|
Inhibition of human recombinant MAOA before repeated washing at 500 uM
|
Homo sapiens
|
86.75
%
|
|
|
Inhibition of human recombinant MAOA after washing at 500 uM by centrifugation-ultrafiltration method
|
Homo sapiens
|
10.26
%
|
|
|
Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM
|
Homo sapiens
|
50.0
%
|
|
|
NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay
|
Plasmodium falciparum
|
740.0
nM
|
|
|
Competitive inhibition of MAOA in rat liver homogenate by spectrophotometrically
|
Rattus norvegicus
|
5.53
nM
|
|
|
Inhibition of MAO-A in rat liver homogenate by spectrophotometry-based Holt method
|
Rattus norvegicus
|
5.0
nM
|
|
|
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells at 500 uM before washing by centrifugation-ultrafiltration method
|
Homo sapiens
|
84.75
%
|
|
|
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells at 500 uM after repeated washing by centrifugation-ultrafiltration method
|
Homo sapiens
|
10.26
%
|
|
|
Inhibition of human MAOA at 500 uM
|
Homo sapiens
|
86.75
%
|
|
|
Reversible inhibition of human MAOA at 500 uM by centrifugation-ultrafiltration method
|
Homo sapiens
|
10.26
%
|
|
|
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine at 500 uM after 15 mins
|
Homo sapiens
|
86.75
%
|
|
|
Irreversible inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine at 500 uM measured after repeated washing by centrifugation-ultrafiltration method
|
Homo sapiens
|
10.26
%
|
|
|
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production at 500 uM by fluorimetric method
|
Homo sapiens
|
85.98
%
|
|
|
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production at 500 uM measured after repeated washing by fluorimetric method
|
Homo sapiens
|
11.45
%
|
|
|
Inhibition of human MAO-A expressed in BTI insect cells using p-tyramine as substrate after 60 mins
|
Homo sapiens
|
5.0
nM
|
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
Homo sapiens
|
1.7
%
|
|
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
-3.3
%
|
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
27.5
%
|
|
|
Inhibition of MAO-B in Sprague-Dawley rat brain mitochondrial suspension using kynuramine as substrate at 10 uM incubated for 5 mins prior to substrate addition measured for 5 mins by spectrophotometry
|
Rattus norvegicus
|
0.0
%
|
|
|
Reversible inhibition of human recombinant MAO-A expressed in baculovirus infected BT1 insect cells at 300 nM incubated for 1 hr followed by compound washout by centrifugation-ultrafiltration method
|
Homo sapiens
|
9.56
%
|
|
|
Reversible inhibition of human recombinant MAO-A expressed in baculovirus infected BT1 insect cells at 300 nM after 1 hr by centrifugation-ultrafiltration method
|
Homo sapiens
|
89.0
%
|
|
|
Competitive reversible inhibition of human recombinant MAO-A expressed in baculovirus infected BT1 insect cells using p-tyramine as substrate assessed as H2O2 production after 15 mins by fluorimetric analysis
|
Homo sapiens
|
5.0
nM
|
|
|
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells using p-tyramine substrate assessed as reduction in H2O2 production
|
Homo sapiens
|
361.38
nM
|
|
|
Inhibition of human MAOA expressed in baculovirus-infected BTI insect cells assessed as H2O2 production by resorufin dye based fluorimetric method
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of recombinant human MAO-A using p-tyramine as substrate assessed as H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins by amplex red assay
|
Homo sapiens
|
110.0
nM
|
|
|
Displacement of [3H](+)-pentazocine from S1R in human Jurkat cell membranes after 2 hrs by liquid scintillation counting
|
Homo sapiens
|
100.0
nM
|
|
|
Displacement of [3H]-DTG from S2R in human Jurkat cell membranes after 1 hr in presence of (+)-pentazocine by liquid scintillation counting
|
Homo sapiens
|
200.0
nM
|
|
|
Inhibition of recombinant human MAO-A assessed as reduction in H2O2 production preincubated for 30 mins followed by p-tyramine substrate addition measured after 30 mins by amplex red reagent based fluorescence assay
|
Homo sapiens
|
102.0
nM
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
3.95
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
0.74
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
9.06
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
7.86
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
4.07
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
3.1
%
|
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
-2.98
%
|
|
|
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
|
-1.36
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
13.94
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
3.102
%
|
|
|
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
|
-0.06
%
|
|
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
|
0.01
%
|
|
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
|
-0.06
%
|
|
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
|
0.01
%
|
|
|
Inhibition of human recombinant MAO-A at 1 mM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
95.3
%
|
|
|
Inhibition of human recombinant MAO-A at 100 uM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
83.14
%
|
|
|
Inhibition of human recombinant MAO-A at 10 uM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
62.44
%
|
|
|
Inhibition of human recombinant MAO-A at 1 uM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
35.76
%
|
|
|
Inhibition of human recombinant MAO-A at 0.1 uM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
24.47
%
|
|
|
Inhibition of human recombinant MAO-A at 0.01 uM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
19.64
%
|
|
|
Inhibition of human recombinant MAO-A at 1 nM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
15.42
%
|
|
|
Inhibition of human recombinant MAO-A at 0.1 nM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
12.85
%
|
|
|
Inhibition of human recombinant MAO-A at 0.01 nM using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method relative to control
|
Homo sapiens
|
7.251
%
|
|
|
Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis
|
Homo sapiens
|
100.0
nM
|
|
