CHEBI:123470 (CID 44273000) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(20)
 
 
Unspecified(29)
 
 
Top Targets:
Neur chan LBD(7)
 
 
 
BioAssay Types:
Literature(49)
 
 
 
BioActivity Types:
IC50(12)
 
 
Ki(6)
 
 
Kd(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 49    Data Row: 49   Total Pages: 1   
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103185420]
Kd 0.0003Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor [AID343089, Type: Literature]
View
2
[SID103185420]
Ki 0.00035Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptor of rat brain membranes [AID40522, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:120758]
View
3
[SID103185420]
IC50 0.00056Partial agonistic activity against specific binding of [3H]-Ro-15-1788 to GABA-A Benzodiazepine receptor in rat cortex [AID40526, Type: Literature]
View
4
[SID103185420]
IC50 0.0006Effect on [3H]flunitrazepam binding to Benzodiazepine receptor [AID40236, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:120788]
View
5
[SID103185420]
IC50 0.0006Effect on [3H]flunitrazepam binding to Benzodiazepine receptor [AID40236, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:120788]
View
6
[SID103185420]
IC50 0.0006Effect on [3H]flunitrazepam binding to Benzodiazepine receptor [AID40236, Type: Literature]Gamma-aminobutyric acid receptor subunit gamma-2 [gi:120788]
View
7
[SID103185420]
IC50 0.0006Binding affinity for rat benzodiazepine receptor inverse agonist site [AID40085, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:120758]
View
8
[SID103185420]
IC50 0.0006In vitro inhibition of binding to GABA-A central benzodiazepine-receptor of rat brain [AID40997, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:120758]
View
9
[SID103185420]
IC50 0.0006Concentration to inhibit [3H]flunitrazepam binding to rat cerebral cortical membrane [AID40235, Type: Literature]
View
10
[SID103185420]
IC50 0.0006Binding affinity towards benzodiazepine receptor inverse agonist site by the displacement of [3H]diazepam in rat cerebral cortical membranes. [AID40509, Type: Literature]
View
11
[SID103185420]
IC50 0.0006In vitro inhibition of 3[H]Diazepam binding to Benzodiazepine receptor from rat cerebral cortical membranes [AID40514, Type: Literature]
View
12
[SID103185420]
IC50 0.000603Inhibition on Benzodiazepine receptor [AID40988, Type: Literature]
View
13
[SID103185420]
Ki 0.00083Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor [AID39937, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:52000955]
View
14
[SID103185420]
Ki 0.00083Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor [AID39937, Type: Literature]Gamma-aminobutyric acid receptor subunit beta-3 [gi:52000955]
View
15
[SID103185420]
Ki 0.00083Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats [AID40967, Type: Literature]
View
16
[SID103185420]
Ki 0.00083Displacing potential to [3H]diazepam binding to benzodiazepine receptor in Wistar rat cerebral cortex [AID40503, Type: Literature]
View
17
[SID103185420]
IC50 0.001Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 expressed in CHO cells [AID577825, Type: Literature]
View
18
[SID103185420]
IC50 0.00115Displacement of [3H]diazepam from GABAA/BzR in rat brain membrane [AID348954, Type: Literature]
View
19
[SID103185420]
Ki 0.0024Binding affinity to Wistar rat benzodiazepine receptor [AID261133, Type: Literature]Gamma-aminobutyric acid receptor subunit pi [gi:3023821]
View
20
[SID103185420]
IC50 0.004Displacement of [3H]flumazenil from GABAA receptor subunit alpha-2 expressed in CHO cells [AID577826, Type: Literature]
View
21
[SID103185420]
IC50 0.6Displacement of 3[H]Flunitrazepam from GABA-A central benzodiazepine receptor of bovine brain membranes [AID41994, Type: Literature]
View
22
[SID103185420]
Ki Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor [AID343090, Type: Literature]
View
23
[SID103185420]
 Plasma concentration in cynomolgus monkey at 5 mg/kg, po [AID261144, Type: Literature]
View
24
[SID103185420]
 In vivo inhibition of binding to GABA-A central benzodiazepine-receptor after ip administration in rats [AID40998, Type: Literature]Gamma-aminobutyric acid receptor subunit alpha-2 [gi:120758]
View
