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ropinirole (CID 5095) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(29)
 
 
Inactive(372)
 
 
Inconclusive(26)
 
 
Unspecified(31)
 
 
Top Targets:
7TM GPCR Srsx(24)
 
 
 
 
p450(13)
 
 
 
NR LBD PPAR(8)
 
 
 
7TM GPCR Srx(7)
 
 
 
 
NR LBD AR(7)
 
 
BioAssay Types:
Confirmatory(278)
 
 
 
 
Literature(117)
 
 
 
 
 
Summary(24)
 
 
Screening(22)
 
 
 
BioActivity Types:
Potency(272)
 
 
 
 
EC50(11)
 
 
Ki(7)
 
 
IC50(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 351    Data Row: 458   Total Pages: 10   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103181541]
EC50 0.004Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation [AID310687, Type: Literature]D(3) dopamine receptor [gi:1169206]
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2
[SID103181541]
Ki 0.0072Binding affinity towards Dopamine receptor D2 by displacement of [3H]U-86170. [AID63977, Type: Literature]D(2) dopamine receptor [gi:118206]
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3
[SID103181541]
EC50 0.0103Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding [AID513742, Type: Literature]D(3) dopamine receptor [gi:1169206]
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4
[SID103181541]
EC50 0.0103Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay [AID461563, Type: Literature]D(3) dopamine receptor [gi:1169206]
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5
[SID103181541]
Ki 0.019Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT. [AID65774, Type: Literature]D(3) dopamine receptor [gi:1169206]
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6
[SID103181541]
EC50 0.0192Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding [AID446402, Type: Literature]D(3) dopamine receptor [gi:1169206]
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7
[SID103181541]
Ki 0.0293Displacement of [3H]spiperone from rat D3 receptor expressed in HEK293 cells [AID513739, Type: Literature]D(3) dopamine receptor [gi:118211]
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8
[SID103181541]
Ki 0.03631Displacement of [3H]spiperone form human cloned dopamine D3 receptor expressed in CHO cells [AID353683, Type: Literature]D(3) dopamine receptor [gi:1169206]
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9
[SID103181541]
EC50 0.083Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation [AID310686, Type: Literature]D(2) dopamine receptor [gi:118206]
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10
[SID103181541]
EC50 0.1Ability to relax the electrically stimulated rabbit ear artery was determined [AID167274, Type: Literature]
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11
[SID103181541]
EC50 0.1Ability to stimulate peripheral prejunctional dopaminergic receptors by 50% inhibition of vasoconstrictor response to field stimulation in isolated perfused rabbit ear artery [AID167710, Type: Literature]
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12
[SID103181541]
EC50 0.1Inhibitory activity against constrictor response to electrical stimulation in the isolated perfused rabbit ear artery(REA) expressing dopamine receptor [AID62577, Type: Literature]
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13
[SID103181541]
EC50 0.304Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding [AID446400, Type: Literature]D(2) dopamine receptor [gi:118206]
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14
[SID103181541]
EC50 0.304Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding [AID513741, Type: Literature]D(2) dopamine receptor [gi:118206]
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15
[SID103181541]
EC50 0.304Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay [AID461562, Type: Literature]D(2) dopamine receptor [gi:118206]
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16
[SID103181541]
Ki 0.69183Displacement of [3H]spiperone form human cloned dopamine D2L receptor expressed in CHO cells [AID353684, Type: Literature]D(2) dopamine receptor [gi:118206]
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17
[SID103181541]
Ki 1.706Binding affinity towards Serotonin 5-hydroxytryptamine 1A receptor by displacement of [3H]-(+)-8-OH-DPAT. [AID4447, Type: Literature]5-hydroxytryptamine receptor 1A [gi:231454]
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18
[SID103181541]
Ki 2.674Displacement of [3H]spiperone from rat D2 receptor expressed in HEK293 cells [AID513738, Type: Literature]D(2) dopamine receptor [gi:47117674]
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19
[SID11111741]
Potency 3.1623qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2D6 [AID891, Type: confirmatory]cytochrome P450 2D6 isoform 1 [Homo sapiens] [gi:40805836]
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20
[SID103181541]
IC50 6.81Displacement of [3H]spiroperidol from homogenized bovine pituitary Dopamine receptor D2 [AID62165, Type: Literature]D(2) dopamine receptor [gi:118205]
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21
[SID11111741]
Potency 17.7828qHTS Assay for Antagonists of Acetylcholine Muscarinic M1 Receptor: Kinetic Measurement of Intracellular Calcium Response [AID943, Type: confirmatory]muscarinic acetylcholine receptor M1 [Rattus norvegicus] [gi:18249941]
