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Buprenorphine (CID 6321408) - Compound BioActivity Data
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BioActivity Outcomes:
Active(48)
 
 
Inactive(7)
 
 
Inconclusive(18)
 
 
Unspecified(84)
 
 
Top Targets:
7TM GPCR Srx(35)
 
 
 
 
GT1 Gtf like(10)
 
 
 
7TM GPCR Srsx(8)
 
 
 
NAD binding 8(1)
 
 
BioAssay Types:
Literature(156)
 
 
 
 
 
BioActivity Types:
IC50(24)
 
 
 
Ki(23)
 
 
EC50(16)
 
 
 
 
 
Kd(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 157    Data Row: 157   Total Pages: 4   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID104234389]
Ki 6.7e-05Displacement of [3H]-diprenorphine from human KOR expressed in CHO cells [AID735689, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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2
[SID104234389]
EC50 0.00011Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay [AID410728, Type: Literature]Mu-type opioid receptor [gi:2851402]
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3
[SID104234389]
EC50 0.00018Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay [AID410731, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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4
[SID104234389]
Ki 0.00019Displacement of [3H]-diprenorphine from rat recombinant MOR expressed in rat C6 cells after 2 hrs [AID735690, Type: Literature]Mu-type opioid receptor [gi:464314]
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5
[SID104234389]
Ki 0.00021Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells [AID410718, Type: Literature]Mu-type opioid receptor [gi:2851402]
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6
[SID104234389]
EC50 0.00027Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr [AID735224, Type: Literature]Mu-type opioid receptor [gi:464314]
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7
[SID104234389]
Ki 0.0004Displacement of [3H]DAMGO from MOR in Hartley guinea pig membrane [AID735692, Type: Literature]Mu-type opioid receptor [gi:3024265]
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8
[SID104234389]
IC50 0.00041Inhibition of [3H]-Naloxone binding to rat brain membrane without NaCl [AID226060, Type: Literature]
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9
[SID104234389]
IC50 0.00044Inhibition of [3H]naloxone binding to rat brain membrane with 100 mM NaCl. [AID226059, Type: Literature]
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10
[SID104234389]
Ki 0.0005Displacement of [3H]U69593 from KOR in Hartley guinea pig membrane [AID735691, Type: Literature]Kappa-type opioid receptor [gi:730228]
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11
[SID104234389]
IC50 0.00059Activity at human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding [AID410730, Type: Literature]Mu-type opioid receptor [gi:2851402]
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12
[SID104234389]
Ki 0.00062Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells [AID410720, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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13
[SID104234389]
Ki 0.0008Displacement of [3H]U-69593 from human cloned kappa opioid receptor [AID298632, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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14
[SID104234389]
Ki 0.0008Binding affinity to cloned human Opioid receptor kappa 1 transfected into hamster ovary cells using [3H]U-69593 as a radioligand. [AID148008, Type: Literature]
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15
[SID104234389]
Ki 0.0013Binding affinity towards mu opioid receptor in guinea pig brain membranes using [3H]- DAMGO as radioligand [AID224557, Type: Literature]Mu-type opioid receptor [gi:3024265]
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16
[SID104234389]
Ki 0.0013Displacement of [3H]DAMGO from MOR in guinea pig brain membrane [AID707752, Type: Literature]Mu-type opioid receptor [gi:3024265]
View
17
[SID104234389]
Ki 0.0015Displacement of [3H]DAMGO from human cloned mu opioid receptor [AID298631, Type: Literature]Mu-type opioid receptor [gi:2851402]
View
18
[SID104234389]
Ki 0.0015Displacement 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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19
[SID104234389]
Ki 0.0015Displacement of [3H]U69593 from KOR in guinea pig brain membrane [AID707750, Type: Literature]Kappa-type opioid receptor [gi:730228]
View
20
[SID104234389]
Ki 0.0015Binding affinity towards kappa opioid receptor in guinea pig brain membranes using [3H]- U-69,593 as radioligand [AID223576, Type: Literature]Kappa-type opioid receptor [gi:730228]
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21
[SID104234389]
Ki 0.0015Binding affinity to cloned human Opioid receptor mu 1 transfected into hamster ovary cells using [3H]DAMGO as a radioligand. [AID150977, Type: Literature]
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22
[SID104234389]
Ki 0.0016Displacement of [3H]Cl-DPDPE from DOR in guinea pig brain membrane [AID707751, Type: Literature]
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23
[SID104234389]