25
[SID103185420]
 Agonist activity at recombinant GABAA receptor subunit alpha-1 expressed in CHO cells at 1 uM by sensitive fluorometric read-out assay relative to midazolam [AID577828, Type: Literature]
View
26
[SID103185420]
 Agonist activity at recombinant GABAA receptor subunit alpha-2 expressed in CHO cells at 1 uM by sensitive fluorometric read-out assay relative to midazolam [AID577829, Type: Literature]
View
27
[SID103185420]
 Anxiolytic activity in NMRI BR mice after ip administration by PTZ test [AID261135, Type: Literature]
View
28
[SID103185420]
 Neurotoxicological activity in NMRI BR mice after ip administration by rotarod test [AID261136, Type: Literature]
View
29
[SID103185420]
 Anxiolytic activity in rat after oral administration by PTZ test [AID261137, Type: Literature]
View
30
[SID103185420]
 Anxiolytic activity in rat after oral administration by vogel conflict test [AID261138, Type: Literature]
View
31
[SID103185420]
 Neurotoxicological activity in rat after oral administration by rotarod test [AID261139, Type: Literature]
View
32
[SID103185420]
 Protective index (PI=TD50/ED50) in rat after oral administration [AID261140, Type: Literature]
View
33
[SID103185420]
 Agonist activity was evaluated by inhibition of the PTZ-induced convulsions at a PTZ dose of 125 mg/ kg [AID112905, Type: Literature]
View
34
[SID103185420]
 Percent of mice not grasping wire at a dose of 300 mg/Kg administered intraperitoneally in horizontal wire test [AID125477, Type: Literature]
View
35
[SID103185420]
 Activity in mouse pentylenetetrazole convulsant test. [AID128303, Type: Literature]
View
36
[SID103185420]
 Agonist activity was evaluated by the inhibition of the pentylenetetrazole (PTZ) induced convulsions after peroral administration [AID128305, Type: Literature]
View
37
[SID103185420]
 Effective dose required for the percentage change in seizure threshold by anti-pentylenetetrazole test in mouse when administered perorally [AID131889, Type: Literature]
View
38
[SID103185420]
 Anxiolytic response measured by antagonism of pentylenetetrazole discriminative stimuli in rats. [AID176300, Type: Literature]
View
39
[SID103185420]
 Anticonvulsant efficacy when administered perorally was determined in rat metrazole anticonvulsant test [AID178307, Type: Literature]
View
40
[SID103185420]
 Antianxiety effect was assessed by the cook-davidson behavior test [AID180952, Type: Literature]
View
41
[SID103185420]
 Antianxiety effect was assessed by the cook-davidson behavior test at 1 mg/kg of compound administered perorally. [AID180957, Type: Literature]
View
42
[SID103185420]
 Antianxiety effect was assessed by the cook-davidson behavior test at 10 mg/kg of compound administered perorally. [AID180958, Type: Literature]
View
43
[SID103185420]
 Antianxiety effect was assessed by the cook-davidson behavior test at 3 mg/kg of compound administered perorally. [AID180959, Type: Literature]
View
44
[SID103185420]
 Minimal effective oral dose to cause VI response decrement in rats; No significant response at highest dose tested [AID184847, Type: Literature]
View
45
[SID103185420]
 Minimal effective oral dose to cause ethanol interaction in rats. [AID184848, Type: Literature]
View
46
[SID103185420]
 Minimal effective oral dose to cause increase in conflict response in rats after po administration. [AID184849, Type: Literature]
View
47
[SID103185420]
 Compound was administered at a dose of 10 mg/Kg intraperitoneally and was evaluated for shock induced suppression of drinking by rat vogel test and number of shocks taken were reported [AID188915, Type: Literature]
View
48
[SID103185420]
 Antianxiety effect in cook-davidson behavior test at 1 mg/kg of compound administered perorally in rats expressed as mean percent change [AID191851, Type: Literature]
View
49
[SID103185420]
 Antianxiety effect in cook-davidson behavior test at 10 mg/kg of compound administered perorally in rats expressed as mean percent change [AID191852, Type: Literature]
View
50
[SID103185420]
 Antianxiety effect in cook-davidson behavior test at 3 mg/kg of compound administered perorally in rats expressed as mean percent change [AID191853, Type: Literature]
View