|
Inhibition of HIV-1 replication in H9 (human lymphoma) cells.
|
Human immunodeficiency virus 1
|
7.0
ug.mL-1
|
|
|
Inhibition of uninfected H9 lymphocytic cell growth
|
Homo sapiens
|
8.0
ug.mL-1
|
|
|
Inhibition of polymerization in wild type HIV-1 RT with poly rC/dG12-18 template primer and [3H]dGTP
|
Human immunodeficiency virus 1
|
730.0
nM
|
|
|
Inhibition against HIV-1 integrase at 1 mM
|
Human immunodeficiency virus 1
|
50.0
%
|
|
|
Inhibition against HIV-1 integrase at 200 uM
|
Human immunodeficiency virus 1
|
50.0
%
|
|
|
Inhibition against HIV-1 integrase at 25 uM
|
Human immunodeficiency virus 1
|
50.0
%
|
|
|
Compound was evaluated for its inhibitory activity against recombinant rat SE(squalene epoxidase)
|
None
|
690.0
nM
|
|
|
Inhibition of FabZ
|
Plasmodium falciparum
|
400.0
nM
|
|
|
Inhibition of FabI
|
Plasmodium falciparum
|
200.0
nM
|
|
|
Inhibition of FabG
|
Plasmodium falciparum
|
300.0
nM
|
|
|
Inhibition of Plasmodium falciparum ENR
|
Plasmodium falciparum
|
250.0
nM
|
|
|
Inhibition of Plasmodium falciparum ENR using NADH substrate
|
Plasmodium falciparum
|
186.0
nM
|
|
|
Inhibition of Plasmodium falciparum ENR using crotonyl-CoA substrate
|
Plasmodium falciparum
|
79.0
nM
|
|
|
Inhibition of Plasmodium falciparum ENR in presence of triclosan
|
Plasmodium falciparum
|
8.0
nM
|
|
|
Inhibition of chymotrypsin like activity of 20S proteasome
|
Homo sapiens
|
200.0
nM
|
|
|
Inhibition of chymotrypsin like activity of 20S proteasome in leukemia Raji B cells at 25 uM after 4 hrs
|
Homo sapiens
|
4.0
%
|
|
|
Inhibition of chymotrypsin like activity of 20S proteasome in leukemia Raji B cells at 25 uM after 24 hrs
|
Homo sapiens
|
10.0
%
|
|
|
Inhibition of yeast G6PD
|
Saccharomyces cerevisiae
|
250.0
nM
|
|
|
Inhibition of 6PGD
|
None
|
720.0
nM
|
|
|
Inhibition of beta amyloid 25-35 fibril formation at 10 uM
|
None
|
13.0
%
|
|
|
Binding affinity to BCL2
|
None
|
234.42
nM
|
|
|
Antioxidant activity assessed as DPPH free radical scavenging activity after 30 mins
|
None
|
2.7
ug.mL-1
|
|
|
Antiviral activity against Influenza (A/PR8/34(H1N1))
|
Influenza A virus (A/Puerto Rico/8/1934(H1N1))
|
391.0
nM
|
|
|
Inhibition of Streptococcus sobrinus glucosyltransferase assessed as blockade of adherent water insoluble glucan synthesis at 100 ug/mL
|
Streptococcus sobrinus
|
26.5
%
|
|
|
Inhibition of Streptococcus sobrinus glucosyltransferase assessed as blockade of adherent water insoluble glucan synthesis at 10 ug/mL
|
Streptococcus sobrinus
|
10.5
%
|
|
|
Inhibition of Streptococcus sobrinus glucosyltransferase assessed as blockade of adherent water insoluble glucan synthesis at 1 ug/mL
|
Streptococcus sobrinus
|
3.0
%
|
|
|
Inhibition of rat squalene epoxidase
|
Rattus norvegicus
|
690.0
nM
|
|
|
Antioxidant activity assessed as DPPH radical scavenging activity
|
None
|
5.6
ug.mL-1
|
|
|
Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release
|
Homo sapiens
|
39.87
nM
|
|
|
Anti-aging activity in human dermal fibroblasts assessed as inhibition rate of MMP1 expression at 10 uM relative to control
|
Homo sapiens
|
46.7
%
|
|
|
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA activation at 1000 molar ratio after 48 hrs relative to TPA
|
Human herpesvirus 4
|
6.4
%
|
|
|
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA activation at 500 molar ratio after 48 hrs relative to TPA
|
Human herpesvirus 4
|
34.9
%
|
|
|
