from human autopsy liver expressed as specific activity [AID102732, Type: Literature]
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31
[SID103192001]
 Compound was tested for inactivation of monoclonal antibody complex (MAO B - MAO B 1C2) from human autopsy liver [AID102733, Type: Literature]
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32
[SID103192001]
 Ratio of Kinetic constants (Km vs. Vmax). [AID125530, Type: Literature]
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33
[SID103192001]
 Kinetic constant (Vmax) determined in rat brain mitochondria. [AID125532, Type: Literature]
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34
[SID103192001]
 Percent inhibition of MAO-catalyzed oxidation in rat brain mitochondria induced by pargyline [AID125534, Type: Literature]
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35
[SID103192001]
 Tested for Km, the substrate concentration with gives half maximum velocity of the monoamine oxidase A catalyzed oxidation. [AID125574, Type: Literature]
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36
[SID103192001]
 Tested for maximum velocity of monoamine oxidase A catalyzed oxidation [AID125693, Type: Literature]
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37
[SID103192001]
 Kinetic value evaluated as catalyzed oxidation (kcat). [AID125695, Type: Literature]
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38
[SID103192001]
 MAO-B Inactivation property expressed as inactivation constant (K inact). [AID126371, Type: Literature]
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39
[SID103192001]
 Cytotoxicity measured as % loss of cells after 60 min [AID86881, Type: Literature]
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40
[SID103192001]
 Cytotoxicity measured as % loss of cells after 90 min [AID86882, Type: Literature]
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41
[SID103192001]
 Catalytic constant was measured against monoamine oxidase B (MAO-B) from beef liver [AID126384, Type: Literature]
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42
[SID103192001]
 Inactivation of monoamine oxidase measured as kinetic constant, Kinact at 1-5 conc range [AID127335, Type: Literature]
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43
[SID103192001]
 Binding affinity towards monoaminooxidase Relative to MPTP [AID127348, Type: Literature]
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44
[SID103192001]
 Compound is tested for the concentration of DOPAC (dihydroxyphenyl-acetic acid) in striatum of mouse brain one week after four daily injections at dose of 20 mg/kg [AID127912, Type: Literature]
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45
[SID103192001]
 Compound is tested for the concentration of HVA in striatum of mouse brain one week after four daily injections at dose of 20 mg/kg [AID127913, Type: Literature]
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46
[SID103192001]
 Compound is tested for the concentration of HVA in striatum of mouse brain one week after four daily injections at doses of 20 mg/kg [AID127914, Type: Literature]
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47
[SID103192001]
 Compound is tested for the concentration of dopamine in striatum of mouse brain one week after four daily injections at 20 mg/kg dose [AID127915, Type: Literature]
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48
[SID103192001]
 Tested for pargyline-induced inhibition of MAO-catalyzed oxidation in rat brain mitochondria (Specific inhibitor = Pargyline hydrochloride at 2.5 uM) (Control = 16.58) [AID195851, Type: Literature]
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49
[SID103192001]
 Turnover number (TN) for human mono-amine oxidase MAO-A [AID102737, Type: Literature]Amine oxidase [flavin-containing] A [gi:113978]
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50
[SID103192001]
 Activity of human liver MAOB assessed as specific activity at 1 mM [AID401023, Type: other]Amine oxidase [flavin-containing] B [gi:113980]
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