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: % 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: Intrinsic clearance measured in human liver microsomes following incubation at 37C. Experimental range <3 to >150 microL/min/mg. Rapid Commun. Mass Spectrom. 2010, 24, 1730-1736.
ASTRAZENECA: Intrinsic clearance measured in rat hepatocytes following incubation at 37C. Experimental range <3 to >150 microL/min/1E6 cells. Rapid Commun. Mass Spectrom. 2010, 24, 1730-1736
ASTRAZENECA: Most acidic pKa value (pKa A1) determined by absorption and potentiometric titration using standard methodology from Sirius Analytical. Experimental range Acids: <= 11.