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Orphenadrine (CID 4601) - Compound BioActivity Data
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BioActivity Outcomes:
Active(29)
 
 
Inactive(101)
 
 
Inconclusive(12)
 
 
Unspecified(154)
 
 
Top Targets:
7tm 4(37)
 
 
 
 
p450(15)
 
 
 
 
Pyr redox dim(6)
 
 
Tryp SPc(4)
 
 
 
bZIP NFE2-lik..(4)
 
 
BioAssay Types:
Confirmatory(209)
 
 
 
 
 
Literature(59)
 
 
 
 
 
Screening(9)
 
 
BioActivity Types:
IC50(126)
 
 
 
 
Potency(92)
 
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 282    Data Row: 296   Total Pages: 15   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103235190]
IC50 0.028DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625155, Type: confirmatory]Muscarinic acetylcholine receptor M5 [gi:543761]
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2
[SID103235190]
IC50 0.125DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625154, Type: confirmatory]Muscarinic acetylcholine receptor M4 [gi:23503039]
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3
[SID103235190]
IC50 0.148DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625151, Type: confirmatory]Muscarinic acetylcholine receptor M1 [gi:113118]
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4
[SID103235190]
IC50 0.16218Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting [AID697787, Type: Literature]Histamine H1 receptor [gi:399890]
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5
[SID103235190]
IC50 0.175DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625153, Type: confirmatory]Muscarinic acetylcholine receptor M3 [gi:113125]
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6
[SID103235190]
IC50 0.376DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625152, Type: confirmatory]Muscarinic acetylcholine receptor M2 [gi:113122]
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7
[SID103235190]
IC50 0.4DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625249, Type: confirmatory]Cytochrome P450 2D6 [gi:84028191]
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8
[SID103235190]
IC50 0.436DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) [AID625192, Type: confirmatory]5-hydroxytryptamine receptor 2A [gi:543727]
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9
[SID103235190]
IC50 0.458DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: confirmatory]Sodium-dependent serotonin transporter [gi:400630]
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10
[SID103235190]
IC50 0.534DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) [AID625218, Type: confirmatory]5-hydroxytryptamine receptor 2C [gi:112816]
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11
[SID103235190]
IC50 0.85114Inhibition of human ERG [AID576612, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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12
[SID103235190]
IC50 1.121DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) [AID625221, Type: confirmatory]5-hydroxytryptamine receptor 6 [gi:1703010]
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13
[SID103235190]
IC50 1.241DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) [AID625269, Type: confirmatory]Histamine H1 receptor [gi:547645]
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14
[SID103235190]
IC50 1.746DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888)) [AID625234, Type: confirmatory]
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15
[SID103235190]
IC50 1.895DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) [AID625202, Type: confirmatory]Alpha-2B adrenergic receptor [gi:613504690]
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16
[SID103235190]
IC50 2.156DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) [AID625201, Type: confirmatory]Alpha-2A adrenergic receptor [gi:1351829]
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17
[SID103235190]
IC50 2.232DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem) [AID625215, Type: confirmatory]
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18
[SID103235190]
IC50 2.492DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin) [AID625225, Type: confirmatory]
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19
[SID103235190]
IC50 2.5Inhibition of human OCT2 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692192, Type: Literature]Solute carrier family 22 member 2 [gi:313104182]
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20
[SID103235190]
IC50 2.666DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: confirmatory]Sodium-dependent noradrenaline transporter [gi:128616]
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