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA activation at 100 molar ratio after 48 hrs relative to TPA
|
Human herpesvirus 4
|
68.1
%
|
|
|
Inhibition of TPA-induced EBV-early antigen activation in human Raji cells assessed as EA activation at 10 molar ratio after 48 hrs relative to TPA
|
Human herpesvirus 4
|
87.7
%
|
|
|
Inhibition of COX2 at 25 uM
|
None
|
13.0
%
|
|
|
Inhibition of COX1 at 30 ug/mL
|
None
|
51.0
%
|
|
|
Inhibition of human neutrophil elastase at 1 uM
|
Homo sapiens
|
26.6
%
|
|
|
Inhibition of human neutrophil elastase at 3 uM
|
Homo sapiens
|
41.3
%
|
|
|
Inhibition of human neutrophil elastase at 10 uM
|
Homo sapiens
|
63.6
%
|
|
|
Inhibition of human neutrophil elastase at 30 uM
|
Homo sapiens
|
71.4
%
|
|
|
Inhibition of human neutrophil elastase at 100 uM
|
Homo sapiens
|
78.4
%
|
|
|
Inhibition of reduced carboxymethylated kappa-casein fibril formation at 50 ug/mL measured every 5 mins after 1000 mins by thioflavin T staining-based binding assay
|
None
|
100.0
%
|
|
|
Inhibition of beta amyloid (1 to 42) fibril formation at 50 ug/mL by thioflavin T staining-based binding assay
|
None
|
100.0
%
|
|
|
Inhibition of beta amyloid (1 to 40) fibril formation
|
None
|
180.0
nM
|
|
|
Inhibition of chymotrypsin like activity of proteasome
|
None
|
86.0
nM
|
|
Inhibition of chymotrypsin like activity of proteasome
|
None
|
170.0
nM
|
|
|
Inhibition of chymotrypsin like activity of 20S proteasome in human MDA-MB-231 cells lysates with high catechol-O-methyltransferase activity assessed as cleavage of Suc-LLVY-AMC substrate at 10 uM after 2 hrs by fluorogenic assay
|
Homo sapiens
|
22.0
%
|
|
|
Inhibition of osteoclastogenesis in RANKL-stimulated mouse osteoclast at 10 uM
|
Mus musculus
|
17.0
%
|
|
|
Inhibition of osteoclastogenesis in RANKL-stimulated mouse osteoclast at 20 uM
|
Mus musculus
|
32.0
%
|
|
|
Inhibition of Plasmodium falciparum FabZ by spectrophotometric analysis
|
Plasmodium falciparum
|
0.03
ug.mL-1
|
|
|
Inhibition of Plasmodium falciparum FabG by spectrophotometric analysis
|
Plasmodium falciparum
|
0.32
ug.mL-1
|
|
|
PUBCHEM_BIOASSAY: Fluorescent Polarization Homogeneous Dose Response HTS to Identify Inhibitors of Mex-5 Binding to TCR-2. (Class of assay: confirmatory) [Related pubchem assays: 1833 (Project Summary), 1832 (Primary HTS)]
|
Caenorhabditis elegans
|
727.0
nM
|
|
|
Cytotoxicity against African green monkey Vero cells assessed as viability at 100 uM after 24 hrs
|
Chlorocebus sabaeus
|
80.0
%
|
|
|
Cytotoxicity against African green monkey CV1 cells assessed as viability at 100 uM after 24 hrs
|
Chlorocebus aethiops
|
97.0
%
|
|
|
Anticancer activity against human PC3 cells xenografted in sc dosed SCID mouse assessed as inhibition of tumor growth at 80 mg/kg, ip qd for 14 days
|
Homo sapiens
|
32.0
%
|
|
|
Antiproliferative activity against rat HSC-T6 cells at 100 uM after 48 hrs by MTT assay
|
Rattus norvegicus
|
33.4
%
|
|
|
Antiproliferative activity against rat HSC-T6 cells at 10 uM after 48 hrs by MTT assay
|
Rattus norvegicus
|
83.8
%
|
|
|
Antiproliferative activity against rat HSC-T6 cells at 50 uM after 48 hrs by MTT assay
|
Rattus norvegicus
|
41.7
%
|
|
|
Inhibition of Influenza A/Udorn/72/H3N2 full length GST-tagged NS1A/FAM-double strand RNA-interaction at 50 uM after 1 hr by fluorescence polarization assay
|
Influenza A virus (A/udorn/1972(H3N2))
|
89.0
%
|
|
|
Inhibition of GST-tagged human DYRK1A using dephosphorylated MBP as substrate at 10 uM after 10 mins by Kinase-Glo plus luminescent kinase assay
