Inhibition of Escherichia coli AlkB deltaN11 mutant using 5'-TTCmTTTTTTTTTTTT-3'-fluorescein as substrate after 4.5 mins by capillary electrophoresis-based laser-induced fluorescence assay
Inhibition of human hexahistidine-tagged full-length FTO expressed in Escherichia coli BL21 (DE3) using 3-methylthymidine as substrate assessed as inhibition of 3-methylthymidine conversion to thymidine after 1 hr by liquid chromatographic analysis
Inhibition of human hexahistidine-tagged full-length FTO expressed in Escherichia coli BL21 (DE3) assessed as residual activity at 200 uM by scintillation proximity assay
ASTRAZENECA: % bound to plasma by equilibrium dialysis. Compound is incubated with whole human plasma at 37C for >5hrs. Method described in B. Testa et al (Eds.), Pharmacokinetic Profiling in Drug Research: Biological, Physicochemical, and Computational Strategies, Wiley-VCH, Weinheim, 2006, pp.119-141. Experimental range 10% to 99.95% bound.
ASTRAZENECA: % bound to plasma by equilibrium dialysis. Compound is incubated with whole rat plasma at 37C for >5hrs. Method described in B. Testa et al (Eds.), Pharmacokinetic Profiling in Drug Research: Biological, Physicochemical, and Computational Strategies, Wiley-VCH, Weinheim, 2006, pp.119-141. Experimental range 10% to 99.95% bound.
Inhibition of recombinant full length N-terminal hexahistidine-tagged human FTO demethylation activity expressed in Escherichia coli BL21 (DE3) incubated for 1 hrs using m3T nucleoside as substrate by LCMS-based assay