Sentence examples for potency improvement from inspiring English sources

Structure guided SAR exploration resulted in >10,000-fold potency improvement for the BRD4-BD1 bromodomain.

Structure guided design was used to optimize the series resulting in a significant potency improvement.

Elaboration of a fragment chemical lead established a new lipophilic aryl Tyr interaction resulting in a substantial potency improvement.

Based upon Ki values, the 3,4-dichlorophenyl analog represented a potency improvement of nearly one order of magnitude.

This task is of special importance in fragment-based drug design, where typically multiple rounds of potency improvement are necessary to generate highly active lead structures out of micromolar initial inhibitors.

Collectively, based on the dose dependent data, contrast potency improvement is estimated to be at least 24-fold higher than Gd in the Vasovist formulation, which is considered the most sensitive vascular agent approved for clinical use [5].

When the same formal transformation was performed on the epimeric (R) diastereomer and desmethyl examples, no correspondingly large potency improvements were observed (29, GI50 = 36 nM; and 31, GI50 = 55 nM).

But there were no significant differences in the samples collected from the Senate letters, and there was no increase in potency or improvement in quality from one Senate sample to the next.

We find that estimating serum potencies improves test error further (model 8, Table 1), with improvements of between 0.01 and 0.12 log2 HI titers.

Ultimately, two independent structural modifications led to a similar shift in binding mode that when combined led to a synergistic improvement in potency and the identification of inhibitors with sub-micromolar HCV NS5B binding potency.

Introduction of a single methyl branch at the 2-position of the side chain as in compound 8 slightly improved activity over that of the unbranched compound 26, and significant improvement in potency was observed with the addition of a second methyl group at this position as in the neopentyl group of compound 27 (omadacycline).