|
Homo sapiens
|
47.6
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced MMP9 expression at 25 uM by Western blotting relative to control
|
Mus musculus
|
70.0
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced MMP9 expression at 50 uM by Western blotting relative to control
|
Mus musculus
|
75.0
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced MMP9 expression at 100 uM by Western blotting relative to control
|
Mus musculus
|
90.0
%
|
|
|
Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion at 10 uM by alphaLISA technique
|
Homo sapiens
|
5.78
%
|
|
|
Inhibition of recombinant human BACE1 using Eu-CEVNLDAEFK-Qsy7 as substrate by HTRF assay
|
Homo sapiens
|
757.0
nM
|
|
|
Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion at 1 nM by alphaLISA technique
|
Homo sapiens
|
-18.24
%
|
|
|
Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion at 0.01 uM by alphaLISA technique
|
Homo sapiens
|
-12.61
%
|
|
|
Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion at 0.1 uM by alphaLISA technique
|
Homo sapiens
|
-0.72
%
|
|
|
Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion at 1 uM by alphaLISA technique
|
Homo sapiens
|
-11.78
%
|
|
|
Inhibition of recombinant human BACE1 using substrate conjugated with reporter EDANS and DABCYL at 0.03 mg/mL
|
Homo sapiens
|
38.0
%
|
|
|
Antialzheimer's disease activity in mouse cortex assessed as inhibition of beta-secretase mediated amyloid beta1-42 production at 1.5 mg/kg
|
Mus musculus
|
18.64
%
|
|
|
Antialzheimer's disease activity in mouse cortex assessed as inhibition of beta-secretase mediated amyloid beta1-42 production at 3 mg/kg
|
Mus musculus
|
51.17
%
|
|
|
Antialzheimer's disease activity in mouse hippocampus assessed as inhibition of beta-secretase mediated amyloid beta1-42 production at 1.5 mg/kg
|
Mus musculus
|
25.48
%
|
|
|
Antialzheimer's disease activity in mouse hippocampus assessed as inhibition of beta-secretase mediated amyloid beta1-42 production at 3 mg/kg
|
Mus musculus
|
39.79
%
|
|
|
Inhibition of mammosphere formation in human MDA-MB-231 cells at 10 uM after 7 days by inverted phase-contrast microscopy
|
Homo sapiens
|
20.1
%
|
|
|
Inhibition of mammosphere formation in human MDA-MB-231 cells at 20 uM after 7 days by inverted phase-contrast microscopy
|
Homo sapiens
|
51.3
%
|
|
|
Competitive inhibition of Spiroplasma sp. MQ1 SssI methyltransferase using pUC18 as substrate measured for 10 mins by Dixon plot analysis
|
Spiroplasma monobiae
|
28.0
nM
|
|
|
Inhibition of DNMT1 in human HeLa cell nuclear extract assessed as methylated substrate level at 10 uM by ELISA
|
Homo sapiens
|
42.0
%
|
|
|
Inhibition of HER2 phosphorylation in human SK-BR-3 cells after 6 hrs by Western blot analysis
|
Homo sapiens
|
18.0
%
|
|
|
Antioxidant activity assessed as superoxide dismutase-like activity by SOD-WST assay
|
None
|
26.1
ug.mL-1
|
|
|
Inhibition of electric eel AChE at 2 mg/ml by Ellman's method
|
Electrophorus electricus
|
-14.31
%
|
|
|
Inhibition of horse BChE at 2 mg/ml by Ellman's method
|
Equus caballus
|
-4.27
%
|
|
|
Inhibition of tetrahymena telomerase using 3'-ACT TCG TAG AGC AGA TTG-5' as substrate incubated for 10 mins prior to extension reaction by telomeric repeat amplification protocol
|
Tetrahymena
|
370.0
nM
|
|
|
Displacement of NLWAAQRYGRELRRMSD-K(FITC)-FVD from Bcl-2 (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
335.0
nM
|
|
|
