Agonist activity at human TLR7 expressed in NF-kappaB-stimulated HEK293 cells assessed as induction of secreted alkaline phosphatase expression by reporter gene assay
Agonist activity at human TLR8 expressed in NF-kappaB-stimulated HEK293 cells assessed as induction of secreted alkaline phosphatase expression by reporter gene 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: % 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.
Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as parasitemia at 10 ug, ip administered for 4 days measured on day 7 by Giemsa-staining based assay
Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as reduction in parasitemia at 10 ug, ip administered for 4 days measured on day 9 by Giemsa-staining based assay
Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as parasitemia at 10 ug, ip co-administered with chloroquine for 4 days measured on day 30 by Giemsa-staining based assay
Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as reduction in parasitemia at 10 ug, ip co-administered with chloroquine for 4 days measured on day 25 by Giemsa-staining based assay
Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as reduction in parasitemia at 10 ug, ip co-administered with chloroquine for 4 days measured on day 23 by Giemsa-staining based assay
Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as reduction in CD3+ cell level in brain at 10 ug, ip co-administered with chloroquine for 4 days measured on day 10 by flow cytometry
Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as reduction in CD3+ cell level in brain at 10 ug, ip administered for 4 days measured on day 10 by flow cytometry