|
Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor
|
Rattus norvegicus
|
25.0
nM
|
|
|
Displacement of [3H]flunitrazepam from rat brain GABA-A Benzodiazepine receptor
|
Rattus norvegicus
|
48.0
nM
|
|
|
Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 2
|
Xenopus laevis
|
737.0
nM
|
|
|
Displacement of [3H]-Ro-15-1788 from rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
156.0
nM
|
|
|
Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
383.0
nM
|
|
|
Binding affinity to rat chimeric GABA-A receptor C6, alpha1-alpha6 chimeric subunit co-expressed with beta-2 gamma2 subunits in HEK293 cells
|
Rattus norvegicus
|
125.0
nM
|
|
|
Inhibition of [3H]flumazenil specific binding at rat GABA-A alpha-1-beta-2-gamma-2 receptor subunits expressed in HEK293 cells
|
Rattus norvegicus
|
50.0
nM
|
|
|
Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells
|
Homo sapiens
|
27.0
nM
|
|
|
Inhibition of [3H]flumazenil binding to recombinant GABA-A receptor alpha-1 subunit in cerebellum
|
None
|
14.0
nM
|
|
|
Inhibition of [3H]flumazenil binding to recombinant GABA-A receptor alpha-1 subunit in spinal cord
|
None
|
130.0
nM
|
|
|
Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells
|
Homo sapiens
|
160.0
nM
|
|
|
Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells
|
Homo sapiens
|
380.0
nM
|
|
|
Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
26.7
nM
|
|
|
Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
26.7
nM
|
|
|
Inhibition of [3H]flumazenil binding to recombinant GABA-A receptor alpha-1-beta-2-gamma-2 subunits
|
None
|
46.3
nM
|
|
|
Binding affinity towards human alpha-1-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells
|
None
|
52.1
nM
|
|
|
Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2
|
None
|
26.7
nM
|
|
|
Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
156.0
nM
|
|
|
Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells
|
None
|
255.1
nM
|
|
|
Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2
|
None
|
156.0
nM
|
|
|
Binding affinity for recombinant rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
383.0
nM
|
|
|
Inhibition of [3H]-flumazenil binding to rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
765.0
nM
|
|
|
Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells
|
None
|
608.5
nM
|
|
|
Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2
|
None
|
383.0
nM
|
|
|
Inhibition of [3H]flumazenil binding to rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK293 cells at 10 uM
|
Rattus norvegicus
|
35.0
%
|
|
|
Binding affinity was determined by displacement of [3H]flumazenil from rat cortex homogenates
|
Rattus norvegicus
|
48.0
nM
|
|
|
Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
19.0
nM
|
|
|
Binding affinity measured using LtK- cell membranes expressing GABA alpha-1-beta-3-gamma-2 receptor
|
None
|
26.7
nM
|
|
|
Potentiation of GABA-evoked Cl- currents in Xenopus oocytes expressing human alpha-2-beta-2-gamma-2 subunits
|
Homo sapiens
|
180.0
nM
|
|
|
Binding affinity measured using LtK- cell membranes expressing GABA alpha-2-beta-3-gamma-2 receptor
|
None
|
156.0
nM
|
|
|
Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
400.0
nM
|
|
|
Binding affinity measured using LtK- cell membranes expressing GABA alpha-3-beta-3-gamma-2 receptor
|
None
|
383.0
nM
|
|
|
Binding affinity for mutant rat GABA-A receptor alpha-4-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
76.0
nM
|
|
|
Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells
|
Rattus norvegicus
|
980.0
nM
|
|
|
Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1
|
Xenopus laevis
|
198.0
nM
|
|
|
Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells
|
Homo sapiens
|
103.0
nM
|
|
|
Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 subtype expressed in L (tk-) cells
|
Homo sapiens
|
27.0
nM
|
|
|
Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 subtype expressed in L (tk-) cells
|
Homo sapiens
|
246.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABA-A Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 expressed in HEK293 cells
|
Rattus norvegicus
|
50.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABA-A Gamma-aminobutyric acid A receptor alpha-2-beta-2-gamma-2 expressed in HEK293 cells
|
Rattus norvegicus
|
765.0
nM
|
|
|
Inhibition of [3H]flumazenil binding to rat Gamma-aminobutyric acid A GABA-A receptor alpha-5-beta-3-gamma-2 expressed in HEK293 cells
|
Rattus norvegicus
|
35.0
%
|
|
|
Binding affinity for rat alpha-1 beta2/3 gamma2 GABA A / BzR receptor
|
Rattus norvegicus
|
26.7
nM
|
|
|
Binding affinity for rat alpha2 beta2/3 gamma2 GABA-A/BzR receptor
|
Rattus norvegicus
|
156.0
nM
|
|
|
Binding affinity for rat alpha-3 beta2/3 gamma2 GABA-A/BzR receptor
|
Rattus norvegicus
|
383.0
nM
|
|
|
Displacement of [3H]Flumazenil from human GABA-Aalpha1 receptor plus beta-2-gamma-2 expressed in HEK293 cells
|
Homo sapiens
|
53.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABA-Aalpha1 receptor plus beta-2-gamma-2 in HEK293 cells
|
Rattus norvegicus
|
50.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABA-Aalpha2 receptor plus beta-2-gamma-2 in HEK293 cells
|
Rattus norvegicus
|
765.0
nM
|
|
|
Inhibition of [3H]flumazenil binding to rat GABA-Aalpha5 receptor plus beta-3-gamma-2 at 10 uM in HEK293 cells
|
Rattus norvegicus
|
35.0
%
|
|
|
Displacement of [3H]flumazenil from rat GABAA alpha-1-beta-2-gamma-2 expressed in HEK293 cells
|
Rattus norvegicus
|
50.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABAA alpha-2-beta-2-gamma-2 expressed in HEK293 cells
|
Rattus norvegicus
|
765.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABAA alpha-5-beta-3-gamma-2 expressed in HEK293 cells at 10 uM
|
Rattus norvegicus
|
35.0
%
|
|
|
Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in L(tk-) cells
|
Homo sapiens
|
27.0
nM
|
|
|
Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in L(tk-) cells
|
Homo sapiens
|
160.0
nM
|
|
|
Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in L(tk-) cells
|
Homo sapiens
|
380.0
