Sentence examples for enzyme potency from inspiring English sources

SAR study describes optimisation of enzyme potency, whole cell potency and evidence of mechanism of action.

Structure-based design strategies were applied to significantly improve enzyme potency and the polarity of the molecule was adjusted to gain cellular activity.

For any JAK small molecule development program, our results suggest that relying solely on enzyme potency and selectivity data may be misleading.

An exploratory chemistry effort focused on expanding the SAR around hydroxamic acid zinc-binding 'warheads' lead to the identification of novel compounds with enzyme potency and antibacterial activity similar to CHIR-090.

We describe herein the design, syntheses and evaluation of a number of bicycloproline P2 bearing HCV protease inhibitors endowed with impressive enzyme potency, enzyme selectivity, cellular activity and favorable ADME profiles.

X-ray crystal structure of the ligand in contact with the NS3/4A protein and modulation of the quinoline heterocyclic region by structure based design and modeling allowed for the optimization of enzyme potency and cellular activity.

There was a broad correlation between the enzyme potencies of the compounds and their effectiveness at inhibiting AKR1C3 activity in cells.

Starting from a lead compound 1a, iterative design and SAR exploitation of the scaffold led to analogues with nM enzyme potencies against TBK1/IKKε.

Optimisation of this series for potency and improved DMPK properties led to compounds 71 and 84, which displayed in vitro enzyme potencies >10-fold improved over the best HTS hits.

As the extent of inhibition depends on the nature of inhibition (competitive, uncompetitive, mixed), the current technology can also be exploited to choose the most effective class of inhibitors and, to a certain extent, reduce the chances of failure in translating nanomolar enzyme potencies into MICs.

Variation of substitutions at the P2 significantly affected the enzyme inhibitory potency of the inhibitors.