The compound was tested for inhibitory activity against Aldose reductase from human placenta
|
None
|
500.0
nM
|
|
Inhibitory concentration against Bcl-xl
|
Homo sapiens
|
500.0
nM
|
|
Displacement of FAM-Bid from human Bcl2 by FP assay
|
Homo sapiens
|
320.0
nM
|
|
Binding affinity to human Bcl2 by ELISA
|
Homo sapiens
|
500.0
nM
|
|
Displacement of FAM-Bak from human Bcl-xL by FP assay
|
Homo sapiens
|
480.0
nM
|
|
Displacement of FAM-Bid from human Mcl1 by FP assay
|
Homo sapiens
|
180.0
nM
|
|
Displacement of FAM-Bim peptide from human Bcl2 by fluorescence polarization assay
|
Homo sapiens
|
170.0
nM
|
|
Displacement of FAM-Bim peptide from human Mcl1 by fluorescence polarization assay
|
Homo sapiens
|
280.0
nM
|
|
Binding affinity to BCL2
|
None
|
467.74
nM
|
|
Cytotoxicity against human HeLa cells by SRB assay
|
Homo sapiens
|
0.08
ug.mL-1
|
|
Cytotoxicity against human HT29 cells by SRB assay
|
Homo sapiens
|
5.0
ug.mL-1
|
|
Cytotoxicity against human KB cells by SRB assay
|
Homo sapiens
|
0.04
ug.mL-1
|
|
Inhibition of Bcl-xL
|
None
|
480.0
nM
|
|
Displacement of FITC-labeled Bak BH3 peptide from Bcl-XL after 30 mins by fluorescence polarization assay
|
None
|
540.0
nM
|
|
Displacement of FITC-labeled Bak BH3 peptide from Bcl-XL after 30 mins by fluorescence polarization assay
|
None
|
480.0
nM
|
|
Displacement of FITC-labeled Bak BH3 peptide from Bcl-2 after 30 mins by fluorescence polarization assay
|
None
|
300.0
nM
|
|
Displacement of FITC-labeled Bak BH3 peptide from Bcl-2 after 30 mins by fluorescence polarization assay
|
None
|
260.0
nM
|
|
Binding affinity to Bcl-xl
|
None
|
480.0
nM
|
|
Binding affinity to BCl2
|
None
|
320.0
nM
|
|
Binding affinity to MCL1
|
None
|
180.0
nM
|
|
Inhibition of HIV1 reverse transcriptase activity at 20 ug/ml
|
Human immunodeficiency virus 1
|
73.2
%
|
|
Inhibition of HIV1 reverse transcriptase activity at 4 ug/ml
|
Human immunodeficiency virus 1
|
76.3
%
|
|
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
|
Homo sapiens
|
10.16
ug.mL-1
|
|
Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
|
Homo sapiens
|
6.71
ug.mL-1
|
|
Antiproliferative activity against mouse B16/F10 cells after 48 hrs by MTT assay
|
Mus musculus
|
5.56
ug.mL-1
|
|
Inhibition of FAM-Bak-BH3 binding to human N-terminal His6-tagged Bcl2 isoform 2 after 4 hrs by fluorescence polarization assay
|
Homo sapiens
|
334.0
nM
|
|
Inhibition of electric eel AChE at 2 mg/ml by Ellman's method
|
Electrophorus electricus
|
-12.38
%
|
|
Inhibition of horse BChE at 2 mg/ml by Ellman's method
|
Equus caballus
|
-2.11
%
|
|
Antiamoebic activity against Entamoeba histolytica
|
Entamoeba histolytica
|
0.00777
ug.mL-1
|
|
Inhibition of biotin-Bim peptide binding to Mcl1 (unknown origin) expressed in Escherichia coli BL21 by ELISA
|
Homo sapiens
|
213.8
nM
|
|
Inhibition of biotin-Bim peptide binding to Mcl1 (unknown origin) expressed in Escherichia coli BL21 by ELISA
|
Homo sapiens
|
170.0
nM
|
|
Inhibition of FAM-Bid peptide binding to Mcl1 (unknown origin) expressed in Escherichia coli BL21 by fluorescence polarization-based binding assay
|
Homo sapiens
|
190.0
nM
|
|
Displacement of FAM-Bid BH3 peptide from recombinant Bcl-2 (unknown origin) expressed in Escherichia coli BL21 after 10 mins by fluorescence polarization assay
|
Homo sapiens
|
558.0
nM
|
|
Displacement of FAM-Bid BH3 peptide from recombinant Mcl-1 (unknown origin) expressed in Escherichia coli BL21 after 10 mins by fluorescence polarization assay
|
Homo sapiens
|
190.0
nM
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
24.45
%
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
68.48
%
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
58.3
%
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
15.81
%
|
|
