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Enkephalin, Ala(2)-MePhe(4)-Gly(5)- (CID 5462471) - Compound BioActivity Data
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BioActivity Outcomes:
Active(148)
 
 
Inactive(41)
 
 
Inconclusive(18)
 
 
Unspecified(84)
 
 
Top Targets:
7TM GPCR Srx(123)
 
 
 
 
 
7TM GPCR Srsx(13)
 
 
 
 
 
Bromo ALL-1(2)
 
 
Menin(2)
 
 
NR LBD TR(2)
 
 
BioAssay Types:
Literature(255)
 
 
 
 
 
Confirmatory(25)
 
 
Screening(5)
 
 
BioActivity Types:
Ki(52)
 
 
 
 
EC50(49)
 
 
 
 
IC50(41)
 
 
 
 
 
Potency(25)
 
 
Kd(6)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 285    Data Row: 291   Total Pages: 6   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103217856]
Ki 2.4e-06Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain after 45 mins [AID312059, Type: Literature]Mu-type opioid receptor [gi:464314]
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2
[SID103217856]
Ki 0.00045Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells [AID603170, Type: Literature]
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3
[SID103217856]
Ki 0.0005Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. [AID150841, Type: Literature]
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4
[SID103217856]
Ki 0.00053Compound was evaluated for the binding affinity of Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from rat brain membrane [AID151757, Type: Literature]
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5
[SID103217856]
Ki 0.00053Binding affinity for mu opioid receptor [AID152071, Type: Literature]
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6
[SID103217856]
Ki 0.00066Binding affinity against Opioid receptor mu 1 in P2 membrane preparation of rat brain by [3H]DAGO displacement. [AID151758, Type: Literature]
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7
[SID103217856]
Ki 0.00087Displacement of [3H]DAMGO from Sprague-Dawley rat mu opioid receptor by liquid scintillation counting [AID514359, Type: Literature]Mu-type opioid receptor [gi:464314]
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8
[SID103217856]
Ki 0.0009Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry [AID450016, Type: Literature]
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9
[SID103217856]
Ki 0.00099Binding affinity against mu opioid receptor [AID224571, Type: Literature]Mu-type opioid receptor [gi:3024265]
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10
[SID103217856]
EC50 0.001Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM [AID327872, Type: Literature]Mu-type opioid receptor [gi:2851402]
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11
[SID103217856]
EC50 0.001Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay [AID327873, Type: Literature]Mu-type opioid receptor [gi:2851402]
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12
[SID103217856]
IC50 0.00101Displacement of [3H]DAMGO from mu opioid receptor in rat brain [AID450520, Type: Literature]Mu-type opioid receptor [gi:464314]
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13
[SID103217856]
IC50 0.0011Potency for inhibition of forskolin-stimulated cyclic AMP accumulation in SH-SY5Y cells [AID201472, Type: Literature]
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14
[SID103217856]
IC50 0.0011Displacement of radiolabeled DAMGO from human mu-type opioid receptor agonist site [AID346442, Type: Literature]Mu-type opioid receptor [gi:2851402]
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15
[SID103217856]
Ki 0.0011Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain [AID268677, Type: Literature]Mu-type opioid receptor [gi:3024265]
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16
[SID103217856]
IC50 0.00113Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane [AID295476, Type: Literature]Mu-type opioid receptor [gi:464314]
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17
[SID103217856]
Ki 0.0012Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting [AID647794, Type: Literature]Mu-type opioid receptor [gi:2851402]
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18
[SID103217856]
IC50 0.00145Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells [AID452776, Type: Literature]Delta-type opioid receptor [gi:311033488]
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19
[SID103217856]
Ki 0.0015Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 2 hrs by liquid scintillation counting [AID707254, Type: Literature]Mu-type opioid receptor [gi:2851402]
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20
[SID103217856]
Ki 0.00155Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells [AID603171, Type: Literature]
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21
[SID103217856]
Ki 0.00159Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting [AID621887, Type: Literature]Mu-type opioid receptor [gi:2851402]
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22
[SID103217856]
Ki 0.0016Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes [AID239174, Type: Literature]
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23
[SID103217856]
IC50 0.0016Binding activity against human Opioid receptor mu 1 using [3H]DAMGO as a radioligand [AID148354, Type: Literature]
