Binding affinity of compound was determined against Glutamate receptor (KA2) using cell membranes prepared from HEK293 cells
|
None
|
750.0
nM
|
|
The effective concentration for 50% glutamate response was measured on Group II Metabotropic glutamate receptor
|
None
|
290.0
nM
|
|
Binding affinity was measured by [3H]- Ionotropic glutamate receptor AMPA binding assay.
|
None
|
500.0
nM
|
|
Compound was evaluated for the inhibition of [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat brain synaptic membrane.
|
None
|
150.0
nM
|
|
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 2 expressed in HEK293 cells
|
Homo sapiens
|
940.0
nM
|
|
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 2 using cell membranes prepared from HEK293 cells
|
None
|
940.0
nM
|
|
Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 2 in HK293 cells using [3H]AMPA as radioligand
|
None
|
940.0
nM
|
|
Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells
|
Homo sapiens
|
868.0
nM
|
|
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA 4 using cell membranes prepared from HEK293 cells
|
None
|
868.0
nM
|
|
Compound was tested for binding affinity against human Ionotropic glutamate receptor AMPA 4 in HEK293 cells using [3H]AMPA as radioligand
|
None
|
868.0
nM
|
|
Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 1 using cell membranes prepared from HEK293 cells
|
None
|
701.0
nM
|
|
Binding affinity against human ionotropic glutamate receptor kainate 1 in HK293 cells using [3H]kainate as radioligand
|
None
|
701.0
nM
|
|
Displacement of [3H]kainate from human Ionotropic glutamate receptor ionotropic kainate 1 expressed in HEK293 cells
|
Homo sapiens
|
701.0
nM
|
|
Ability to bind to Ionotropic glutamate receptor ionotropic kainate 3 was evaluated
|
None
|
789.0
nM
|
|
Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 3 using cell membranes prepared from HEK293 cells
|
None
|
789.0
nM
|
|
Ability to bind to Ionotropic glutamate receptor kainate (kainate 2) was evaluated.
|
None
|
750.0
nM
|
|
Binding affinity against Ionotropic glutamate receptor kainate by displacing [3H]KA from purified rat synaptic membranes
|
None
|
350.0
nM
|
|
Binding affinity was measured by [3H]- KAIN receptor binding assay.
|
None
|
400.0
nM
|
|
Compound tested for binding affinity towards Ionotropic glutamate receptor kainate
|
None
|
400.0
nM
|
|
Compound was evaluated for the inhibition of [3H]-KA binding to Ionotropic glutamate receptor kainate from rat brain synaptic membrane.
|
None
|
120.0
nM
|
|
Inhibition of specific binding of [3H]kainate to Ionotropic glutamate receptor kainate in rat brain membranes
|
None
|
700.0
nM
|
|
Binding affinity towards Ionotropic glutamate receptor kainate by displacement of [3H]-kainic acid radioligand
|
None
|
63.0
nM
|
|
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
|
None
|
22.0
nM
|
|
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
|
Rattus norvegicus
|
340.0
nM
|
|
Compound was tested for the inhibition of metabotropic glutamate receptor 2 (mGluR2).
|
None
|
290.0
nM
|
|
Binding affinity was measured by NMDA sensitive [3H]- glutamic acid receptor binding assay.
|
None
|
200.0
nM
|
|
Compound was evaluated for the inhibition of [3H]MK-801 binding at N-methyl-D-aspartate glutamate receptor
|
None
|
120.0
nM
|
|
Compound was evaluated for the inhibition of [3H]-CGS-19,755 binding at N-methyl-D-aspartate glutamate receptor
|
None
|
172.0
nM
|
|
Inhibition of N-methyl-D-aspartate glutamate receptor by using [3H]CPP as a radioligand from the rat cortical membranes.
|
None
|
171.0
nM
|
|
Compound was evaluated for the inhibition of [3H]CGS-19,755 binding to NMDA receptor from rat brain synaptic membrane.
|
None
|
80.0
nM
|
|
Inhibition of [3H]CPP binding to rat N-methyl-D-aspartate glutamate receptor
|
Rattus norvegicus
|
70.0
nM
|
|
Binding affinity towards NMDA receptor by displacement of [3H]CGP-39653 radioligand.
|
None
|
200.0
nM
|
|
Effective concentration against NR1/NR2B receptor
|
None
|
800.0
nM
|
|
Effective concentration against NR1/NR2C receptor
|
None
|
700.0
nM
|
|
Effective concentration against NR1/NR2D receptor
|
None
|
400.0
nM
|
|
In vitro binding affinity against synaptic membrane from rat brain using [3H]-AMPA as the radioligand
|
None
|
500.0
nM
|
|
In vitro binding affinity against synaptic membrane from rat brain using [3H]KAIN as the radioligand
|
None
|
270.0
nM
|
|
In vitro binding affinity against synaptic membrane from rat brain using [3H](S)-Glu as the radioligand
|
Rattus norvegicus
|
170.0
nM
|
|
Inhibitory activity against Tetanus neurotoxin (TeNt) light chain by using fluorescent synaptobrevin derivative [Pya88]S 39-88 as substrate at 10e-3 M.
