U 69593 (CID 105104) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(94)
 
 
Inactive(52)
 
 
Inconclusive(31)
 
 
Unspecified(29)
 
 
Top Targets:
7TM GPCR Srx(10)
 
 
 
Tubulin-bindi..(2)
 
 
PMP22 Claudin(2)
 
 
NR LBD TR(2)
 
 
NR LBD ROR li..(2)
 
 
BioAssay Types:
Literature(152)
 
 
 
 
 
Confirmatory(48)
 
 
 
 
Screening(2)
 
 
BioActivity Types:
Potency(46)
 
 
 
 
Ki(27)
 
 
 
IC50(13)
 
 
Kd(9)
 
 
EC50(6)
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 145    Data Row: 206   Total Pages: 5   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103177815]
Ki 0.0003Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. [AID147987, Type: Literature]
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2
[SID103177815]
Ki 0.000475Binding affinity to kappa opioid receptor [AID488649, Type: Literature]
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3
[SID103177815]
Ki 0.00106Tested for inhibitory effect on binding of [3H]bremazocine to opioid receptor kappa in guinea pig cerebellum membranes [AID148101, Type: Literature]
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4
[SID103177815]
Ki 0.00111Binding affinity against opioid receptor kappa 1 from human cloned receptor [AID147998, Type: Literature]
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5
[SID103177815]
Ki 0.00118Binding affinity against opioid receptor by displacing radioligand [3HlU69,593 [AID149067, Type: Literature]
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6
[SID103177815]
Ki 0.0014Binding constant against wild type EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells [AID148576, Type: Literature]
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7
[SID103177815]
Ki 0.00189Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig [AID149135, Type: Literature]
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8
[SID103177815]
IC50 0.002Binding affinity towards Opioid receptor kappa 1 by the displacement of [125I]-(D-Pro10)-Dynorphin A [AID147862, Type: Literature]
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9
[SID103177815]
IC50 0.002Inhibition of [125I]-(D-Pro10)-Dynorphin A binding to human kappa opioid receptor from membranes of HEK293 cells [AID147868, Type: Literature]
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10
[SID103177815]
Ki 0.002Binding affinity towards Mutant D216N, D217N, E218Q Opioid receptor kappa 1 EL-2 expressed in HEK cells [AID141256, Type: Literature]
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11
[SID103177815]
Ki 0.002Binding constant against D216N,D217N,E218Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells [AID55440, Type: Literature]
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12
[SID103177815]
IC50 0.0021Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand [AID148688, Type: Literature]
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13
[SID103177815]
EC50 0.0022Effective concentration required for in vitro agonist potency in guinea-pig ileum myenteric plexus preparation (GPI) [AID73741, Type: other]
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14
[SID103177815]
EC50 0.00225Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux [AID302207, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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15
[SID103177815]
EC50 0.00225Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux [AID302207, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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16
[SID103177815]
EC50 0.00225Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux [AID302207, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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17
[SID103177815]
EC50 0.00225Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux [AID302207, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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18
[SID103177815]
Ki 0.0024Binding constant against E203Q,D204N,D206N EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells [AID65519, Type: Literature]
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19
[SID103177815]
Ki 0.0024Binding affinity towards Mutant E203Q, D204N, D206N, Opioid receptor kappa 1 EL-2 expressed in HEK cells [AID141261, Type: Literature]
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20
[SID103177815]
Ki 0.003Binding affinity towards mutant E203Q,D204N,D206N,E209Q Opioid receptor kappa 1 EL-2 expressed in HEK cells [AID141263, Type: Literature]
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21
[SID103177815]
Ki 0.003Binding constant against E203Q,D204N,D206N,E209Q EL-2 Opioid receptor kappa 1 using [3H]diprenorphine as radioligand expressed in HEK cells [AID65522, Type: Literature]
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22
[SID103177815]
Kd 0.0043Binding affinity at Opioid receptor kappa 1 in guinea pig brain membrane determined by using [3H]U-69593 as radioligand [AID148826, Type: Literature]
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23
[SID103177815]
Ki 0.0048Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes [AID149124, Type: Literature]
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24
[SID103177815]
EC50 0.0066Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay [AID378998, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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25
[SID103177815]