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24
[SID103217856]
Ki 0.0016Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes. [AID151468, Type: Literature]
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25
[SID103217856]
Ki 0.00164Binding affinity towards Opioid receptor mu 1 [AID151616, Type: Literature]
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26
[SID103217856]
EC50 0.0017Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding [AID365600, Type: Literature]Mu-type opioid receptor [gi:2851402]
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27
[SID103217856]
IC50 0.002Displacement of [3H]naloxone from mu opioid receptor expressed in CHO cell membrane [AID480390, Type: Literature]
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28
[SID103217856]
IC50 0.0022Displacement of [3H]U69593 from delta opioid receptor in guinea pig cerebellum membrane [AID334454, Type: Literature]
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29
[SID103217856]
IC50 0.0025Inhibition of human mu opioid receptor [AID340259, Type: Literature]Mu-type opioid receptor [gi:2851402]
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30
[SID103217856]
EC50 0.00266Activity at CCK2R-MOPR coexpressed in CHO cells co-transfected with delta-6-Galphaqi4-myr assessed as intracellular calcium release by FLIPR [AID411826, Type: Literature]
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31
[SID103217856]
IC50 0.003Binding affinity against rat mu-opioid receptor expressed in CHO cells by competitive inhibition of 1 nM [3H]DAMGO [AID141775, Type: Literature]Mu-type opioid receptor [gi:464314]
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32
[SID103217856]
EC50 0.00304Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter [AID698512, Type: Literature]
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33
[SID103217856]
EC50 0.00304Agonist activity at FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis [AID730862, Type: Literature]Mu-type opioid receptor [gi:2851402]
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34
[SID103217856]
EC50 0.00318Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting [AID690645, Type: Literature]Mu-type opioid receptor [gi:2851402]
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35
[SID103217856]
IC50 0.00318Agonist activity at mu opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation [AID514364, Type: Literature]
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36
[SID103217856]
Ki 0.00334Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells [AID603169, Type: Literature]
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37
[SID103217856]
IC50 0.0035The compound was tested for binding affinity towards rat Opioid receptor mu 1 by displacing [3H]DAMGO. [AID151457, Type: Literature]
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38
[SID103217856]
Ki 0.0038Binding affinity to mu opioid receptor [AID437485, Type: Literature]
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39
[SID103217856]
Ki 0.0039Inhibition of [3H]DAGO binding to mu 1 opioid receptor in rat brain membranes [AID151592, Type: Literature]
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40
[SID103217856]
Ki 0.0039Binding affinity to opioid receptor mu was determined in rat brain using [3H]DAGO as radioligand [AID149294, Type: Literature]
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41
[SID103217856]
Ki 0.004Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library [AID141655, Type: Literature]
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42
[SID103217856]
Ki 0.0061Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane [AID151601, Type: Literature]
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43
[SID103217856]
Ki 0.0067Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells [AID411820, Type: Literature]
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44
[SID103217856]
EC50 0.00686Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting [AID621022, Type: Literature]Delta-type opioid receptor [gi:311033488]
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45
[SID103217856]
EC50 0.0082Activity at mu opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding [AID450021, Type: Literature]
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46
[SID103217856]
IC50 0.00825Agonistic activity in electrically stimulated guinea pig ileum preparation (GPI) [AID78859, Type: Literature]
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47
[SID103217856]
IC50 0.00825Opioid agonistic activity against Guinea pig ileum [AID79042, Type: Literature]
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48
[SID103217856]
IC50 0.00989Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes [AID151432, Type: Literature]
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49
[SID103217856]
IC50 0.0099Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes [AID151447, Type: Literature]
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50
[SID103217856]
IC50 0.0099Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes [AID242329, Type: Literature]
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