nM
|
|
|
Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 receptor expressed in HEK293T cells
|
None
|
61.9
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-2-beta-2-gamma-2 receptor expressed in HEK293T cells
|
None
|
408.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 D56C receptor mutant expressed in HEK293T cells
|
None
|
67.6
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 A79C receptor mutant expressed in HEK293T cells
|
None
|
577.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 T81C receptor mutant expressed in HEK293T cells
|
None
|
108.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 T126C receptor mutant expressed in HEK293T cells
|
None
|
72.7
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 M130C receptor mutant expressed in HEK293T cells
|
None
|
15.5
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 R132C receptor mutant expressed in HEK293T cells
|
None
|
35.8
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 L140C receptor mutant expressed in HEK293T cells
|
None
|
63.1
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 R144C receptor mutant expressed in HEK293T cells
|
None
|
38.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 X161 receptor mutant expressed in HEK293T cells
|
None
|
427.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 R185C receptor mutant expressed in HEK293T cells
|
None
|
67.4
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 R194C receptor mutant expressed in HEK293T cells
|
None
|
62.6
nM
|
|
|
Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1 F99C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
180.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha1 A160C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
81.4
nM
|
|
|
Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha1 T162C beta-2-gamma-2 receptor mutant expressed in HEK293T cells
|
None
|
109.0
nM
|
|
|
Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1 G200C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
598.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha1 V202C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
556.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha1 S204C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
433.0
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha1 S205C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
41.2
nM
|
|
|
Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1 T206C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
76.4
nM
|
|
|
Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1 V211C beta2gamma2 receptor mutant expressed in HEK293T cells
|
None
|
67.8
nM
|
|
|
Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-3-beta-2-gamma-2 receptor expressed in HEK293T cells
|
None
|
975.0
nM
|
|
|
Activity at rat wild type GABAA alpha-1V211Cbeta-2-gamma-2 mutant receptor expressed in xenopus oocytes assessed as GABA-elicited response by two electrode voltage clamp method relative to control
|
Rattus norvegicus
|
341.0
nM
|
|
|
Activity at rat GABAA alpha-1H101Cbeta-2-gamma-2 mutant receptor expressed in xenopus oocytes assessed as change in GABA-induced current amplitude at 10 uM after 1 min exposure to GABA by two electrode voltage clamp method
|
Rattus norvegicus
|
220.0
%
|
|
|
Activity at rat GABAA alpha-1H101Cbeta-2-gamma-2 mutant receptor expressed in xenopus oocytes assessed as change in GABA-induced current amplitude at 10 uM after 1 min exposure to GABA by two electrode voltage clamp method
|
Rattus norvegicus
|
96.0
%
|
|
|
Activity at rat wild type GABAA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as GABA-elicited response by two electrode voltage clamp method relative to control
|
Rattus norvegicus
|
191.0
nM
|
|
|
Displacement of [3H]flumazenil from Benzodiazepine receptor in bovine cerebral cortex membrane
|
Bos taurus
|
51.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells
|
Rattus norvegicus
|
50.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells
|
Rattus norvegicus
|
765.0
nM
|
|
|
Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells
|
Rattus norvegicus
|
35.0
nM
|
|
|
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting
|
Homo sapiens
|
26.7
nM
|
|
|
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting
|
Homo sapiens
|
156.0
nM
|
|
|
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting
|
Homo sapiens
|
383.0
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
177.44
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
78.05
%
|
|
|
Displacement of [3H]-flunitrazepam from rat brain GABA-A receptor benzodiazepine site after 20 mins by liquid scintillation counting
|
Rattus norvegicus
|
44.0
nM
|
|
|
Positive allosteric modulation of human recombinant GABA-A receptor alpha1beta2gamma2 expressed in HEK293 cells assessed as potentiation of of GABA induced chloride currents treated every 60 secs measured for 7 secs by electrophysiological method
|
Homo sapiens
|
240.0
nM
|
|
|
Displacement of [3H]RO15-1788 from recombinant rat GABAalpha1 receptor expressed in HEK293 cells after 1 hr
|
Rattus norvegicus
|
26.7
nM
|
|
|
Displacement of [3H]RO15-1788 from recombinant rat GABAalpha2 receptor expressed in HEK293 cells after 1 hr
|
Rattus norvegicus
|
156.0
nM
|
|
|
Displacement of [3H]RO15-1788 from recombinant rat GABAalpha3 receptor expressed in HEK293 cells after 1 hr
|
Rattus norvegicus
|
383.0
nM
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
0.52
%
|
|
|
Inhibition of GABAA receptor alpha1 (unknown origin)
|
Homo sapiens
|
20.0
nM
|
|
|
Inhibition of GABAA receptor alpha3 (unknown origin)
|
Homo sapiens
|
400.0
nM
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
4.533
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.09
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.09
%
|
|
|
Positive allosteric modulator activity at rat alpha1beta2gamma2L GABA-A receptor expressed in Xenopus laevis oocytes in presence of EC2-5 GABA by two-electrode voltage clamp assay
|
Rattus norvegicus
|
340.0
nM
|
|