Cytotoxicity against ER-negative Homo sapiens (human) MDA-MB-468 cells assessed as inhibition of cell viability at 5 to 80 ug/ml after 24 to 72 hr by MTT assay
|
Homo sapiens
|
3.0
%
|
|
|
Antioxidant activity in Homo sapiens (human) epidermal microsomal fractions assessed as inhibition of UV-induced lipid peroxidation measured at 6 to 48 hr
|
Homo sapiens
|
41.0
%
|
|
|
Antioxidant activity in Homo sapiens (human) dermis cytosolic form assessed as inhibition of UV-induced nitric oxide production administered before UV induction at 48 hr by Griess assay
|
Homo sapiens
|
30.0
%
|
|
|
Antioxidant activity in Homo sapiens (human) epidermis cytosolic form assessed as inhibition of UV-induced nitric oxide production administered before UV induction at 48 hr by Griess assay
|
Homo sapiens
|
30.0
%
|
|
|
Antioxidant activity in Homo sapiens (human) dermis assessed as inhibition of UV-induced hydrogen peroxide production administered before UV induction at 48 hr by DHR assay
|
Homo sapiens
|
30.0
%
|
|
|
Antioxidant activity in Homo sapiens (human) epidermis assessed as inhibition of UV-induced hydrogen peroxide production administered before UV induction at 48 hr by DHR assay
|
Homo sapiens
|
30.0
%
|
|
|
Inhibition of Plasmodium falciparum FabZ using crotonoyl-CoA as substrate preincubated for 10 mins prior to substrate addition
|
Plasmodium falciparum
|
700.0
nM
|
|
|
Inhibition of Clostridium histolyticum collagenase using N-[3-(2-Furyl)acryloyl]-Leu-Gly-Pro-Ala as substrate at 100 ug/ml after 15 mins by spectrophotometric analysis relative to control
|
Clostridium histolyticum
|
41.16
%
|
|
|
Inhibition of human neutrophil elastase assessed as N-methoxysuccinyl-Ala-Ala-Pro-Val p-nitroanilide conversion to p-nitroaniline at 100 ug/ml after 1 hr by spectrophotometric analysis relative to control
|
Homo sapiens
|
88.17
%
|
|
|
Inhibition of recombinant Plasmodium falciparum FabZ using crotonoyl-CoA as substrate after 10 mins
|
Plasmodium falciparum
|
30.0
nM
|
|
|
Inhibition of recombinant Plasmodium falciparum 3D7 FabG using acetoacetyl-CoA as substrate after 10 mins in presence of NADPH
|
Plasmodium falciparum 3D7
|
320.0
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
49.04
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
45.88
%
|
|
|
Inhibition of human GST-fused DYRK1A expressed in Escherichia coli using KISGRLSPIMTEQ as substrate
|
Homo sapiens
|
330.0
nM
|
|
|
Inhibition of 67LR co-localization in lipid rafts containing cholera toxin labeled GM1 gangliosides in human A431 cells after 30 mins by immunofluorescence-based confocal microscopic analysis (Rvb = 75%)
|
Homo sapiens
|
47.0
%
|
|
|
Binding affinity to STAT1 (unknown origin) by surface plasmon resonance assay
|
Homo sapiens
|
700.0
nM
|
|
|
Binding affinity to rat brain cell membrane
|
Rattus norvegicus
|
25.0
nM
|
|
|
Antimalarial activity against chloroquine-sensitive/mefloquine-resistant Plasmodium falciparum D6 by malaria SYBR green 1-based fluorescence (MSF) assay
|
Plasmodium falciparum D6
|
73.0
nM
|
|
|
Antimalarial activity against chloroquine /mefloquine/pyrimethamine-resistant Plasmodium falciparum C235 by malaria SYBR green 1-based fluorescence (MSF) assay
|
Plasmodium falciparum
|
610.0
nM
|
|
|
Inhibition of human type O erythrocyte ICAM1-mediated Plasmodium falciparum infection with at 50 uM
|
Homo sapiens
|
85.0
%
|
|
|
Inhibition of Plasmodium falciparum FabZ
|
Plasmodium falciparum
|
0.03
ug.mL-1
|
|
|
Inhibition of Plasmodium falciparum FabG
