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DNA Polymerase Activity Assay from Article 10.1128/aac.01311-05: "Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound."
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
GGTase-I Activity Assay from Article 10.1016/s0960-894x(03)00095-7: "Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives."
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
FTase Activity Assay from Article 10.1016/s0960-894x(03)00095-7: "Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives."
Assay data:11 Active, 3 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 11 Tested
CDK Kinase Inhibition Assay from Article 10.1016/s0960-894x(03)00792-3: "Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides."
Assay data:22 Active, 17 Activity ≤ 1 µM, 22 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Activity against PROGEST/BO in the Eurofins Panlabs screen (BI) by Radioactive Assay
Assay data:1 Tested
SummaryRelated BioAssays by Target
Activity against ESTROGEN/BO in the Eurofins Panlabs screen (BI) by Radioactive Assay
To determine the fetal calf serum protein binding, the plasma is diluted to 50 % with pH 7.4 phosphate buffer and warmed to 37 C before adding test compounds achieving 5 uM concentration. The dialysis buffer is added to one side of the chamber of the RED device, and the incubation is initiated by the addition of 300 uL of the test compound protein solution to the opposing chamber. The samples are incubated for 4 hours. Equal volumes from the buffer and the plasma chambers are transferred into separate wells. 50 uL of 50 % blank plasma are added to the buffer samples, and 50 uL of buffer are added to the 50 % plasma samples to ensure matrix matching of samples from both the free and bound fractions. Acetonitrile containing internal standard are added to precipitate the protein. The supernatants are analyzed by LC-MS/MS and the results are calculated. The assay has been performed by Concept Life Sciences Ltd.
Assay data:9 Tested
Summary
Inhibition of Bovine milk xanthine oxidase using xanthine as substrate assessed as decrease in uric acid level preincubated for 5 mins followed by substrate addition by spectrophotometric analysis
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of bovine pancreatic alpha chymotrypsin using N-succinyl-Gly-Gly-Phe-p-nitroanilide as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured for 30 mins
Assay data:8 Active, 2 Activity ≤ 1 µM, 8 Tested
Binding affinity to calf thymus DNA at upto 18 micromol/ml by fluorescence spectroscopic method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Binding affinity to calf brain tubulin colchicine binding site assessed as retention half time at 3 uM incubated for 30 mins by fluorescence based photon-counting instrument
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to calf brain tubulin colchicine binding site assessed as Koff at 3 uM incubated for 30 mins by fluorescence based photon-counting instrument
Displacement of fluorescent probe (R)-(+)-ethyl 5-amino2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-ylcarbamate from calf brain tubulin colchicine binding site assessed as dissociation constant at 0.05 to 70 uM incubated for 30 mins by fluorescence based assay
Displacement of fluorescent probe (R)-(+)-ethyl 5-amino2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-ylcarbamate from calf brain tubulin colchicine binding site assessed as binding constant at 0.05 to 70 uM incubated for 30 mins by fluorescence based assay
Assay data:2 Tested
Displacement of 2-methoxy-5-(2,3,4-trimethoxyphenyl)-2,4,6-cycloheptatriene-1-one from calf brain tubulin colchicine site
Inhibition of calf brain tubulin assembly measured upto 100 mins
Binding affinity to bovine milk XO using xanthine as substrate assessed as inhibition constant by 1/V-axis intercept replot based method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to bovine milk XO using xanthine as substrate assessed as inhibition constant by Dixon plot based method
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to calf thymus DNA by DAPI staining based competitive binding assay
Binding affinity to calf thymus DNA by acridine orange staining based competitive binding assay
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