Keith W. Ward

TL;DR: Reduced molecular flexibility, as measured by the number of rotatable bonds, and low polar surface area or total hydrogen bond count are found to be important predictors of good oral bioavailability, independent of molecular weight.

TL;DR: Allometric scaling approaches were less successful at predicting human clearance than methods based on clearance as a set fraction of liver blood flow from an individual species, and commonly used prospective measures of allometric scaling success failed to discriminate between successful and failed allometric predictions.

TL;DR: A chemical lead that selectively inhibited the C3aR in a high throughput screen was identified and chemically optimized, and the resulting antagonist, N2-[(2,2-diphenylethoxy)acetyl]-l-arginine (SB 290157), functioned as a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia (RBL)-2H3 cells expressing the human C3iR.

TL;DR: Estimating human volume and mean residence time based on monkey data alone was the most accurate approach evaluated and the value of the monkey as a species for pharmacokinetic lead optimization was confirmed.