|
Cell free inhibiting activity against Streptococcus pneumoniae 5635(Wild type ribosomes for transcription/translation assay)
|
Streptococcus pneumoniae
|
170.0
nM
|
|
|
Antimicrobial activity against Naegleria fowleri Lee (M67) at day 2
|
Naegleria fowleri
|
2.6
nM
|
|
|
Antimicrobial activity against Naegleria fowleri Lee (M67) at day 3
|
Naegleria fowleri
|
3.1
nM
|
|
|
Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs
|
Homo sapiens
|
25.0
ug.mL-1
|
|
|
Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs
|
Homo sapiens
|
160.0
ug.mL-1
|
|
|
Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs
|
Homo sapiens
|
190.0
ug.mL-1
|
|
|
Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs
|
Homo sapiens
|
180.0
ug.mL-1
|
|
|
Antiproliferative effect against HeLa cells after 48 hrs
|
Homo sapiens
|
240.0
ug.mL-1
|
|
|
Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs
|
Homo sapiens
|
160.0
ug.mL-1
|
|
|
Inhibition of Plasmodium falciparum in HRP2 ELISA
|
Plasmodium falciparum
|
2.57
ug.mL-1
|
|
|
Inhibition of Plasmodium falciparum AZ10011003 isolate in HRP2 ELISA
|
Plasmodium falciparum
|
2.444
ug.mL-1
|
|
|
Inhibition of Plasmodium falciparum AZ10011008 isolate in HRP2 ELISA
|
Plasmodium falciparum
|
5.342
ug.mL-1
|
|
|
Inhibition of Plasmodium falciparum AZ10011017 isolate in HRP2 ELISA
|
Plasmodium falciparum
|
1.976
ug.mL-1
|
|
|
Inhibition of Plasmodium falciparum AZ10011022 isolate in HRP2 ELISA
|
Plasmodium falciparum
|
2.19
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay
|
Plasmodium falciparum
|
10.13
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay
|
Plasmodium falciparum
|
1.623
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs by SYBR green fluorescence assay
|
Plasmodium falciparum
|
15.28
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green fluorescence assay
|
Plasmodium falciparum
|
2.734
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay
|
Plasmodium falciparum
|
10.07
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay
|
Plasmodium falciparum
|
1.848
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay
|
Plasmodium falciparum
|
14.36
ug.mL-1
|
|
|
In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay
|
Plasmodium falciparum
|
4.489
ug.mL-1
|
|
|
Antimalarial activity against Plasmodium falciparum D6 as reduced [3H]hypoxanthine uptake after 72 hrs
|
Plasmodium falciparum
|
3.747
ug.mL-1
|
|
|
Antimalarial activity against Plasmodium falciparum W2 as reduced [3H]hypoxanthine uptake after 72 hrs
|
Plasmodium falciparum
|
5.5
ug.mL-1
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum 7G8 C1 mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
141.8
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 C1 mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
95.7
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
103.4
nM
|
|
|
Antimalarial activity after 96hrs against Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
228.1
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
43.3
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 T76K1 mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
121.8
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum 7G8 T76K1 mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
114.8
nM
|
|
|
Antimalarial activity after 96hrs against Plasmodium falciparum GCO3 C2 mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
48.0
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 C4 mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
66.7
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 C6 mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
76.7
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 SDD mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
63.3
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 SND mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
47.8
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 CDY mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
70.2
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum 3BA6 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
180.3
nM
|
|
|
Antimalarial activity against Plasmodium falciparum 3BA6 SDD with CRT and MDR1 mutation after 96 hrs in [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
154.7
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum 3BA6 SND mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
157.9
nM
|
|
|
Antimalarial activity after 96 hrs against Plasmodium falciparum 3BA6 CDY mutant CRT/MDR1 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
194.2
nM
|
|
|
Antimalarial activity as 3rd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs dose then 48 hrs drug-free
|
Plasmodium falciparum 3D7
|
52.7
nM
|
|
|
Antimalarial activity as 3rd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs dose then 48 hrs drug-free
|
Plasmodium falciparum
|
31.0
nM
|
