|
Mammalian cell cytotoxicity test in chinese hamster V79 cells (clonogenic cytotoxicity)
|
None
|
500.0
ug.mL-1
|
|
|
Inhibitory effect on DNA gyrase supercoiling activity from Escherichia coli K-12 C600
|
Escherichia coli
|
0.59
ug.mL-1
|
|
|
Inhibition of DNA gyrase supercoiling in Escherichia coli.
|
Escherichia coli
|
1.8
ug.mL-1
|
|
|
Tested for inhibitory activity against DNA gyrase supercoiling in Escherichia coli (KL-16)
|
Escherichia coli
|
0.53
ug.mL-1
|
|
|
Minimum concentration of the drug needed to produce linear DNA at an intensity relative to oxolinic acid(at 10 ug/mL)
|
Escherichia coli
|
2.25
ug.mL-1
|
|
|
Inhibitory concentration in supercoiling inhibition Escherichia coli DNA gyrase assay
|
Escherichia coli
|
6.3
ug.mL-1
|
|
|
50% inhibitory concentration against DNA-gyrase
|
Escherichia coli
|
7.5
ug.mL-1
|
|
|
Gyrase inhibitory activity against Escherichia coli
|
Escherichia coli
|
1.0
ug.mL-1
|
|
|
In vitro antibacterial activity was determined as inhibitory concentration causing 50% DNA-gyrase supercoiling inhibition (SCI)
|
Escherichia coli
|
1.75
ug.mL-1
|
|
|
Inhibition constant against DNA Gyrase isolated from Escherichia coli
|
Escherichia coli
|
1.6
ug ml-1
|
|
|
Inhibition constant against DNA Gyrase isolated from Micrococcus luteus
|
Micrococcus luteus
|
84.0
ug ml-1
|
|
|
Inhibition of Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as inhibition of pBR322 DNA supercoiling
|
Mycobacterium leprae
|
10.0
ug.mL-1
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
21.1
%
|
|
|
Inhibition of Mycobacterium leprae wild type DNA gyrase A2B2 assessed as DNA supercoiling inhibition
|
Mycobacterium leprae
|
15.0
ug.mL-1
|
|
|
Inhibition of Mycobacterium leprae DNA gyrase subunit A G89C mutant assessed as DNA supercoiling inhibition
|
Mycobacterium leprae
|
160.0
ug.mL-1
|
|
|
Inhibition of Mycobacterium leprae DNA gyrase subunit A A91V mutant assessed as DNA supercoiling inhibition
|
Mycobacterium leprae
|
80.0
ug.mL-1
|
|
|
Inhibition of Mycobacterium leprae wild type DNA gyrase subunit B D205N mutant assessed as DNA supercoiling inhibition
|
Mycobacterium leprae
|
20.0
ug.mL-1
|
|
|
Antimicrobial activity against Escherichia coli harboring DNA gyrase GyrA QRDR
|
Escherichia coli
|
0.3
ug.mL-1
|
|
|
Antimicrobial activity against Pseudomonas aeruginosa harboring DNA gyrase GyrA QRDR
|
Pseudomonas aeruginosa
|
0.5
ug.mL-1
|
|
|
Antimicrobial activity against Staphylococcus aureus harboring DNA gyrase GyrA QRDR
|
Staphylococcus aureus
|
10.0
ug.mL-1
|
|
|
Antimicrobial activity against Streptococcus pneumoniae harboring DNA gyrase GyrA QRDR
|
Streptococcus pneumoniae
|
40.0
ug.mL-1
|
|
|
Antimicrobial activity against Mycobacterium smegmatis harboring DNA gyrase GyrA QRDR
|
Mycobacterium smegmatis
|
10.0
ug.mL-1
|
|
|
Antimicrobial activity against Mycobacterium tuberculosis harboring DNA gyrase GyrA QRDR
|
Mycobacterium tuberculosis
|
10.0
ug.mL-1
|
|
|
Antimicrobial activity against Mycobacterium fortuitum harboring DNA gyrase GyrA QRDR
|
Mycobacterium fortuitum
|
1.0
ug.mL-1
|
|
|
Antimicrobial activity against Escherichia coli harboring DNA gyrase GyrB QRDR
|
Escherichia coli
|
0.3
ug.mL-1
|
|
|
Antimicrobial activity against Pseudomonas aeruginosa harboring DNA gyrase GyrB QRDR
|
Pseudomonas aeruginosa
|
0.5
ug.mL-1
|
|
|
Antimicrobial activity against Staphylococcus aureus harboring DNA gyrase GyrB QRDR
|
Staphylococcus aureus
|
10.0
ug.mL-1
|
|
|
Antimicrobial activity against Streptococcus pneumoniae harboring DNA gyrase GyrB QRDR
|
Streptococcus pneumoniae
|
40.0
ug.mL-1
|
|
|
Antimicrobial activity against Mycobacterium smegmatis harboring DNA gyrase GyrB QRDR
|
Mycobacterium smegmatis
|
10.0
ug.mL-1
|
|
|
Antimicrobial activity against Mycobacterium tuberculosis harboring DNA gyrase GyrB QRDR
|
Mycobacterium tuberculosis
|
10.0
ug.mL-1
|
|
|
Antimicrobial activity against Mycobacterium fortuitum harboring DNA gyrase GyrB QRDR
|
Mycobacterium fortuitum
|
1.0
ug.mL-1
|
|
|
PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhimurium using a modified counterscreen. (Class of assay: confirmatory) [Related pubchem assays: 2253, 1863, 1874 ]
|
None
|
560.0
nM
|
|
|
PUBCHEM_BIOASSAY: A Counter Screen to identiry small molecule screen for inhibitors of the PhoP region in Salmonella Typhimurium. (Class of assay: confirmatory) [Related pubchem assays: 2253, 1863, 1981, 1874 ]
|
None
|
800.0
nM
|
|
|
PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in Salmonella Typhimurium. (Class of assay: confirmatory) [Related pubchem assays: 2253, 1981, 1874 ]
|
None
|
390.0
nM
|
|
|
PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in Salmonella typhi. (Class of assay: confirmatory) [Related pubchem assays: 1864, 2252, 1985 ]
|
None
|
310.0
nM
|
|
|
PUBCHEM_BIOASSAY: A screen for inhibitors of the PhoP region in Salmonella Typhi using a modified counterscreen. (Class of assay: confirmatory)
|
None
|
230.0
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
|
-8.2
%
|
|
|
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
|
24.5
%
|
|
|
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
|
18.4
%
|
|
|
Antitubercular activity against Mycobacterium tuberculosis
|
Mycobacterium tuberculosis
|
0.5
ug.mL-1
|
|
|
Inhibition of Mycobacterium leprae DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 2 hrs at 30 degC by ethidium bromide based gel electrophoresis
|
Mycobacterium leprae
|
8.0
ug.mL-1
|
|
|
Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 1 hr at 37 degC by ethidium bromide based gel electrophoresis
|
Mycobacterium tuberculosis
|
6.0
ug.mL-1
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
65.85
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
89.51
%
|
|
|
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
|
666.0
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
|
-5.24
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
12.52
%
|
|
|
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
|
0.25
%
|
|
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
|
0.25
%
|
|
