|
In vitro effective concentration towards human motilin receptor
|
None
|
400.0
nM
|
|
|
Compound was tested for in vitro motilin receptor binding affinity
|
None
|
43.65
nM
|
|
|
Compound was tested for in vitro motilin receptor binding affinity after treatment with hydrochloric acid solution (pH 2.5)
|
None
|
70.79
nM
|
|
|
Inhibition of N-acetylphenylalanine-tRNA peptide bond formation by fragment reaction at 10e-5 M
|
None
|
0.0
%
|
|
|
Inhibition of N-acetylphenylalanine-tRNA peptide bond formation by puromycin reaction at 10E-5 M
|
None
|
3.0
%
|
|
|
Inhibition of N-acetylphenylalanine-tRNA peptide bond formation by puromycin reaction at 10E-6 M
|
None
|
0.0
%
|
|
|
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells
|
None
|
1.0
%
|
|
|
Compound was tested for the in vitro smooth muscle contractile activity
|
Oryctolagus cuniculus
|
316.23
nM
|
|
|
Cell free inhibiting activity against erythromycin-susceptible strain Streptococcus pneumoniae 5635 (Wild type ribosomes for transcription/translation assay)
|
Streptococcus pneumoniae
|
120.0
nM
|
|
|
Inhibition of ribosome function in a coupled transcription and translational assay using Escherichia coli S30 extracts
|
Escherichia coli
|
80.0
nM
|
|
|
Inhibition of protein synthesis in Escherichia coli cell-free translational system
|
Escherichia coli
|
900.0
nM
|
|
|
Antiinflammatory activity in topically dosed CD1 mouse assessed as inhibition of PMA-induced ear edema at 0.5 mg/ear
|
Mus musculus
|
42.0
%
|
|
|
Inhibition of LPS-induced TNFalpha release in human PBMC at 10 uM relative to Dexamethasone
|
Homo sapiens
|
22.0
%
|
|
|
Inhibition of LPS-induced IL1-beta release in human PBMC at 10 uM relative to cyclohexane
|
Homo sapiens
|
-32.0
%
|
|
|
Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs
|
Homo sapiens
|
180.0
ug.mL-1
|
|
|
Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs
|
Homo sapiens
|
400.0
ug.mL-1
|
|
|
Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs
|
Homo sapiens
|
300.0
ug.mL-1
|
|
|
Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs
|
Homo sapiens
|
310.0
ug.mL-1
|
|
|
Antiproliferative effect against HeLa cells after 48 hrs
|
Homo sapiens
|
400.0
ug.mL-1
|
|
|
Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs
|
Homo sapiens
|
170.0
ug.mL-1
|
|
|
Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assay
|
Homo sapiens
|
50.12
nM
|
|
|
Inhibition of human CYP3A4 expressed in Escherichia coli using diethoxyfluorescein substrate measured in 25 to 30 mins by time dependent inhibition assay
|
Homo sapiens
|
190.0
nM
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
14.0
%
|
|
|
Agonist activity at human recombinant motilin receptor expressed in HEK293 cells by FLIPR assay
|
Homo sapiens
|
630.96
nM
|
|
|
Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay
|
Homo sapiens
|
50.12
nM
|
|
|
Displacement of [14C]ERY from erythromycin-sensitive Escherichia coli BL21 ribosome
|
Escherichia coli BL21
|
11.0
nM
|
|
|
Displacement of [14C]ERY from erythromycin-sensitive Propionibacterium acnes EG7NS ribosome
|
Propionibacterium acnes
|
29.0
nM
|
|
|
Inhibition of ribosomal activity in erythromycin-sensitive Escherichia coli BL21 assessed as luciferase production by transcriptional and translational assay
|
Escherichia coli BL21
|
760.0
nM
|
|
|
Inhibition of ribosomal activity in erythromycin-sensitive Propionibacterium acnes EG7NS assessed as luciferase production by transcriptional and translational assay
|
Propionibacterium acnes
|
170.0
nM
|
|
|
Inhibition of ribosomal activity in erythromycin-resistant Propionibacterium acnes GE4E carrying Erm(X) gene assessed as luciferase production by transcriptional and translational assay
|
Propionibacterium acnes
|
52.0
%
|
|
|
Inhibition of human ERG expressed in HEK cells at 30 uM
|
Homo sapiens
|
27.0
%
|
|
|
Inhibition of human ERG expressed in HEK cells at 300 uM
|
Homo sapiens
|
90.0
%
|
|
|
Inhibition of human ERG expressed in HEK cells
|
Homo sapiens
|
39.0
nM
|
|
|
Inhibition of human ERG expressed in HEK cells at 30 uM
|
Homo sapiens
|
50.0
%
|
|
|
Inhibition of human ERG at 30 uM
|
Homo sapiens
|
27.0
%
|
|
|
Inhibition of human ERG at 300 uM
|
Homo sapiens
|
90.0
%
|
|
|
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
|
60.0
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
|
|
|
Inhibition of ribosomal subunit assembly in Escherichia coli assessed as reduction in mature 23S rRNA at 100 ug/ml
|
Escherichia coli
|
30.0
%
|
|
|
Inhibition of ribosomal subunit assembly in Escherichia coli assessed as reduction in mature 23S rRNA at 100 ug/ml in presence of E-peptide
|
Escherichia coli
|
60.0
%
|
|
|
Inhibition of ribosomal subunit assembly in Escherichia coli assessed as reduction in mature 23S rRNA at 7 ug/ml in presence of E-peptide
|
Escherichia coli
|
60.0
%
|
|
|
Displacement of [14C]-erythromycin from Escherichia coli K-12 70S ribosome after 10 mins by competitive binding assay
|
Escherichia coli K-12
|
15.0
nM
|
|