|
|
Inhibition of quorum sensing-regulated elastase production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 2 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
77.0
%
|
|
|
Inhibition of quorum sensing-regulated elastase production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 4 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
45.0
%
|
|
|
Inhibition of quorum sensing-regulated elastase production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 8 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
51.0
%
|
|
|
Inhibition of quorum sensing-regulated chitinase production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 2 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
66.0
%
|
|
|
Inhibition of quorum sensing-regulated chitinase production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 4 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
15.0
%
|
|
|
Inhibition of quorum sensing-regulated chitinase production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 8 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
10.0
%
|
|
|
Inhibition of quorum sensing-regulated pyocyanin production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 2 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
43.0
%
|
|
|
Inhibition of quorum sensing-regulated pyocyanin production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 4 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
32.0
%
|
|
|
Inhibition of quorum sensing-regulated pyocyanin production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 8 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
16.0
%
|
|
|
Inhibition of quorum sensing-regulated alginate production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 2 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
63.0
%
|
|
|
Inhibition of quorum sensing-regulated alginate production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 4 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
56.0
%
|
|
|
Inhibition of quorum sensing-regulated alginate production in Pseudomonas aeruginosa NH57388A mucoid isolate harboring GFP-fused avian sarcoma virus lasB gene assessed as enzyme activity per cell at 8 ug/mL after 24 hrs relative to control
|
Pseudomonas aeruginosa
|
52.0
%
|
|
|
Antiplasmodial activity after 96 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity
|
Plasmodium falciparum 3D7
|
940.0
nM
|
|
|
Antiplasmodial activity after 120 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity
|
Plasmodium falciparum 3D7
|
410.0
nM
|
|
|
Inhibition of Escherichia coli ribosome
|
Escherichia coli
|
300.0
nM
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 1 ug/ml by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
37.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 0.5 ug/ml by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
65.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 0.25 ug/ml by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
78.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 0.125 ug/ml by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
85.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in las1 and rhl1 deficient Pseudomonas aeruginosa TNP093 at 1 ug/ml after 9 hrs by Cat-2,3-diO reporter gene assay
|
Pseudomonas aeruginosa
|
100.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in rhl1 deficient Pseudomonas aeruginosa TNP092 at 1 ug/ml after 9 hrs by Cat-2,3-diO reporter gene assay
|
Pseudomonas aeruginosa
|
90.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in las1 deficient Pseudomonas aeruginosa TNP091 at 1 ug/ml after 9 hrs by Cat-2,3-diO reporter gene assay
|
Pseudomonas aeruginosa
|
99.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 1 ug/ml after 11.5 hrs by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
-63.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 1 ug/ml after 9.5 hrs by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
-70.2
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 1 ug/ml after 7.5 hrs by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
-73.0
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa TNP090 mutant harboring las and rhl gene at 1 ug/ml after 5.5 hrs by Cat-2,3-diO reporter gene assay relative to untreated control
|
Pseudomonas aeruginosa
|
-30.9
%
|
|
|
Inhibition of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa at 1.0 ug/ml
|
Pseudomonas aeruginosa
|
70.0
%
|
|
|
PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Response HTS to Identify Compounds Cytotoxic to Streptococcus. (Class of assay: confirmatory) [Related pubchem assays: 1900 (Counter Screen), 1677 (Project Summary), 1902 (Retest at Dose), 1662 (Primary HTS)]
|
Streptococcus
|
66.0
nM
|
|
|
PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Identify Compounds Cytotoxic to SK(-)GAS Group A Streptococcus. (Class of assay: confirmatory) [Related pubchem assays: 1677 (Project Summary), 1662 (Primary HTS)]
