Sentence examples for improved potency for from inspiring English sources

Among them, (5Z,8Z,11Z,14Z -N- fur-3-ylmethyl)icosa-5Z,8Z,11Z,14Z -N- fur-3-ylmethylbehaves as the most potent endocannabinoid transporter inhibitor described to date (IC5Z,8Z,11Z,14Z -N- fur-3-ylmethyl potency for the anandamide transporter, high selectivity for CB1 and VR1 receptors, and modest selectivity for CB2.

Our results demonstrated a good correlation between computational and experimental data, and all six analogues displayed an improved potency for inhibiting IN binding to LEDGF/p75 in vitro to respect to the parent compound Lavendustin B. Additionally, these analogs show to inhibit weakly LEDGF/p75-independent IN catalytic activity suggesting a multimodal allosteric mechanism of action.

This guided production of an inhibitor with 125-fold improved potency for KLK4 and enhanced selectivity over off-target proteases, including closely related KLKs.

Compounds with a biphenylmethyl group in the positiontion show improved potency for aggrecanase with IC50 values in the low nanomolar range [ 76].

Although neither drug is able to cross the blood brain barrier, their improved potency for targeting xCT made them important tools for further evaluating combination therapy in culture with our cannabinoid-based redox therapeutic, CBD.

In this study, both compounds showed improved potency and selectivity for CD22 (IC50 70 nM) and 712-fold more selective for CD22 than for MAG.

Altogether, our results provide an insight into the SAR of pyrido[2,3-d]pyrimidin-7-ones for the development of drug candidates with improved potency and selectivity for the targeted treatment of CML.

Substitution of the formamide for the 2-fluoro-phenyl ring resulted in WAY-150138 (24) and improved potency ∼20-fold for both viral strains.

These studies suggested that substitutions around the phenoxy ring of this scaffold can impart improved potency and selectivity for MEKK2.

Although the aryl ring at C-4 was not required for activity, its presence improved potency further, as did small lipophilic meta-substituents (L44−45).

Possible binding poses were investigated by in silico modelling, providing a basis for optimisation of fragment binding and improved potency against NDH-2.