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zaleplon (CID 5719) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(11)
 
 
Inactive(375)
 
 
Inconclusive(23)
 
 
Unspecified(174)
 
 
Top Targets:
7TM GPCR Srx(26)
 
 
 
7TM GPCR Srsx(23)
 
 
 
NR LBD PPAR(14)
 
 
 
p450(10)
 
 
 
 
NR LBD ER(9)
 
 
 
BioAssay Types:
Confirmatory(197)
 
 
 
Literature(108)
 
 
 
 
 
Screening(101)
 
 
 
Summary(24)
 
 
 
BioActivity Types:
Potency(174)
 
 
 
IC50(144)
 
 
 
 
 
EC50(17)
 
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 474    Data Row: 583   Total Pages: 12   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103558703]
EC50 0.29Modulation of human GABA-A alpha1beta2gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726249, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-1 [gi:27808653]
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2
[SID103558703]
EC50 0.29Modulation of human GABA-A alpha1beta2gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726249, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:116242488]
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3
[SID103558703]
EC50 0.29Modulation of human GABA-A alpha1beta2gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726249, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-2 [gi:292495010]
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4
[SID103558703]
IC50 0.412DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flunitrazepam) [AID625261, Type: other]
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5
[SID103558703]
EC50 1.63Modulation of human GABAA alpha2beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726248, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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6
[SID103558703]
EC50 1.63Modulation of human GABAA alpha2beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726248, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:126302547]
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7
[SID103558703]
EC50 1.63Modulation of human GABAA alpha2beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726248, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:116242488]
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8
[SID103558703]
GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator [AID742654, Type: other]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:116242488]
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9
[SID103558703]
GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator [AID742654, Type: other]Gamma-aminobutyric acid receptor subunit alpha-1 [gi:27808653]
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10
[SID103558703]
GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator [AID742654, Type: other]Gamma-aminobutyric acid receptor subunit beta-1 [gi:23831128]
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11
[SID48416707]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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12
[SID103558703]
EC50 1Modulation of human GABAA alpha3beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726247, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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13
[SID103558703]
EC50 1Modulation of human GABAA alpha5beta3gamma3 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726251, Type: Literature]
View
14
[SID103558703]
EC50 1Modulation of human GABAA alpha3beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726247, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-3 [gi:462149]
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15
[SID103558703]
EC50 1Modulation of human GABAA alpha3beta3gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currents [AID726247, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:116242488]
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16
[SID103558703]
Km 124Activity of aldehyde oxidase in human liver cytosol [AID547835, Type: Literature]Aldehyde oxidase [gi:215273968]
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17
[SID103558703]
Activity of aldehyde oxidase in human liver cytosol assessed as enzyme activity per mg of cytosol [AID547836, Type: Literature]Aldehyde oxidase [gi:215273968]
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18
[SID103558703]
IC50 DRUGMATRIX: Vascular Endothelinal Growth Factor (VEGF) radioligand binding (ligand: [125I] VEGF) [AID625231, Type: other]Vascular endothelial growth factor receptor 1 [gi:143811474]
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19
[SID103558703]
IC50 DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) [AID625251, Type: other]Cytochrome P450 3A4 [gi:116241312]
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20
[SID103558703]
IC50 DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) [AID625227, Type: other]Substance-K receptor [gi:229462950]
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21
[SID103558703]
IC50 DRUGMATRIX: Leukotriene LTC4 Synthase enzyme inhibition (substrate: LTA4) [AID625144, Type: other]Leukotriene C4 synthase [gi:239977155]
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22
[SID103558703]
IC50 DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) [AID625178, Type: other]Matrix metalloproteinase-9 [gi:269849668]
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23
[SID103558703]
IC50 DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) [AID625205, Type: other]Beta-2 adrenergic receptor [gi:296439450]