|
Plasmodium falciparum
|
0.2
ug.mL-1
|
|
|
Reduction in amyloid beta levels in Tg2576 mouse
|
Mus musculus
|
50.0
%
|
|
|
Reduction in amyloid beta plaques in Tg2576 mouse
|
Mus musculus
|
50.0
%
|
|
|
Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintillation counting method
|
Homo sapiens
|
500.0
nM
|
|
|
Inhibition of amyloid beta (1 to 42) (unknown origin) aggregation at 100 uM incubated at 37 degC for 16 hrs by thioflavin T fluorescence assay
|
Homo sapiens
|
95.1
%
|
|
|
Inhibition of amyloid beta (1 to 42) (unknown origin) aggregation incubated at 37 degC for 16 hrs by thioflavin T fluorescence assay
|
Homo sapiens
|
500.0
nM
|
|
|
Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 1 uM after 5 days by CellTiter 96 Aqueous assay
|
Homo sapiens
|
124.1
nM
|
|
|
Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 10 uM after 5 days by CellTiter 96 Aqueous assay
|
Homo sapiens
|
122.6
nM
|
|
|
Inhibition of rat Dyrk1A using Woodtide as substrate after 40 mins by P81 membrane assay in presence of [33P]-g-ATP
|
Rattus norvegicus
|
330.0
nM
|
|
|
Inhibition of wild type His-tagged translin/trax E126A mutant (unknown origin) coexpressed in Escherichia coli BL21 cells using RNase Alert as substrate at 30 uM incubated for 10 mins prior to substrate addition monitored over 60 mins by fluorescence assay
|
Homo sapiens
|
88.0
%
|
|
|
Antiviral activity against HBV infected in human HuS-E/2 cells assessed as inhibition of viral mRNA level at 50 uM treated for 20 hrs measured after 7 days by RT-PCR method relative to control
|
Hepatitis B virus
|
80.0
%
|
|
|
Binding affinity to recombinant human transthyretin expressed in Escherichia coli BL21 by STD-NMR spectroscopic method
|
Homo sapiens
|
400.0
nM
|
|
|
Inhibition of recombinant human ACE at 100 uM using Mca-R-P-PG-F-S-A-F-K(Dnp)-OH as substrate measured every 2 mins for 8 mins by fluorescence assay
|
Homo sapiens
|
82.02
%
|
|
|
Antiviral activity against Chikungunya virus infected in HEK293T cells assessed as reduction in infectious virus particle production by luciferase reporter gene assay
|
Chikungunya virus
|
6.54
ug.mL-1
|
|
|
Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 20 uM incubated for 24 hrs under dark condition by thioflavin-T based fluorometric assay relative to control
|
Homo sapiens
|
86.1
%
|
|
|
Displacement of [3H]resveratrol from Sprague-Dawley rat brain plasma membranes after 1 hr by beta counting method
|
Rattus norvegicus
|
25.0
nM
|
|
|
Inhibition of enolase (unknown origin) at 0.625 uM using 2-PG relative to control
|
Homo sapiens
|
63.0
%
|
|
|
Inhibition of LDH (unknown origin) at 0.625 uM using 2-PG relative to control
|
Homo sapiens
|
63.0
%
|
|
|
Inhibition of pyruvate kinase (unknown origin) at 0.625 uM using 2-PG relative to control
|
Homo sapiens
|
63.0
%
|
|
|
Inhibition of recombinant human His-tagged PGAM1 expressed in Escherichia coli BL21 competent cells by kinase-glo assay
|
Homo sapiens
|
490.0
nM
|
|
|
Inhibition of human recombinant GST-tagged DYRK1A expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate after 40 mins in presence of [gamma33P-ATP]
|
Homo sapiens
|
330.0
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
|
13.39
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
5.85
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
17.83
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
27.87
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
29.27