|
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM, Erythromycin: 100 uM) in Caco-2 cells
|
None
|
101.0
%
|
|
|
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
|
58.8
%
|
|
|
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
|
45.8
%
|
|
|
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
|
-19.0
%
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
7.0
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
75.85
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
92.42
%
|
|
|
Antibiofilm activity against Klebsiella planticola MTCC 530 after 24 hrs by crystal violet assay
|
Raoultella planticola
|
0.19
ug.mL-1
|
|
|
Antibiofilm activity against Staphylococcus aureus MLS-16 MTCC 2940 after 24 hrs by crystal violet assay
|
Staphylococcus aureus
|
0.21
ug.mL-1
|
|
|
Antibiofilm activity against Staphylococcus aureus MTCC 96 after 24 hrs by crystal violet assay
|
Staphylococcus aureus
|
0.25
ug.mL-1
|
|
|
Displacement of [14C]erythromycin from Escherichia coli ribosomes after 30 mins by scintillation spectrometer analysis
|
Escherichia coli
|
750.0
nM
|
|
|
Antimicrobial activity against Micrococcus luteus MTCC 2470 assessed as inhibition of biofilm formation after 24 hrs by crystal violet staining-based assay
|
Micrococcus luteus
|
0.24
ug.mL-1
|
|
|
Antimicrobial activity against Staphylococcus aureus MTCC 96 assessed as inhibition of biofilm formation after 24 hrs by crystal violet staining-based assay
|
Staphylococcus aureus
|
0.32
ug.mL-1
|
|
|
Antimicrobial activity against Staphylococcus aureus MLS-16 MTCC 2940 assessed as inhibition of biofilm formation after 24 hrs by crystal violet staining-based assay
|
Staphylococcus aureus
|
0.32
ug.mL-1
|
|
|
Antimicrobial activity against Klebsiella planticola MTCC 530 assessed as inhibition of biofilm formation after 24 hrs by crystal violet staining-based assay
|
Raoultella planticola
|
0.21
ug.mL-1
|
|
|
Antimicrobial activity against Pseudomonas aeruginosa MTCC 2453 assessed as inhibition of biofilm formation after 24 hrs by crystal violet staining-based assay
|
Pseudomonas aeruginosa
|
0.26
ug.mL-1
|
|
|
Antibacterial activity against Pseudomonas aeruginosa assessed as growth inhibition after 24 hrs by microplate reader analysis
|
Pseudomonas aeruginosa
|
33.2
ug.mL-1
|
|
|
Antibiofilm activity against Pseudomonas aeruginosa at 50 ug/ml after 24 hrs by microplate reader analysis
|
Pseudomonas aeruginosa
|
45.7
%
|
|
|
Antimicrobial activity against Staphylococcus aureus MLS-16 MTCC 2940 assessed as inhibition of biofilm formation after 24 hrs
|
Staphylococcus aureus
|
0.23
ug.mL-1
|
|
|
Antimicrobial activity against Bacillus subtilis MTCC 121 assessed as inhibition of biofilm formation after 24 hrs
|
Bacillus subtilis
|
0.19
ug.mL-1
|
|
|
Antimicrobial activity against Escherichia coli MTCC 739 assessed as inhibition of biofilm formation after 24 hrs
|
Escherichia coli
|
0.31
ug.mL-1
|
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
45.0
%
|
|
|
Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Inhibition of bio-film formation of Micrococcus luteus MTCC 2470 incubated for 24 hrs at 37 degC under static conditions by crystal violet staining method
|
Micrococcus luteus
|
310.0
nM
|
|
|
Inhibition of bio-film formation of Staphylococcus aureus MLS16 MTCC 2940 incubated for 24 hrs at 37 degC under static conditions by crystal violet staining method
|
Staphylococcus aureus
|
250.0
nM
|
|
|
Inhibition of bio-film formation of Bacillus subtilis MTCC 121 incubated for 24 hrs at 37 degC under static conditions by crystal violet staining method
|
Bacillus subtilis
|
420.0
nM
|
|
|
Inhibition of bio-film formation of Escherichia coli MTCC 739 incubated for 24 hrs at 37 degC under static conditions by crystal violet staining method
|
Escherichia coli
|
430.0
nM
|
|
|
Inhibition of bio-film formation of Klebsiella planticola MTCC 530 incubated for 24 hrs at 37 degC under static conditions by crystal violet staining method
|
Raoultella planticola
|
350.0
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
|
-5.62
%
|
|
|
Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis relative to untreated control
|
Escherichia coli
|
99.0
%
|
|
|
Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity after 45 mins by Fe(SCN)3 dye based spectrometric analysis relative to untreated control
|
Escherichia coli
|
101.0
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
3.28
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
21.16
%
|
|
|
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
|
0.0
%
|
|
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
|
-0.22
%
|
|
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
|
-0.22
%
|
|
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
|
0.0
%
|
|
|
Antibacterial activity against Streptococcus pneumoniae ATCC 49617
|
Streptococcus pneumoniae
|
51.0
nM
|
|
|
Antibacterial activity against Streptococcus pneumoniae ATCC BAA1663
|
Streptococcus pneumoniae
|
37.0
nM
|
|
