Sentence examples for potency of the initial from inspiring English sources

Structure-based design aided in optimizing the potency of the initial lead (2, IC50 of 11 μM) to a potent (11l, 190 nM) EGLN-1 inhibitor.

Optimization of initial peptidic leads resulted in the development of several classes of small molecule inhibitors, which have comparable potency to the initial peptidomimetics, while eliminating the remaining amino acid residues.

One of the top-scored molecules was synthesized and shown to have similar potency to the initial hit.

The potency of the weak initial lead structure was enhanced using library-based SAR methods.

The other six compounds, which were selected for further evaluation on the basis of their apparent potency in the initial screen and their structural diversity, were sulconazole, suloctidil, nerolidol, dioxybenzone, hexylresorcinol and retinyl acetate.

Compound 23 showed similar potency and LE as those of the initial hit 14, and lacks the metabolically and chemically labile ester functional group.

Most of them (30 out of 35) showed an inhibitory potency higher than the initial screening hit 1a (IC50 = 74 μM).

It is likely that additional determinant(s) controls the potency of the late restriction activity following initial binding of a TRIM protein with HIV-1 Gag.

SAR analysis was performed to further improve antiviral potency and to optimize drug-like properties of the initial hits.

Amongst the modifications explored, a 1,3,4-triazole ring (as in compound 4) as a replacement of the initial pyrazole provided good potency against PI3Kα, with excellent kinase selectivity.

Several issues of the initial lead structures had to be resolved, such as potency, selectivity over related GPCRs and P-gp efflux limiting brain exposure in this series.