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
3.47
%
|
|
|
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
|
-2.04
%
|
|
|
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
|
6.28
%
|
|
|
Inhibition of HFIP-pretreated amyloid beta (1 to 42 residues) (unknown origin) self aggregation at 25 uM after 7 days by ThT-based fluorometric method relative to control
|
Homo sapiens
|
52.9
%
|
|
|
Inhibition of Streptococcus mutans F-ATPase activity relative to control
|
Streptococcus mutans
|
50.0
%
|
|
|
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
|
Escherichia coli
|
580.0
nM
|
|
|
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
|
Escherichia coli
|
360.0
nM
|
|
|
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
|
90.0
%
|
|
|
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
|
98.0
%
|
|
|
Inhibition of HAT (unknown origin) relative to control
|
Homo sapiens
|
50.0
%
|
|
|
Antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP263 promastigotes infected in BALB/c mouse peritoneal macrophages assessed as decrease in parasitic infection index at 48 uM incubated for 72 hrs by light microscopy relative to control
|
Leishmania infantum
|
97.7
%
|
|
|
Antileishmanial activity against stationary phase of Leishmania infantum MHOM/MA/67/ITMAP263 infected in BALB/c mouse assessed as decrease in parasitic load in liver at 12.5 mg/kg/day administered orally via gavage as bid for 5 days on 7th day post infection and measured on day 30 by limiting dilution assay relative to control
|
Leishmania infantum
|
47.5
%
|
|
|
Antileishmanial activity against stationary phase of Leishmania infantum MHOM/MA/67/ITMAP263 infected in BALB/c mouse assessed as decrease in parasitic load in liver at 25 mg/kg/day administered orally via gavage as bid for 5 days on 7th day post infection and measured on day 30 by limiting dilution assay relative to control
|
Leishmania infantum
|
93.6
%
|
|
|
Antileishmanial activity against stationary phase of Leishmania infantum MHOM/MA/67/ITMAP263 promastigotes infected in BALB/c mouse assessed as decrease in parasitic load in liver at 50 mg/kg/day administered orally via gavage as bid for 5 days on 7th day post infection and measured on day 30 by limiting dilution assay relative to control
|
Leishmania infantum
|
98.7
%
|
|
|
Inhibition of chymotrypsin-like activity of purified human 20S proteasome assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 30 mins by fluorometric analysis
|
Homo sapiens
|
86.0
nM
|
|
|
Inhibition of RAD52 (unknown origin) assessed as reduction in RAD52-ssDNA interaction using Cy3-dT30-Cy5 ssDNA by FRET assay
|
Homo sapiens
|
277.0
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
|
99.33
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
99.51
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
720.0
nM
|
|
|
MERS 3CL-Pro protease inhibition percentage at 10 µM by FRET kind of response from peptide substrate
|
Middle East respiratory syndrome
|
10.0
%
|
|
MERS 3CL-Pro protease inhibition percentage at 10 µM by FRET kind of response from peptide substrate
|
Middle East respiratory syndrome
|
16.0
%
|
|
|
Chymotrypsin inhibition percentage at 10 µM by FRET kind of response from peptide substrate
|
Homo sapiens
|
-0.5
%
|
|
|
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
|
-0.15
%
|
|
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
|
0.29
%
|
|
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
|
-0.15
%
