Chlordiazepoxide (CID 2712) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(36)
 
 
Inactive(372)
 
 
Inconclusive(49)
 
 
Unspecified(276)
 
 
Top Targets:
Neur chan LBD(30)
 
 
 
 
7TM GPCR Srx(21)
 
 
 
7TM GPCR Srsx(15)
 
 
 
p450(8)
 
 
TRP 2(5)
 
 
BioAssay Types:
Screening(294)
 
 
 
Literature(191)
 
 
 
 
 
Confirmatory(73)
 
 
 
 
BioActivity Types:
IC50(160)
 
 
 
 
 
Potency(56)
 
 
 
 
Ki(17)
 
 
EC50(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 725    Data Row: 733   Total Pages: 15   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103165933]
IC50 0.2Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor [AID40230, Type: Literature]
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2
[SID103165933]
IC50 0.2Inhibition of specific binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptors [AID40519, Type: Literature]
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3
[SID103165933]
IC50 0.2Inhibitory concentration against specific binding of [3H]diazepam to Benzodiazepine receptor in rat brain [AID40521, Type: Literature]
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4
[SID103165933]
IC50 0.248In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat [AID40661, Type: Literature]
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5
[SID103165933]
Ki 0.275Binding affinity by displacement of [3H]Ro-151788 from recombinant human gamma-aminobutyric-acid A receptor alpha3,beta3,gamma2 stably expressed in L cells [AID73245, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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6
[SID103165933]
Ki 0.32Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-5-beta-3-gamma-2) stably expressed in L(tk-) cells. [AID73526, Type: Literature]
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7
[SID103165933]
IC50 0.33Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortex [AID40231, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:120758]
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8
[SID103165933]
Ki 0.368Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 [AID73380, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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9
[SID103165933]
Ki 0.368Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells [AID239702, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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10
[SID103165933]
Ki 0.392Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells [AID239700, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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11
[SID103165933]
Ki 0.392Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 [AID73080, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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12
[SID103165933]
Ki 0.438Binding affinity against rat benzodiazepine (BZD) receptor [AID39933, Type: Literature]
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13
[SID103165933]
IC50 0.442Inhibition of binding of tritiated 3[H]diazepam radioligand to rat brain homogenates [AID40833, Type: Literature]
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14
[SID103165933]
Ki 0.46Displacement of [3H]Ro-151788 from human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 stably expressed in L(tk-) cells [AID73090, Type: Literature]
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15
[SID103165933]
Ki 0.46Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-2-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes [AID73081, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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16
[SID103165933]
Ki 0.471Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 [AID73235, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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17
[SID103165933]
Ki 0.471Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells [AID239701, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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18
[SID103165933]
Ki 0.52Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-5-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes [AID73382, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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19
[SID103165933]
Ki 0.56Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-1-beta-3-gamma-2) stably expressed in L(tk-) cells. [AID72930, Type: Literature]
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20
[SID103165933]
Ki 0.605Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells [AID239699, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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21
[SID103165933]
Ki 0.605Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 [AID72918, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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22
[SID103165933]
IC50 0.71Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cerebral cortex membrane [AID40227, Type: Literature]
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23
[SID103165933]
Ki 0.74Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-3-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes [AID73236, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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24
[SID103165933]
Ki 0.77Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-1-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes [AID72919, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:120773]
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25
[SID103165933]
IC50 0.79Displacement of 3[H]Flunitrazepam from GABA-A central benzodiazepine receptor of bovine brain membranes [AID41994, Type: Literature]
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26
[SID103165933]
IC50 0.79Inhibition of [3H]flunitrazepam binding to benzodiazepine receptor in bovine brain membrane [AID41998, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-1 [gi:120752]
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27
[SID103165933]
IC50 0.91Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor in synaptic membranes of rat cerebral cortex [AID40835, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:120758]
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28
[SID103165933]
IC50 1.1Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes [AID41996, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-1 [gi:120752]
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29
[SID103165933]
IC50 1.429DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flunitrazepam) [AID625261, Type: other]
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30
[SID103165933]
IC50 1.795DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) [AID625269, Type: other]Histamine H1 receptor [gi:547645]
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31
[SID103165933]
IC50 1.795DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) [AID625269, Type: other]Histamine H1 receptor [gi:547645]
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32
[SID49648393]
 Primary cell-based high-throughput screening for identification of compounds that allosterically activate MrgX1 receptor signaling [AID588675, Type: screening]MAS-related GPR member X1 [Homo sapiens] [gi:195969650]
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33
[SID49648393]
 Primary cell-based high-throughput screening for identification of compounds that allosterically activate MrgX1 receptor signaling [AID588675, Type: screening]MAS-related GPR member X1 [Homo sapiens] [gi:195969650]
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34
[SID103165933]
 Activity in rat elevated plus maze assay at 5 mg/kg, ip [AID259155, Type: Literature]
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35
[SID103165933]
 Binding constant was determined by displacing potential to [3H]-diazepam binding in cerebral cortex homogenates of rat [AID40839, Type: Literature]
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36
[SID103165933]
 Mouse behavior activity was determined; D = Depressant [AID134938, Type: Literature]
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37
[SID48415753]
 DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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38
[SID103856643]
 Wombat Data for BeliefDocking [AID493017, Type: Literature] [geneid:2554]
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39
[SID103856643]
 Wombat Data for BeliefDocking [AID493017, Type: Literature] [geneid:2554]
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40
[SID103165933]
IC50 100Inhibition of binding of [125I]gastrin to guinea pig gastric glands [AID76082, Type: Literature]
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41
[SID103165933]
IC50 100Binding affinity towards cholecystokinin receptor by displacement of [125I]CCK-33 from guinea pig brain tissue [AID52277, Type: Literature]
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42
[SID103165933]
IC50 100Binding affinity towards cholecystokinin receptor by the displacement of [125I]CCK-33 in rat pancreatic tissue [AID52418, Type: Literature]
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43
[SID103165933]
 Modulatory effect on coapplication with GABA at human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 in Xenopus oocyte. [AID72922, Type: Literature]
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44
[SID103165933]
 Volume of distribution at steady state in human after iv administration [AID540209, Type: Literature]
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45
[SID103165933]
 Clearance in human after iv administration [AID540210, Type: Literature]
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46
[SID103165933]
 Fraction unbound in human after iv administration [AID540211, Type: Literature]
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47
[SID103165933]
 Mean residence time in human after iv administration [AID540212, Type: Literature]
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48
[SID103165933]
 Half life in human after iv administration [AID540213, Type: Literature]
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49
[SID103165933]
 Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans [AID588211, Type: Literature]
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50
[SID103165933]
 Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents [AID588212, Type: Literature]
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