|
None
|
0.0
%
|
|
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing mGluR2 receptor
|
None
|
610.0
nM
|
|
Displacement of L-[3H]glutamate from N-methyl-D-aspartate glutamate receptor in rat brain synaptic membranes
|
Rattus norvegicus
|
870.0
nM
|
|
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
|
Homo sapiens
|
5.7
nM
|
|
Percent inhibition against AMPA receptor at 1 uM
|
Homo sapiens
|
613.0
nM
|
|
Antagonist activity against AMPA receptor expressed in motoneurones by inhibition of fDR-VRP in the neonatal rat spinal cord
|
Rattus norvegicus
|
214.0
nM
|
|
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
|
Homo sapiens
|
250.0
nM
|
|
Binding affinity to mGluR5 receptor expressed in BHK cells
|
Homo sapiens
|
390.0
nM
|
|
Displacement of [3H]CGP-39653 from rat NMDA receptor expressed in BHK cells
|
Rattus norvegicus
|
200.0
nM
|
|
Displacement of [3H]kainic acid from rat KA receptor expressed in BHK cells
|
Rattus norvegicus
|
70.0
nM
|
|
Displacement of [3H]AMPA from rat AMPA receptor expressed in BHK cells
|
Rattus norvegicus
|
80.0
nM
|
|
Displacement of [3H]AMPA from AMPA receptor in rat cortical synaptosome
|
Rattus norvegicus
|
340.0
nM
|
|
Displacement of [3H]KAIN from KA receptor in rat cortical synaptosome
|
Rattus norvegicus
|
380.0
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor in rat cortical synaptosome
|
Rattus norvegicus
|
200.0
nM
|
|
Activity at rat NR1/NR2D receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology
|
Rattus norvegicus
|
450.0
nM
|
|
Inhibition of [3H]D-Asp uptake at human EAAT3 in HEK293 cells
|
Homo sapiens
|
51.0
nM
|
|
Displacement of [3H]SYM2081 from rat recombinant iGluR5
|
Rattus norvegicus
|
140.0
nM
|
|
Displacement of [3H]SYM2081 from rat recombinant iGluR5
|
Rattus norvegicus
|
138.04
nM
|
|
Displacement of [3H]SYM2081 from rat recombinant iGluR6
|
Rattus norvegicus
|
331.0
nM
|
|
Displacement of [3H]SYM2081 from rat recombinant iGluR6
|
Rattus norvegicus
|
331.13
nM
|
|
Displacement of [3H]SYM2081 from rat recombinant iGluR7
|
Rattus norvegicus
|
494.0
nM
|
|
Displacement of [3H]SYM2081 from rat recombinant iGluR7
|
Rattus norvegicus
|
489.78
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membrane
|
Rattus norvegicus
|
69.0
nM
|
|
Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR1 expressed in Sf9 cells
|
Rattus norvegicus
|
169.0
nM
|
|
Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR2(R) expressed in Sf9 cells
|
Rattus norvegicus
|
282.0
nM
|
|
Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR3 expressed in Sf9 cells
|
Rattus norvegicus
|
249.0
nM
|
|
Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR4 expressed in Sf9 cells
|
Rattus norvegicus
|
354.0
nM
|
|
Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cells
|
Rattus norvegicus
|
140.0
nM
|
|
Displacement of [3H]kainic acid from rat recombinant iGluR6(V,C,R) receptor expressed in Sf9 cells
|
Rattus norvegicus
|
332.0
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor in rat brain membranes
|
Rattus norvegicus
|
290.0
nM
|
|
Displacement of [3H]AMPA from AMPA receptor in rat brain membranes
|
Rattus norvegicus
|
170.0
nM
|
|
Displacement of [3H]kainic acid from kainate receptor in rat brain membranes
|
Rattus norvegicus
|
92.0
nM
|
|
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
|
Homo sapiens
|
570.0
nM
|
|
Displacement of [3H]AMPA from AMPA receptor in Sprague-Dawley rat brain membranes
|
Rattus norvegicus
|
340.0
nM
|
|
Displacement of [3H]KA from KA receptor in Sprague-Dawley rat brain membranes
|
Rattus norvegicus
|
380.0
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes
|
Rattus norvegicus
|
200.0
nM
|
|
Displacement of [3H]AMPA from rat iGluR2 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
280.0
nM
|
|
Displacement of [3H]AMPA from rat iGluR2 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
281.84
nM
|
|
Displacement of [3H]SYM2081 from rat iGluR5 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
140.0
nM
|
|
Displacement of [3H]SYM2081 from rat iGluR5 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
138.04
nM
|
|
Displacement of [3H]SYM2081 from rat iGluR6 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
330.0
nM
|
|
Displacement of [3H]SYM2081 from rat iGluR6 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
331.13
nM
|
|
Displacement of [3H]SYM2081 from rat iGluR7 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
490.0
nM
|
|
Displacement of [3H]SYM2081 from rat iGluR7 receptor expressed in Sf9 cells baculovirus system after 1 to 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
489.78
nM
|
|
Antagonist activity at NMDA receptor (unknwon origin)
|
Homo sapiens
|
70.0
nM
|
|
Binding affinity to full length rat GluA3