|
|
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
|
0.29
%
|
|
|
Modulation of NF-kappaB in Sprague-Dawley rat BMM assessed as inhibition of M-CSF/RANKL-induced osteoclast differentiation by measuring decrease in TRAP-positive multinucleated cells at 100 uM measured after 5 days by TRAP-staining based assay relative to control
|
Rattus norvegicus
|
92.0
%
|
|
|
Binding affinity to recombinant Influenza A virus (A/USA:Huston/AA/1945 H1N1)) N-terminal His6-tagged PA endonuclease assessed as dissociation constant by SPR analysis
|
influenza A virus
|
956.32
nM
|
|
|
Inhibition of biotinylated 5-(4-((Z)-3-Carboxy-3-hydroxyacryloyl)-4-(4-chlorobenzyl)piperidine-1-carbonyl)-2-((13,35-dioxo-39-((3aR,4R,6aS)-2-oxohexahydro-1H-thieno[3,4-d]imidazole-4-yl)-3,6,9,16,19,22,25,28,31-nonaoxa-12,34-diazanonatriacontyl)oxy)benzoic acid binding to Influenza A virus (A/California/07/2009(H1N1)) N-terminal GST-tagged polymerase acidic subunit N-terminal domain expressed in Escherichia coli BL21 (DE3) RIL cells measured after 120 mins by Alphascreen assay
|
Influenza A virus (A/California/07/2009(H1N1))
|
870.0
nM
|
|
|
Binding affinity to wild type TTR (unknown origin) expressed in bacterial expression system by isothermal titration calorimetry
|
Homo sapiens
|
400.0
nM
|
|
|
Inhibition of recombinant His-tagged PGAM1 (unknown origin) expressed in Escherichia coli BL21 using 3-PG as substrate in presence of ADP by Kinase-Glo max luminescent assay
|
Homo sapiens
|
490.0
nM
|
|
|
Stabilization of wild type human transthyretin expressed in Escherichia coli BL21(DE3) assessed as decrease in TTR-amyloid beta fibril formation at 10 uM preincubated for 6 hrs with transthyretin followed by measuring after 96 hrs maintaining pH of 4.4 by thioflavin T binding assay relative to control
|
Homo sapiens
|
53.0
%
|
|
|
Inhibition of 6His-tagged human RD52 assessed as reduction in RD52 binding to Cy3-dT30-Cy5 ssDNA incubated for 30 mins by FRET assay
|
Homo sapiens
|
277.0
nM
|
|
|
Inhibition of cytochrome c (unknown origin) assessed as reduction in cyt c-CL complex formation at 10 uM incubated for 15 mins in presence of cardiolipin by Trp-59 fluorescence assay relative to control
|
Homo sapiens
|
63.0
%
|
|
|
Inhibition of cytochrome c (unknown origin) assessed as reduction in cyt c-CL peroxidase activity at 10 uM up to 20 mins in presence of cardiolipin by Amplex red staining based fluorescence assay relative to control
|
Homo sapiens
|
50.0
%
|
|
|
Inhibition of cytochrome c (unknown origin) assessed as reduction reduction of cyt c from its ferric state to ferrous state at 10 uM incubated for 20 mins in presence of cardiolipin by UV-vis Spectrophotometric assay relative to control
|
Homo sapiens
|
62.0
%
|
|
|
Inhibition of COL1A1 promotor activity in human LX2 cells at 20 uM incubated for 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
19.19
%
|
|
|
Inhibition of COL1A1 promotor activity in human LX2 cells at 50 uM incubated for 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
32.25
%
|
|
|
Reversal of Pgp-mediated paclitaxel resistance in human LCC6MDR cells assessed as paclitaxel IC50 at 1 uM after 5 days by Cell Titer-Glo luminescence assay (Rvb = 152.5 +/- 9.7 uM)
|
Homo sapiens
|
124.1
nM
|
|
|
Reversal of Pgp-mediated paclitaxel resistance in human LCC6MDR cells assessed as paclitaxel IC50 at 10 uM after 5 days by Cell Titer-Glo luminescence assay (Rvb = 152.5 +/- 9.7 uM)
|
Homo sapiens
|
122.6
nM
|
|