EC50 0.0066Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay [AID378998, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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26
[SID103177815]
EC50 0.0066Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay [AID378998, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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27
[SID103177815]
EC50 0.0066Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay [AID378998, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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28
[SID103177815]
Ki 0.0073Binding affinity for the Opioid receptor kappa 1 [AID149131, Type: Literature]
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29
[SID103177815]
IC50 0.008Displacement of [3H]naloxone from kappa opioid receptor expressed in HEK293 cell membrane [AID480391, Type: Literature]
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30
[SID103177815]
ED50 0.024Effective dose for agonistic activity towards human kappa opioid receptor from membranes of HEK293 cells was determined by radiolabeled [35S]GTP-gamma-S, assay [AID147846, Type: Literature]
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31
[SID103177815]
EC50 0.028Effective concentration required for in vitro evaluation of agonist activity on mouse vas deferens preparation [AID127786, Type: other]
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32
[SID103177815]
Ki 0.052Binding affinity for the Opioid receptor mu 1 [AID147910, Type: Literature]
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33
[SID103177815]
EC50 0.0643Stimulation of [35S]GTP-gamma-S binding at kappa opioid receptor in human brain cortical membrane [AID268069, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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34
[SID103177815]
EC50 0.0643Stimulation of [35S]GTP-gamma-S binding at kappa opioid receptor in human brain cortical membrane [AID268069, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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35
[SID103177815]
EC50 0.0643Stimulation of [35S]GTP-gamma-S binding at kappa opioid receptor in human brain cortical membrane [AID268069, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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36
[SID103177815]
EC50 0.0643Stimulation of [35S]GTP-gamma-S binding at kappa opioid receptor in human brain cortical membrane [AID268069, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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37
[SID103177815]
IC50 0.139Inhibitory concentration was determined against Opioid receptors using [3H]- bremazocine radioligand [AID150239, Type: Literature]
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38
[SID103177815]
IC50 0.14Tested for inhibitory concentration against [3H]bremazocine binding to total sites of opioid receptor in guinea pig brain membrane [AID148620, Type: Literature]
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39
[SID103177815]
IC50 0.248Binding affinity towards Opioid receptor mu 1 by the displacement of [125I]Enkephalin; Not determined [AID148357, Type: Literature]
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40
[SID103177815]
IC50 0.25Inhibition of [125I]Enkephalin binding to human mu opioid receptor from membranes of HEK293 cells [AID150825, Type: Literature]
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41
[SID103177815]
Ki 0.551Tested for inhibitory effect on binding of [3H]DAMGO to opioid receptor mu in guinea pig cerebellum membranes [AID149019, Type: Literature]
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42
[SID103177815]
ED50 0.684Ability to stimulate binding to mu-opioid receptor using GTP-gamma -S-binding assay in guinea pig caudate membranes under unblocked condition [AID152215, Type: Literature]
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43
[SID103177815]
Kd 0.684Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition [AID138706, Type: Literature]
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44
[SID103177815]
Kd 0.684Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition [AID141497, Type: Literature]
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45
[SID103177815]
Ki 1.099Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain [AID268680, Type: Literature]
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46
[SID103177815]
Ki 1.145Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. [AID150841, Type: Literature]
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47
[SID103177815]
Ki 1.358Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain [AID268678, Type: Literature]
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48
[SID103177815]
IC50 1.76Inhibitory concentration was determined against Opioid receptor mu 1 using [3H]- DAMGO radioligand [AID149863, Type: Literature]
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49
[SID103177815]
Ki 1.88Binding affinity of compound was determined against Opioid receptor mu 1 from native receptor in guinea pig [AID147914, Type: Literature]
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50
[SID103177815]
Kd 1.98Binding affinity against Delta opioid receptor in using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes blocked with 20 nM NTI [AID56281, Type: Literature]
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