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Nalbuphine (CID 5311304) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(27)
 
 
Inactive(80)
 
 
Inconclusive(16)
 
 
Unspecified(180)
 
 
Top Targets:
7TM GPCR Srx(49)
 
 
 
 
 
7TM GPCR Srsx(17)
 
 
 
p450(16)
 
 
 
 
 
NR LBD ER(9)
 
 
 
 
NR LBD AR(8)
 
 
 
 
BioAssay Types:
Literature(79)
 
 
 
 
 
Confirmatory(51)
 
 
 
Screening(20)
 
 
Summary(15)
 
 
 
BioActivity Types:
IC50(124)
 
 
 
 
Potency(62)
 
 
 
Ki(8)
 
 
 
EC50(6)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 301    Data Row: 303   Total Pages: 7   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103234668]
Ki 0.00089Displacement of [3H]DAMGO from human opioid gamma receptor expressed in CHO cells [AID286302, Type: Literature]Mu-type opioid receptor [gi:2851402]
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2
[SID103234668]
IC50 0.001Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand [AID152239, Type: Literature]
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3
[SID103234668]
Ki 0.0016Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting [AID416813, Type: Literature]Mu-type opioid receptor [gi:2851402]
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4
[SID103234668]
Ki 0.0022Displacement of [3H]U-69593 from human opioid kappa receptor expressed in CHO cells [AID286303, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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5
[SID103234668]
Ki 0.003Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting [AID416815, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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6
[SID103234668]
EC50 0.014Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding [AID286312, Type: Literature]Mu-type opioid receptor [gi:2851402]
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7
[SID103234668]
IC50 0.024DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625163, Type: other]Mu-type opioid receptor [gi:2851402]
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8
[SID103234668]
EC50 0.027Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding [AID286308, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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9
[SID103234668]
EC50 0.046Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding [AID417156, Type: Literature]Mu-type opioid receptor [gi:2851402]
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10
[SID103234668]
EC50 0.056Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding [AID417160, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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11
[SID103234668]
EC50 0.065Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting [AID640424, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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12
[SID103234668]
IC50 0.083Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand [AID147859, Type: Literature]
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13
[SID103234668]
IC50 0.096Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding [AID417162, Type: Literature]Mu-type opioid receptor [gi:2851402]
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14
[SID103234668]
IC50 0.11Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as inhibition of DAGO-stimulated [35S]GTPgammaS binding [AID286314, Type: Literature]Mu-type opioid receptor [gi:2851402]
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15
[SID103234668]
IC50 0.111DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625162, Type: other]Kappa-type opioid receptor [gi:116242691]
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16
[SID103234668]
Ki 0.24Displacement of [3H]naltrindole from human opioid delta receptor expressed in CHO cells [AID286304, Type: Literature]Delta-type opioid receptor [gi:311033488]
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17
[SID103234668]
EC50 0.25Agonist activity at human KOPR expressed in U2OS cells assessed as beta-arrestin2 recruitment after 90 mins by DiscoveRx PathHunter assay [AID640395, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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18
[SID103234668]
IC50 0.353Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand [AID148078, Type: Literature]
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19
[SID103234668]
Ki 0.58Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting [AID416814, Type: Literature]Delta-type opioid receptor [gi:311033488]
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20
[SID103234668]
IC50 1.886DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) [AID625161, Type: other]Delta-type opioid receptor [gi:311033488]
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21
[SID48416304]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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22
[SID103234668]
Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis [AID678721, Type: Literature]
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23
[SID103234668]
Partial agonist activity at KOPR expressed in human U2OS cells co-expressing GFP-tagged beta-arrestin2 assessed as translocation of GFP-tagged beta-arrestin2 at 10 uM incubated 120 mins in serum deprived medium prior drug addition measured after 10 mins by confocal microscopy [AID640431, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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24
[SID103234668]
Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins [AID678716, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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25
[SID103234668]
Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins [AID678717, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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26
[SID103234668]
Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins [AID678715, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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27
[SID103234668]
Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins [AID678712, Type: Literature]Cytochrome P450 1A2 [gi:117144]
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28
[SID103234668]
IC50 DRUGMATRIX: CYP450, 2E1 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625250, Type: other]Cytochrome P450 2E1 [gi:117250]
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29
[SID103234668]
IC50 DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) [AID625253, Type: other]D(2) dopamine receptor [gi:118206]
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30
[SID103234668]
IC50 DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) [AID625252, Type: other]D(1A) dopamine receptor [gi:118228]
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31
[SID103234668]
DRUGMATRIX: Peptidase, ELA2 (Neutrophil Elastase 2) enzyme inhibition (substrate: N-MeOSuc-Ala-Ala-Pro-Val-pNA) [AID625176, Type: other]Neutrophil elastase [gi:119292]
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32
[SID103234668]
IC50 DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625186, Type: other]Receptor tyrosine-protein kinase erbB-2 [gi:119533]
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33
[SID103234668]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein) [AID625181, Type: other]Mitogen-activated protein kinase 1 [gi:119554]
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34
[SID103234668]
IC50 DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1) [AID625257, Type: other]Endothelin-1 receptor [gi:119606]
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35
[SID103234668]
IC50 DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) [AID625263, Type: other]Glucocorticoid receptor [gi:121069]
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36
[SID103234668]
IC50 DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) [AID625270, Type: other]Histamine H2 receptor [gi:123120]
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37
[SID103234668]
IC50 DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) [AID625271, Type: other]3-hydroxy-3-methylglutaryl-coenzyme A reductase [gi:123343]
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38
[SID103234668]
IC50 DRUGMATRIX: Insulin radioligand binding (ligand: [125I] Insulin) [AID625273, Type: other]Insulin receptor [gi:124531]
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39
[SID103234668]
IC50 DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625185, Type: other]Tyrosine-protein kinase Fyn [gi:125370]
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40
[SID103234668]
IC50 DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625187, Type: other]Tyrosine-protein kinase Lck [gi:125474]
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41
[SID103234668]
IC50 DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) [AID625146, Type: other]Arachidonate 15-lipoxygenase [gi:126397]
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42
[SID103234668]
IC50 DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P) [AID625226, Type: other]Substance-P receptor [gi:128359]
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43
[SID103234668]
IC50 DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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44
[SID103234668]
DRUGMATRIX: Neuropeptide Y Y1 radioligand binding (ligand: [125I] Peptide YY) [AID625156, Type: other]Neuropeptide Y receptor type 1 [gi:128997]
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45
[SID103234668]
IC50 DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF) [AID625168, Type: other]Platelet-activating factor receptor [gi:129557]
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46
[SID103234668]
Specific activity of expressed human recombinant UGT2B7H [AID624620, Type: Literature]UDP-glucuronosyltransferase 2B7 [gi:136727]
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47
[SID103234668]
Specific activity of expressed human recombinant UGT2B7Y [AID624621, Type: Literature]UDP-glucuronosyltransferase 2B7 [gi:136727]
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48
[SID103234668]
IC50 DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) [AID625194, Type: other]Adenosine receptor A1 [gi:231473]
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49
[SID103234668]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein) [AID625180, Type: other]Mitogen-activated protein kinase 3 [gi:232066]
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50
[SID103234668]
IC50 DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC) [AID625174, Type: other]Caspase-1 [gi:266321]
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