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Orphenadrine (CID 4601) - Compound BioActivity Data
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BioActivity Outcomes:
Active(29)
 
 
Inactive(100)
 
 
Inconclusive(12)
 
 
Unspecified(153)
 
 
Top Targets:
7TM GPCR Srx(22)
 
 
 
 
7TM GPCR Srsx(16)
 
 
 
 
p450(15)
 
 
 
 
Pyr redox dim(6)
 
 
B zip1(4)
 
 
BioAssay Types:
Confirmatory(92)
 
 
 
 
Literature(59)
 
 
 
 
 
Screening(9)
 
 
BioActivity Types:
IC50(126)
 
 
 
 
Potency(91)
 
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 280    Data Row: 294   Total Pages: 6   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: other]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: other]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: other]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: other]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: other]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: other]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: other]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: other]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: other]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: other]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: other]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: other]
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15
[SID103235190]
IC50 1.895DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) [AID625202, Type: other]Alpha-2B adrenergic receptor [gi:27151763]
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16
[SID103235190]
IC50 2.156DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) [AID625201, Type: other]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: other]
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18
[SID103235190]
IC50 2.492DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin) [AID625225, Type: other]
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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: other]Sodium-dependent noradrenaline transporter [gi:128616]
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21
[SID103235190]
IC50 3.391DRUGMATRIX: 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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22
[SID103235190]
IC50 4.3Inhibition of human OCT2 A270S mutant expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692193, Type: Literature]
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23
[SID103235190]
Ki 6The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex. [AID156805, Type: Literature]
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24
[SID103235190]
IC50 6.961DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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25
[SID103235190]
IC50 12.6Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy [AID386625, Type: Literature]Solute carrier family 22 member 1 [gi:313104181]
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26
[SID48416355]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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27
[SID85209919]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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28
[SID103235190]
Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis [AID678721, Type: Literature]
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29
[SID103235190]
Cmax in human [AID692185, Type: Literature]
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30
[SID103235190]
IC50 65Inhibition of human MATE1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692195, Type: Literature]Multidrug and toxin extrusion protein 1 [gi:74731723]
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31
[SID103235190]
IC50 97.7237Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay [AID697786, Type: Literature]Histamine H1 receptor [gi:547645]
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32
[SID103235190]
IC50 100Inhibition of human MATE2-K expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692196, Type: Literature]Multidrug and toxin extrusion protein 2 [gi:74727585]
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33
[SID103235190]
IC50 100Inhibition of human OCT1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay [AID692194, Type: Literature]Solute carrier family 22 member 1 [gi:313104181]
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34
[SID103235190]
IC50 DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP) [AID625167, Type: other]cGMP-specific 3',5'-cyclic phosphodiesterase [gi:317373261]
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35
[SID103235190]
IC50 DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) [AID625243, Type: other]Prostaglandin G/H synthase 1 [gi:317373262]
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36
[SID103235190]
DRUGMATRIX: Protein Serine/Threonine Kinase PKCalpha enzyme inhibition (substrate: Histone) [AID625179, Type: other]Protein kinase C alpha type [gi:317373571]
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37
[SID103235190]
IC50 DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) [AID625147, Type: other]Melanocortin receptor 3 [gi:395398606]
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38
[SID103235190]
DRUGMATRIX: Calcitonin radioligand binding (ligand: [125I] Calcitonin (salmon)) [AID625214, Type: other]Calcitonin receptor [gi:550544247]
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39
[SID103235190]
DRUGMATRIX: Chemokine CXCR1 (IL-8A) [AID625240, Type: other]C-X-C chemokine receptor type 1 [gi:108936015]
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40
[SID103235190]
IC50 DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625162, Type: other]Kappa-type opioid receptor [gi:116242691]
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41
[SID103235190]
IC50 DRUGMATRIX: Vascular Endothelinal Growth Factor (VEGF) radioligand binding (ligand: [125I] VEGF) [AID625231, Type: other]Vascular endothelial growth factor receptor 1 [gi:143811474]
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42
[SID103235190]
IC50 DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) [AID625251, Type: other]Cytochrome P450 3A4 [gi:116241312]
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43
[SID103235190]
IC50 DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) [AID625227, Type: other]Substance-K receptor [gi:229462950]
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44
[SID103235190]
IC50 DRUGMATRIX: Leukotriene LTC4 Synthase enzyme inhibition (substrate: LTA4) [AID625144, Type: other]Leukotriene C4 synthase [gi:239977155]
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45
[SID103235190]
IC50 DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) [AID625229, Type: other]Thromboxane-A synthase [gi:254763392]
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46
[SID103235190]
IC50 DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) [AID625178, Type: other]Matrix metalloproteinase-9 [gi:269849668]
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47
[SID103235190]
IC50 DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) [AID625205, Type: other]Beta-2 adrenergic receptor [gi:296439450]
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48
[SID103235190]
DRUGMATRIX: CYP450, 2A6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625246, Type: other]Cytochrome P450 2A6 [gi:308153612]
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49
[SID103235190]
IC50 DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) [AID625161, Type: other]Delta-type opioid receptor [gi:311033488]
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50
[SID103235190]
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy [AID386623, Type: Literature]Solute carrier family 22 member 1 [gi:313104181]
View