CHEMBL389521 (CID 44430582) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(45)
 
 
Inactive(2)
 
 
Inconclusive(20)
 
 
Unspecified(64)
 
 
Top Targets:
7TM GPCR Srx(15)
 
 
 
 
BioAssay Types:
Literature(131)
 
 
 
 
 
BioActivity Types:
Ki(21)
 
 
 
EC50(18)
 
 
 
 
Kd(10)
 
 
 
IC50(9)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 131    Data Row: 131   Total Pages: 3   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103532570]
Ki 6e-05Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells [AID147411, Type: Literature]
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2
[SID103532570]
EC50 8e-05Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes ; Nd: no data [AID147763, Type: Literature]
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3
[SID103532570]
Ki 8e-05Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting [AID621019, Type: Literature]Nociceptin receptor [gi:730230]
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4
[SID103532570]
Kd 8.8e-05Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay [AID453424, Type: Literature]
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5
[SID103532570]
EC50 9e-05Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1 [AID246515, Type: Literature]Nociceptin receptor [gi:730230]
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6
[SID103532570]
Kd 9.2e-05Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay [AID453607, Type: Literature]
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7
[SID103532570]
Ki 0.0001Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells [AID148869, Type: Literature]
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8
[SID103532570]
Kd 0.0001Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1 [AID148877, Type: Literature]
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9
[SID103532570]
Ki 0.00013Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells [AID315424, Type: Literature]Nociceptin receptor [gi:730230]
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10
[SID103532570]
Ki 0.00018Inhibition of [3H]nociceptin binding to human Opioid receptor like 1 [AID239061, Type: Literature]Nociceptin receptor [gi:730230]
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11
[SID103532570]
IC50 0.00021Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay [AID453420, Type: Literature]
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12
[SID103532570]
IC50 0.00022Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay [AID453419, Type: Literature]
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13
[SID103532570]
IC50 0.00022Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay [AID453416, Type: Literature]
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14
[SID103532570]
Ki 0.0003Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells [AID148870, Type: Literature]Nociceptin receptor [gi:730230]
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15
[SID103532570]
Ki 0.00039Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells [AID367833, Type: Literature]Nociceptin receptor [gi:730230]
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16
[SID103532570]
EC50 0.00045Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells [AID148859, Type: Literature]Nociceptin receptor [gi:730230]
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17
[SID103532570]
Kd 0.00049Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay [AID453421, Type: Literature]
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18
[SID103532570]
IC50 0.00054Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay [AID453418, Type: Literature]
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19
[SID103532570]
IC50 0.0006Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells [AID316812, Type: Literature]Nociceptin receptor [gi:730230]
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20
[SID103532570]
Kd 0.00067Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay [AID453423, Type: Literature]
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21
[SID103532570]
Kd 0.00071Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay [AID453422, Type: Literature]
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22
[SID103532570]
IC50 0.00073Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells [AID389114, Type: Literature]Nociceptin receptor [gi:548427]
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23
[SID103532570]
IC50 0.00091Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay [AID453417, Type: Literature]
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24
[SID103532570]
EC50 0.0011Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding [AID453408, Type: Literature]
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25
[SID103532570]
EC50 0.0011Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding [AID453410, Type: Literature]
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26
[SID103532570]
EC50 0.0012Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding [AID453411, Type: Literature]
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27
[SID103532570]
EC50 0.0015Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding [AID368094, Type: Literature]Nociceptin receptor [gi:730230]
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28
[SID103532570]
IC50 0.0017Displacement of radiolabeled nociceptin from human ORL1 receptor [AID346443, Type: Literature]Nociceptin receptor [gi:730230]
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29
[SID103532570]
IC50 0.0021Inhibition of human ORL1 receptor [AID340260, Type: Literature]Nociceptin receptor [gi:730230]
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30
[SID103532570]
EC50 0.00391Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding [AID316813, Type: Literature]Nociceptin receptor [gi:730230]
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31
[SID103532570]
EC50 0.0056Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding [AID453409, Type: Literature]
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32
[SID103532570]
EC50 0.0081Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting [AID621024, Type: Literature]Nociceptin receptor [gi:730230]
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33
[SID103532570]
EC50 0.013Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay [AID389115, Type: Literature]Nociceptin receptor [gi:548427]
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34
[SID103532570]
ED50 0.0193Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction [AID316817, Type: Literature]Nociceptin receptor [gi:548426]
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35
[SID103532570]
EC50 0.024Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1 [AID148861, Type: Literature]
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36
[SID103532570]
EC50 0.063Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay [AID148860, Type: Literature]
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37
[SID103532570]
EC50 0.0785Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting [AID621023, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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38
[SID103532570]
EC50 0.0785Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting [AID621023, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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39
[SID103532570]
EC50 0.0785Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting [AID621023, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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40
[SID103532570]
EC50 0.0785Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting [AID621023, Type: Literature]Kappa-type opioid receptor [gi:116242691]
View
41
[SID103532570]
Ki 0.147Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting [AID621889, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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42
[SID103532570]
Ki 0.147Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting [AID621889, Type: Literature]Kappa-type opioid receptor [gi:116242691]
View
43
[SID103532570]
Ki 0.147Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting [AID621889, Type: Literature]Kappa-type opioid receptor [gi:116242691]
View
44
[SID103532570]
Ki 0.147Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting [AID621889, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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45
[SID103532570]
Ki 0.27Binding affinity for opioid receptor type, human Opioid receptor mu 1 expressed in membrane homogenates of COS-1 or CHO cells [AID150974, Type: Literature]
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46
[SID103532570]
Ki 0.437Displacement 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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47
[SID103532570]
Ki 0.437Displacement 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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48
[SID103532570]
Ki 0.437Displacement 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]
View
49
[SID103532570]
Ki 0.437Displacement 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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50
[SID103532570]
Ki 1.5Binding affinity for opioid receptor type, human Opioid receptor kappa 1 expressed in membrane homogenates of COS-1 or CHO cells [AID148004, Type: Literature]
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