Inhibition of Bcl-2 (unknown origin) using 5-FAM-Bid-BH3 as substrate preincubated for 30 mins before substrate addition measured after 20 mins by fluorescence polarization technique
|
Homo sapiens
|
620.0
nM
|
|
PubChem BioAssay. SW480 viability from Cell TiterGlo-IC50. (Class of assay: confirmatory)
|
None
|
956.3
nM
|
|
PubChem BioAssay. RKO viability from Cell TiterGlo-IC50. (Class of assay: confirmatory)
|
None
|
915.6
nM
|
|
PubChem BioAssay. HCT116 viability from Cell TiterGlo-IC50. (Class of assay: confirmatory)
|
None
|
784.4
nM
|
|
PubChem BioAssay. SNU-C1 viability from Cell TiterGlo-IC50. (Class of assay: confirmatory)
|
None
|
353.8
nM
|
|
PubChem BioAssay. DLD-1 viability from Cell TiterGlo-IC50. (Class of assay: confirmatory)
|
None
|
834.5
nM
|
|
Inhibition of Bcl-xL (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
640.0
nM
|
|
Inhibition of Mcl-1 (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
310.0
nM
|
|
Competitive binding affinity to Mcl-1 (unknown origin) using 5-FAM-Bid-BH3 peptide preincubated for 30 mins before 5-FAM-Bid-BH3 peptide addition and measured 20 mins after 5-FAM-Bid-BH3 peptide addition by fluorescence polarization assay
|
Homo sapiens
|
390.0
nM
|
|
Competitive binding affinity to Bcl-XL (unknown origin) using 5-FAM-Bid-BH3 peptide preincubated for 30 mins before 5-FAM-Bid-BH3 peptide addition and measured 20 mins after 5-FAM-Bid-BH3 peptide addition by fluorescence polarization assayy
|
Homo sapiens
|
770.0
nM
|
|
Competitive binding affinity to Bcl-2 (unknown origin) using 5-FAM-Bid-BH3 peptide preincubated for 30 mins before 5-FAM-Bid-BH3 peptide addition and measured 20 mins after 5-FAM-Bid-BH3 peptide addition by fluorescence polarization assay
|
Homo sapiens
|
560.0
nM
|
|
Displacement of FAM-Bid peptide from N-terminal 8x His-tagged MCl-1 (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay
|
Homo sapiens
|
260.0
nM
|
|
Displacement of FAM-Bid peptide from N-terminal 8x His-tagged Bcl-2 (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay
|
Homo sapiens
|
431.0
nM
|
|
Inhibition of Bcl-2 (unknown origin) using FAM-Bid peptide as substrate at 50 uM by fluorescence polarization-based assay
|
Homo sapiens
|
100.0
%
|
|
Inhibition of Bcl-2 (unknown origin) using FAM-Bid peptide as substrate by fluorescence polarization-based assay
|
Homo sapiens
|
440.0
nM
|
|
Inhibition of Bcl-XL (unknown origin) using FAM-Bid peptide as substrate at 50 uM by fluorescence polarization-based assay
|
Homo sapiens
|
100.0
%
|
|
Inhibition of Bcl-XL (unknown origin) using FAM-Bid peptide as substrate by fluorescence polarization-based assay
|
Homo sapiens
|
310.0
nM
|
|
Inhibition of 5-FAM-Bid peptide binding to Bcl-2 (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
440.0
nM
|
|
Inhibition of 5-FAM-Bid peptide binding to Bcl-XL (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
310.0
nM
|
|
Inhibition of 5-FAM-Bid peptide binding to MCL-1 (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
640.0
nM
|
|
Inhibition of FAM-Bid binding to human MCL1 expressed in Escherichia coli BL21 after 30 mins by fluorescence polarization assay
|
Homo sapiens
|
856.0
nM
|
|
Inhibition of FAM-Bid binding to human MCL1 expressed in Escherichia coli BL21 after 30 mins by fluorescence polarization assay
|
Homo sapiens
|
162.0
nM
|
|
Inhibition of FAM-Bid binding to human BCL2 expressed in Escherichia coli BL21 after 30 mins by fluorescence polarization assay
|
Homo sapiens
|
511.0
nM
|
|
Inhibition of 5-FAM-QEDIIRNIARHLAQVGDSMDRSIPPG binding to Mcl-1 (unknown origin) preincubated for 30 mins followed by FAM-labeled peptide addition measured after 20 mins by fluorescence polarization assay
|
Homo sapiens
|
180.0
nM
|
|
Inhibition of 5-FAM-QEDIIRNIARHLAQVGDSMDRSIPPG binding to Bcl-2 (unknown origin) preincubated for 30 mins followed by FAM-labeled peptide addition measured after 20 mins by fluorescence polarization assay