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22
[SID103181541]
Reversal of reserpine-induced hypolocomotion in Sprague-Dawley rat Parkinson's disease model at 10 umol/kg, sc measured after 6 hrs administered 18 hrs after reserpine challenge [AID446406, Type: Literature]
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23
[SID103181541]
Induction of rotational activity in 6-OHDA induced unilaterally lesioned Sprague-Dawley rat Parkinson's disease model assessed as duration of action at 10 umol/kg, sc [AID446407, Type: Literature]
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24
[SID103181541]
Induction of rotational activity in 6-OHDA induced unilaterally lesioned Sprague-Dawley rat Parkinson's disease model assessed as duration of action at 5 umol/kg, sc [AID446583, Type: Literature]
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25
[SID85209268]
Ligands of bioamine (Class A) GPCRs [AID2062, Type: other]
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26
[SID103181541]
Effect on behavioral activity in 6-OHDA-induced unilateral lesion Sprague-Dawley rat model assessed as turning behavior at 5 umol/kg, sc measured for 11 hrs [AID461574, Type: Literature]
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27
[SID144203807]
qHTS of D3 Dopamine Receptor Agonist: qHTS [AID652048, Type: screening]D(3) dopamine receptor isoform e [Homo sapiens] [gi:89191863]
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28
[SID144203807]
qHTS of D3 Dopamine Receptor Potentiators: qHTS [AID652051, Type: screening]D(3) dopamine receptor isoform e [Homo sapiens] [gi:89191863]
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29
[SID11111741]
Cytochrome panel assay with activity outcomes [AID1851_2, Type: other]cytochrome P450 2D6 isoform 2 [Homo sapiens] [gi:68509921]
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30
[SID103181541]
Selectivity ratio for Ki for rat D2 receptor to Ki for rat D3 receptor [AID513740, Type: Literature]
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31
[SID103181541]
Selectivity ratio of EC50 for human dopamine D2 receptor to EC50 for human dopamine D3 receptor [AID513743, Type: Literature]
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32
[SID103181541]
Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis [AID539464, Type: Literature]
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33
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia [AID625279, Type: Literature]
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34
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis [AID625280, Type: Literature]
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35
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis [AID625281, Type: Literature]
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36
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis [AID625282, Type: Literature]
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37
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests [AID625283, Type: Literature]
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38
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure [AID625284, Type: Literature]
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39
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis [AID625285, Type: Literature]
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40
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis [AID625286, Type: Literature]
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41
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly [AID625287, Type: Literature]
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42
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice [AID625288, Type: Literature]
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43
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease [AID625289, Type: Literature]
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44
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty [AID625290, Type: Literature]
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45
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal [AID625291, Type: Literature]
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46
[SID103181541]
Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score [AID625292, Type: Literature]
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47
[SID104171231]
qHTS profiling for inhibitors of Plasmodium falciparum proliferation [AID504749, Type: Literature]
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48
[SID103181541]
Selectivity ratio of EC50 for human dopamine D2 receptor to EC50 for human dopamine D3 receptor [AID461566, Type: Literature]
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49
[SID103181541]
Selectivity for human dopamine D3 receptor over human dopamine D2 receptor [AID310688, Type: Literature]
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50
[SID103181541]
Oral bioavailability in human [AID311524, Type: Literature]
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