Ki 0.0016Binding affinity towards delta opioid receptor in guinea pig brain membranes using [3H]- CI-DPDPE as radioligand [AID220389, Type: Literature]
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24
[SID104234389]
IC50 0.002Agonist activity at kappa opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction [AID735226, Type: Literature]Kappa-type opioid receptor [gi:730228]
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25
[SID104234389]
EC50 0.0023Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay [AID224558, Type: Literature]
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26
[SID104234389]
EC50 0.0023GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells [AID148340, Type: Literature]
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27
[SID104234389]
Ki 0.0025Displacement 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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28
[SID104234389]
Ki 0.0029Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells [AID410719, Type: Literature]Delta-type opioid receptor [gi:311033488]
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29
[SID104234389]
Ki 0.0045Displacement of [3H]DPDPE from human cloned delta opioid receptor [AID298633, Type: Literature]Delta-type opioid receptor [gi:311033488]
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30
[SID104234389]
Ki 0.0045Binding affinity to cloned human Opioid receptor delta 1 transfected into hamster ovary cells using [3H]DPDPE as a radioligand. [AID148238, Type: Literature]
View
31
[SID104234389]
Ki 0.0061Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting [AID621888, Type: Literature]Delta-type opioid receptor [gi:311033488]
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32
[SID104234389]
IC50 0.00813Agonistic activity in electrically stimulated guinea pig ileum preparation (GPI) [AID78859, Type: Literature]
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33
[SID104234389]
EC50 0.0102Partial agonist activity at human MOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting [AID621021, Type: Literature]Mu-type opioid receptor [gi:2851402]
View
34
[SID104234389]
EC50 0.0148Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding [AID298634, Type: Literature]Mu-type opioid receptor [gi:2851402]
View
35
[SID104234389]
IC50 0.015Activity at human cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-induced [35S]GTPgammaS binding [AID410733, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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36
[SID104234389]
EC50 0.021Agonist activity at MOR in guinea pig vas deferens [AID707740, Type: Literature]Mu-type opioid receptor [gi:3024265]
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37
[SID104234389]
EC50 0.021Agonist activity at DOR in guinea pig vas deferens [AID707741, Type: Literature]
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38
[SID104234389]
EC50 0.021Agonist activity at KOR in guinea pig vas deferens [AID707739, Type: Literature]Kappa-type opioid receptor [gi:730228]
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39
[SID104234389]
IC50 0.02114Agonist activity was evaluated using mouse vas deferens assay. [AID138338, Type: Literature]
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40
[SID104234389]
Ki 0.0774Displacement 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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41
[SID104234389]
EC50 0.116Partial 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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42
[SID104234389]
IC50 7.58578Inhibitory concentration against potassium channel HERG [AID243151, Type: Literature]
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43
[SID104234389]
Km 24Drug glucuronidation reaction catalyzed by human recombinant UGT2B7 [AID624640, Type: Literature]UDP-glucuronosyltransferase 2B7 [gi:136727]
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44
[SID104234389]
Antagonist activity at MOR in mouse vas deferens assessed as inhibition of DAMGO-induced response [AID735687, Type: Literature]Mu-type opioid receptor [gi:1171911]
View
45
[SID104234389]
Agonist activity at kappa opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction in presence of MOR antagonist CTAP [AID735228, Type: Literature]Kappa-type opioid receptor [gi:730228]
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46
[SID104234389]
Agonist activity at kappa opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction in presence of KOR antagonist norBNI [AID735229, Type: Literature]Kappa-type opioid receptor [gi:730228]
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47
[SID104234389]
Antagonist activity at DOR in mouse vas deferens assessed as inhibition of DPDPE-induced response [AID735230, Type: Literature]Delta-type opioid receptor [gi:417418]
View
48
[SID48415665]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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49
[SID104234389]
EC50 10Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding [AID298635, Type: Literature]Kappa-type opioid receptor [gi:116242691]
View
50
[SID104234389]
EC50 10Partial 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]
View