|
Rattus norvegicus
|
500.0
nM
|
|
Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluK3 receptor expressed in sf9 cells by liquid scintillation counting
|
Rattus norvegicus
|
494.0
nM
|
|
Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluKK2(VCR) receptor expressed in sf9 cells by liquid scintillation counting
|
Rattus norvegicus
|
331.0
nM
|
|
Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluKK1(Q)1b receptor expressed in sf9 cells by liquid scintillation counting
|
Rattus norvegicus
|
140.0
nM
|
|
Displacement of [3H]AMPA from full length recombinant rat GluKA2(R) receptor expressed in sf9 cells by liquid scintillation counting
|
Rattus norvegicus
|
282.0
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor in rat brain cortex after 60 mins by Packard TopCount microplate scintillator counting
|
Rattus norvegicus
|
200.0
nM
|
|
Displacement of [3H]KA from kainate receptor in rat brain cortex after 60 mins by Packard TopCount microplate scintillator counting
|
Rattus norvegicus
|
380.0
nM
|
|
Displacement of [3H]AMPA from AMPA receptor in rat brain cortex after 30 mins by Packard TopCount microplate scintillator counting
|
Rattus norvegicus
|
340.0
nM
|
|
Displacement of [3H]Kainic acid from kainate receptor in Wistar rat brain after 60 mins
|
Rattus norvegicus
|
170.0
nM
|
|
Displacement of [3H]Kainic acid from kainate receptor in Wistar rat brain after 60 mins
|
Rattus norvegicus
|
240.0
nM
|
|
Displacement of [3H]CGP 39653 from NMDA receptor agonist binding site in Wistar rat cerebral cortex after 20 mins
|
Rattus norvegicus
|
370.0
nM
|
|
Displacement of [3H]CGP 39653 from NMDA receptor agonist binding site in Wistar rat cerebral cortex after 20 mins
|
Rattus norvegicus
|
410.0
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor agonist binding site in Wistar rat cerebral cortex at 10 uM after 20 mins relative to control
|
Rattus norvegicus
|
10.0
%
|
|
Displacement of [3H]Kainic acid from kainate receptor in Wistar rat brain at 10 uM after 60 mins relative to control
|
Rattus norvegicus
|
0.0
%
|
|
Displacement of [3H]-AMPA from AMPA receptor in rat brain cortical membranes
|
Rattus norvegicus
|
340.0
nM
|
|
Displacement of [3H]-KA from kainate receptor in rat brain cortical membranes
|
Rattus norvegicus
|
380.0
nM
|
|
Displacement of [3H]CGP-39653 from NMDA receptor in rat brain cortical membranes
|
Rattus norvegicus
|
200.0
nM
|
|
Agonist activity at human mGluR3 receptor expressed in HEK cells
|
Homo sapiens
|
60.0
nM
|
|
Binding affinity to human mGluR3 receptor expressed in HEK cells
|
Homo sapiens
|
57.54
nM
|
|
Displacement of [3H]AMPA from AMPA receptor in rat cortical synaptosomes
|
Rattus norvegicus
|
340.0
nM
|
|
Displacement of [3H]KA from Kainate receptor in rat cortical synaptosomes
|
Rattus norvegicus
|
380.0
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor in rat cortical synaptosomes
|
Rattus norvegicus
|
200.0
nM
|
|
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
|
Rattus norvegicus
|
57.54
nM
|
|
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
|
Rattus norvegicus
|
60.0
nM
|
|
Cis-inhibition of human LAT1 expressed in TREx HEK293 cells at 200 uM assessed as inhibition of [3H]-gabapentin uptake at 200 uM preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis relative to BCH
|
Homo sapiens
|
-2.4
%
|
|
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
|
4.15
%
|
|
Displacement of [3H]AMPA from AMPA receptor in rat brain synaptic cortical membranes after 30 mins by scintillation counting method
|
Rattus norvegicus
|
340.0
nM
|
|
Displacement of [3H]KA from KA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method
|
Rattus norvegicus
|
380.0
nM
|
|
Displacement of [3H]CGP39653 from NMDA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method
|
Rattus norvegicus
|
200.0
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
|
8.67
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
12.78
%
|
|
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
|
-0.04
%
|
|
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
|
-0.11
%
|
|
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
|
-0.11
%
|
|
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
|
-0.04
%
|
|
Displacement of [3H]CPP from rat brain cortical membranes NMDA receptor incubated for 30 mins by equilibrium binding assay
|
Rattus norvegicus
|
200.0
nM
|
|
Displacement of [3H]AMPA from rat brain cortical membranes AMPA receptor incubated for 30 mins by equilibrium binding assay
|
Rattus norvegicus
|
600.0
nM
|
|
Displacement of [3H]KA from rat brain cortical membranes Kainate receptor incubated for 30 mins by equilibrium binding assay
|
Rattus norvegicus
|
250.0
nM
|
|