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24
[SID103558703]
DRUGMATRIX: CYP450, 2A6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625246, Type: other]Cytochrome P450 2A6 [gi:308153612]
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25
[SID103558703]
IC50 DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) [AID625161, Type: other]Delta-type opioid receptor [gi:311033488]
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26
[SID103558703]
IC50 DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP) [AID625167, Type: other]cGMP-specific 3',5'-cyclic phosphodiesterase [gi:317373261]
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27
[SID103558703]
IC50 DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) [AID625243, Type: other]Prostaglandin G/H synthase 1 [gi:317373262]
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28
[SID103558703]
DRUGMATRIX: Protein Serine/Threonine Kinase PKCalpha enzyme inhibition (substrate: Histone) [AID625179, Type: other]Protein kinase C alpha type [gi:317373571]
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29
[SID103558703]
IC50 DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) [AID625147, Type: other]Melanocortin receptor 3 [gi:395398606]
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30
[SID103558703]
IC50 DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) [AID625229, Type: other]Thromboxane-A synthase [gi:254763392]
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31
[SID103558703]
DRUGMATRIX: Calcitonin radioligand binding (ligand: [125I] Calcitonin (salmon)) [AID625214, Type: other]Calcitonin receptor [gi:550544247]
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32
[SID103558703]
DRUGMATRIX: Chemokine CXCR1 (IL-8A) [AID625240, Type: other]C-X-C chemokine receptor type 1 [gi:108936015]
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33
[SID103558703]
IC50 DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625162, Type: other]Kappa-type opioid receptor [gi:116242691]
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34
[SID103558703]
IC50 DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) [AID625148, Type: other]Melanocortin receptor 4 [gi:60392672]
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35
[SID103558703]
IC50 DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625247, Type: other]Cytochrome P450 2C19 [gi:60416369]
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36
[SID103558703]
IC50 DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) [AID625202, Type: other]Alpha-2B adrenergic receptor [gi:27151763]
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37
[SID103558703]
IC50 DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) [AID625223, Type: other]Sigma non-opioid intracellular receptor 1 [gi:74752153]
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38
[SID103558703]
IC50 DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) [AID625172, Type: other]Progesterone receptor [gi:75071465]
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39
[SID103558703]
IC50 DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625249, Type: other]Cytochrome P450 2D6 [gi:84028191]
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40
[SID103558703]
IC50 DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625154, Type: other]Muscarinic acetylcholine receptor M4 [gi:23503039]
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41
[SID103558703]
IC50 DRUGMATRIX: Estrogen ERbeta radioligand binding (ligand: [3H] Estradiol) [AID625259, Type: other]Estrogen receptor beta [gi:6166154]
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42
[SID103558703]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) [AID625220, Type: other]5-hydroxytryptamine receptor 4 [gi:6224984]
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43
[SID103558703]
IC50 DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625248, Type: other]Cytochrome P450 2C9 [gi:6686268]
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44
[SID103558703]
IC50 DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) [AID625145, Type: other]Cysteinyl leukotriene receptor 1 [gi:20138087]
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45
[SID103558703]
IC50 DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) [AID625203, Type: other]Alpha-2C adrenergic receptor [gi:20141211]
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46
[SID103558703]
IC50 DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) [AID625204, Type: other]Beta-1 adrenergic receptor [gi:48429211]
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47
[SID103558703]
DRUGMATRIX: Protein Tyrosine Phosphatase, PTPRC (CD45) enzyme inhibition (substrate: DiFMUP) [AID625188, Type: other]Receptor-type tyrosine-protein phosphatase C [gi:33112650]
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48
[SID103558703]
IC50 DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein) [AID625182, Type: other]Mitogen-activated protein kinase 14 [gi:2499600]
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49
[SID103558703]
IC50 DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin) [AID625213, Type: other]B2 bradykinin receptor [gi:2506481]
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50
[SID103558703]
IC50 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) [AID625221, Type: other]5-hydroxytryptamine receptor 6 [gi:1703010]
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