|
Streptococcus
|
60.0
nM
|
|
|
PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Identify Inhibitors of Streptokinase Promotor Activity. (Class of assay: confirmatory) [Related pubchem assays: 1677 (Project Summary), 1662 (Primary HTS)]
|
Streptococcus pyogenes M1 GAS
|
60.0
nM
|
|
|
Bactericidal activity against Streptococcus pyogenes VT 59 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs
|
Streptococcus pyogenes
|
20.0
%
|
|
|
Bactericidal activity against Klebsiella pneumoniae VT 1367 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs
|
Klebsiella pneumoniae
|
20.0
%
|
|
|
Bactericidal activity against Escherichia coli ATCC 25922 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs
|
Escherichia coli
|
20.0
%
|
|
|
Bactericidal activity against Pseudomonas aeruginosa ATCC 27853 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs
|
Pseudomonas aeruginosa
|
20.0
%
|
|
|
Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 assessed as decrease of CFU after 24 hrs
|
Staphylococcus aureus
|
0.12
ug.mL-1
|
|
|
Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 infected in human THP1 cells assessed as decrease of CFU after 24 hrs
|
Staphylococcus aureus
|
0.024
ug.mL-1
|
|
|
Antibacterial activity against methicillin-sensitive Listeria monocytogenes EGD assessed as decrease of CFU after 24 hrs
|
Listeria monocytogenes EGD-e
|
2.66
ug.mL-1
|
|
|
Antibacterial activity against methicillin-sensitive Listeria monocytogenes EGD infected in human THP1 cells assessed as decrease of CFU after 24 hrs
|
Listeria monocytogenes EGD-e
|
2.86
ug.mL-1
|
|
|
Inhibition of quorum sensing activity in Pseudomonas aeruginosa ATCC 27853 assessed as N-acylhomoserin lactones production at 5 ug/ml after 24 hrs by measuring beta-galactosidase activity by spectrophotometry
|
Pseudomonas aeruginosa
|
76.0
%
|
|
|
Antiparasitic activity against yellow fluorescent protein expressing Toxoplasma gondii 2F-1 treated immediately after infection for 48 hrs followed by reinoculated into fresh HFF monolayers measured after 48 hrs
|
Toxoplasma gondii
|
600.0
nM
|
|
|
Antiparasitic activity against yellow fluorescent protein expressing Toxoplasma gondii 2F-1 treated 6 hrs after infection for 42 hrs followed by reinoculated into fresh HFF monolayers measured after 48 hrs
|
Toxoplasma gondii
|
600.0
nM
|
|
|
Antimalarial activity against Plasmodium falciparum after 68 hrs
|
Plasmodium falciparum
|
0.5
ug.mL-1
|
|
|
Antiinflammatory activity in mouse splenocytes assessed as inhibition of LPS-induced IL-6 production at 50 uM preincubated for 2 hrs prior to LPS challenge by sandwich ELISA
|
Mus musculus
|
84.0
%
|
|
|
Antiinflammatory activity in mouse splenocytes assessed as inhibition of LPS-induced IL-6 production in mouse splenocytes at 25 uM preincubated for 2 hrs prior to LPS challenge by sandwich ELISA
|
Mus musculus
|
74.0
%
|
|
|
Antiinflammatory activity in mouse splenocytes assessed as inhibition of LPS-induced IL-6 production at 12 uM preincubated for 2 hrs prior to LPS challenge by sandwich ELISA
|
Mus musculus
|
61.0
%
|
|
|
Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products at 500 uM preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method relative to control
|
Homo sapiens
|
99.0
%
|
|
|
Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products at 500 uM preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method relative to control
|
Homo sapiens
|
68.0
%
|
|
|
Inhibition of ribosome nascent peptide exit tunnel in Escherichia coli S30 extract assessed as inhibition of prokaryotic translation in presence of amino acids incubated for 20 mins by luciferase reporter gene assay
|
Escherichia coli
|
292.0
nM
|
|
|
Antichlamydial activity against Chlamydia trachomatis serovar L2 infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay
|
Chlamydia trachomatis
|
727.0
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
|
-1.27
%
|
|
|
Antimalarial activity against Plasmodium falciparum 3D7 after 96 hrs
|
Plasmodium falciparum
|
53.0
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
|
-2.537
%
|
|
|
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
|
-0.08
%
|
|
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
|
-0.08
%
|
|
|
Inhibition of quorum sensing system in Chromobacterium violaceum ATCC 31532 assessed as reduction in violacein production at 400 uM relative to control
|
Chromobacterium violaceum
|
90.6
%
|
|
|
Inhibition of quorum sensing in Chromobacterium violaceum ATCC 31532 assessed as reduction in violacein production at 40 uM relative to control
|
Chromobacterium violaceum
|
90.6
%
|
|
|
Inhibition of mitochondrial COX1 expression in human GFP-labelled MDA-MB-231 cells at 30 uM incubated for 72 hrs under low oxygen condition by Western blot analysis
|
Homo sapiens
|
30.0
%
|
|
