Inhibition of human recombinant GSK3beta using biotin- AAEELDSRAGS(PO3H2)PQL as substrate and [gamma32P]ATP after 20 mins by scintillation proximity assay
ASTRAZENECA: Octan-1-ol/water (pH7.4) distribution coefficent measured by a shake flask method described in J. Biomol. Screen. 2011, 16, 348-355. Experimental range -1.5 to 4.5
ASTRAZENECA: Solubility in pH7.4 buffer using solid starting material using the method described in J. Assoc. Lab. Autom. 2011, 16, 276-284. Experimental range 0.10 to 1500 uM
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.