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Baclofen (CID 2284) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(36)
 
 
Inactive(622)
 
 
Inconclusive(49)
 
 
Unspecified(238)
 
 
Top Targets:
7TM GPCR Srx(26)
 
 
 
 
PBP1 GABAb re..(20)
 
 
 
7TM GPCR Srsx(20)
 
 
 
 
Neur chan LBD(14)
 
 
NR LBD ER(13)
 
 
 
BioAssay Types:
Confirmatory(402)
 
 
 
 
 
Literature(185)
 
 
 
 
Screening(124)
 
 
Summary(25)
 
 
BioActivity Types:
Potency(386)
 
 
 
 
 
IC50(159)
 
 
 
 
EC50(10)
 
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 698    Data Row: 945   Total Pages: 19   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103194022]
IC50 0.03Displacement of [3H]GABA from Gamma-aminobutyric acid A (GABA-A) receptor in rat brain membranes [AID72152, Type: Literature]
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2
[SID103194022]
IC50 0.03In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes [AID71389, Type: other]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643481]
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3
[SID103194022]
IC50 0.03In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes [AID71389, Type: other]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643494]
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4
[SID103194022]
IC50 0.035Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum [AID71258, Type: Literature]
View
5
[SID103194022]
IC50 0.05Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA [AID255079, Type: Literature]Adenosine receptor A3 [gi:1351831]
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6
[SID103194022]
IC50 0.06Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor in rat brain membranes [AID71395, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643494]
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7
[SID103194022]
IC50 0.06Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor in rat brain membranes [AID71395, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643481]
View
8
[SID103194022]
IC50 0.107Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex [AID71401, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643494]
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9
[SID103194022]
IC50 0.107Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex [AID71401, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643481]
View
10
[SID103194022]
IC50 0.2Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranes [AID71399, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643494]
View
11
[SID103194022]
IC50 0.2Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptosomes after 30 minutes [AID71398, Type: other]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643494]
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12
[SID103194022]
IC50 0.2Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain synaptosomes after 30 minutes [AID71398, Type: other]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643481]
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13
[SID103194022]
IC50 0.2Displacement of [3H]baclofen from Gamma-aminobutyric acid type B receptor of rat brain membranes [AID71399, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643481]
View
14
[SID103194022]
Ki 0.22Displacement of [3H]GABA from GABABreceptor in rat brain synaptic membranes [AID339808, Type: Literature]
View
15
[SID103194022]
IC50 0.33Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor. [AID71390, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643494]
View
16
[SID103194022]
IC50 0.33Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor. [AID71390, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643481]
View
17
[SID103194022]
IC50 0.42Displacement of [3H]baclofen from gamma-aminobutyric-acid B receptor [AID71388, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643481]
View
18
[SID103194022]
IC50 0.42Displacement of [3H]baclofen from gamma-aminobutyric-acid B receptor [AID71388, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643494]
View
19
[SID103194022]
EC50 0.75Agonist activity at human recombinant GABABreceptor expressed in CHO-K1 cells assessed as inhibition of intracellular calcium release by FLIPR [AID339809, Type: Literature]
View
20
[SID103194022]
EC50 1.7Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay [AID729173, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643873]
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21
[SID103194022]
EC50 1.7Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay [AID729173, Type: Literature]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643641]
View
22
[SID103194022]
IC50 1.8The inhibitory concentration of compound against sodium dependent [3H]GABA synaptosomal uptake in rats [AID180672, Type: Literature]
View
23
[SID855960]
Potency 5.6234qHTS Assay for Identification of Small Molecule Antagonists for NFkB Signaling Pathway [AID895, Type: confirmatory]NFKB1 protein [Homo sapiens] [gi:21620132]
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24
[SID103194022]
IC50 6.4Compound was tested for its effect on EFS stimulated neuronal cholinergic contractions of guinea pig tracheal rings after 10 minutes [AID78144, Type: other]
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25
[SID90341690]
Potency 9.2Nrf2 qHTS screen for inhibitors: Validation [AID493153, Type: confirmatory] [geneid:4780]
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26
[SID90341690]
Potency 9.2Nrf2 qHTS screen for inhibitors: Validation [AID493153, Type: confirmatory]nuclear factor erythroid 2-related factor 2 isoform 2 [Homo sapiens] [gi:224028257]
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27
[SID10321186]
MDR-1 [AID377, Type: other]multidrug resistance protein 1 [Homo sapiens] [gi:42741659]
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28
[SID103194022]
GABA-B receptor agonist [AID742537, Type: other]Gamma-aminobutyric acid type B receptor subunit 1 [gi:12643873]
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29
[SID103194022]
GABA-B receptor agonist [AID742537, Type: other]Gamma-aminobutyric acid type B receptor subunit 2 [gi:12643641]
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30
[SID85208873]
Ligands of Class C GPCRs [AID2059, Type: other]
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31
[SID85208873]
Ligands of peptide (Class A) GPCRs [AID2063, Type: other]
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32
[SID48415601]
DSSTox (FDAMDD) FDA Maximum (Recommended) Daily Dose Database [AID1195, Type: other]
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33
[SID103194022]
FDA HLAED, liver enzyme composite activity [AID588214, Type: Literature]
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34
[SID103194022]
FDA HLAED, alkaline phosphatase increase [AID588215, Type: Literature]
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35
[SID103194022]
FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase [AID588216, Type: Literature]
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36
[SID103194022]
Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method [AID604020, Type: Literature]
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37
[SID103194022]
EC50 100Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method [AID729172, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:120788]
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38
[SID103194022]
EC50 100Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method [AID729172, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-2 [gi:52000957]
View
39
[SID103194022]
EC50 100Agonist activity at rat GABA-A alpha1beta2gamma2 receptor expressed in human TSA201 cells by whole cell voltage-clamp method [AID729172, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-1 [gi:51317298]
View
40
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-1 [gi:51317298]
View
41
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:52000955]
View
42
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-2 [gi:52000957]
View
43
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]GABA theta subunit [gi:81902501]
View
44
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-3 [gi:120790]
View
45
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-6 [gi:232127]
View
46
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:120758]
View
47
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-3 [gi:120761]
View
48
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-4 [gi:120763]
View
49
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-5 [gi:120764]
View
50
[SID103194022]
IC50 1047Inhibition of [3H]muscimol binding to GABA-A receptor of rat cortex [AID71997, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-1 [gi:120769]
View