|
Homo sapiens
|
450.0
nM
|
|
Inhibition of biotinylated Bim peptide binding to His-tagged Bcl-2 (unknown origin) preincubated for 1 hr followed by biotinylated Bim peptide addition measured after 2 hrs by ELISA
|
Homo sapiens
|
600.0
nM
|
|
Inhibition of 6-carboxyfluorescein succinimidyl ester fluorescence tagged-Bid BH3 peptide (79 to 99 residues) binding to Bcl-2 (unknown origin) after 30 mins by fluorescence polarization assay
|
Homo sapiens
|
420.0
nM
|
|
Inhibition of 6-carboxyfluorescein succinimidyl ester fluorescence tagged-Bid BH3 peptide (79 to 99 residues) binding to Mcl-1 (unknown origin) after 30 mins by fluorescence polarization assay
|
Homo sapiens
|
200.0
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
|
66.34
%
|
|
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
|
97.0
%
|
|
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
|
93.0
%
|
|
Inhibition of Bcl2 (unknown origin)
|
Homo sapiens
|
320.0
nM
|
|
Inhibition of Bcl-xL (unknown origin)
|
Homo sapiens
|
480.0
nM
|
|
Inhibition of MCl-1 (unknown origin)
|
Homo sapiens
|
180.0
nM
|
|
Inhibition of Pseudomonas aeruginosa IMPDH at 35.1 uM using IMP as substrate in the presence of NAD+ incubated for 70 secs relative to control
|
Pseudomonas aeruginosa
|
100.0
%
|
|
Inhibition of Pseudomonas aeruginosa IMPDH using IMP as substrate in the presence of NAD+ incubated for 70 secs
|
Pseudomonas aeruginosa
|
900.0
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
|
15.02
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
8.739
%
|
|
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
|
7.89
%
|
|
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
|
6.48
%
|
|
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
|
6.48
%
|
|
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
|
7.89
%
|
|
Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) at 20uM using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis
|
Homo sapiens
|
101.2
%
|
|
Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis
|
Homo sapiens
|
250.0
nM
|
|
Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with high 200 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis
|
Homo sapiens
|
250.0
nM
|
|
Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and high 20 uM FAS incubated for 35 mins by MS analysis
|
Homo sapiens
|
260.0
nM
|
|
Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using high 10 uM hFX-CP as substrate mixture with 10 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis
|
Homo sapiens
|
330.0
nM
|
|
Displacement of FAM-Bid peptide from recombinant N-terminal His6x-tagged human Mcl-1 expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assay
|
Homo sapiens
|
190.0
nM
|
|
Inhibition of FAM-conjugated ssDNA binding to His-tagged wild type RAD52 (unknown origin) expressed in Rosetta2(DE3)/pLysS cells measured after 30 mins by high-throughput fluorescence polarization assay relative to control
|
Homo sapiens
|
60.0
%
|
|
Binding affinity to Mc1-1 (unknown origin) by fluorescence polarization competition assay
|
Homo sapiens
|
180.0
nM
|
|
Binding affinity to Bcl-2 (unknown origin) by fluorescence polarization competition assay
|
Homo sapiens
|
460.0
nM
|
|
Binding affinity to Bc1-xL (unknown origin) by fluorescence polarization competition assay
|
Homo sapiens
|
610.0
nM
|
|
Disruption of interaction between human recombinant GST-tagged MKK3/VF-tagged MYC expressed in HEK293T cells at 20 uM measured after 2 hrs by TR-FRET assay
|
Homo sapiens
|
31.0
%
|
|
Inhibition of porcine heart malate dehydrogenase preincubated for 5 min followed by nicotinamide adenine dinucleotide addition and monitered for 90 sec by spectrophotometric method
|
Sus scrofa
|
820.0
nM
|
|