Sentence examples for binding potency and selectivity from inspiring English sources

We demonstrated that compounds in which the amine had been exchanged for an ether or a thioether retained binding potency and selectivity.

Of these, (3R -7-hydroxy-N- 1S -2-methyl-[4-methyl-4-pyridine-3-yl-carboxamide (3R -7-hydroxy-N- 1S -2-methyl-[4-methyl-4-pyridine-3-yl-carboxamideGTPγS functional assay, with a Ke = 0.18 nM at the KOR and 273R -7-hydroxy-N- 1S -2-methyl-[4-methyl-4-pyridine-3-yl-carboxamideDOR, respectively.

These compounds have a high binding potency and selectivity for one of the p53 binding sites on Mdm2.

Studies of linker strand-binding adenine isosteres identified SAR trends in potency and selectivity that were consistent with binding interactions observed in structures of the inhibitors bound to AKT1 and to the counter-screening target PKA.

In addition, an enormous amount of kinase-targeting medicinal chemistry has been enabled by structural biology studies that can help elucidate the binding modalities of compounds and assist in improving potency and selectivity profiles by informing key contacts between inhibitor and target.

Novel zinc binding groups (ZBGs) represent a novel strategy to obtain optimal potency and selectivity for zinc metalloproteases inhibitors.

It was hypothesised that the potency and selectivity of imatinib could be improved by maintaining binding to the inactive conformation of the Abl kinase domain, but incorporating alternative binding groups to the N-methylpiperazine moiety, while preserving an amide pharmacophore to retain H-bond interactions to Glu286 and Asp381.

The cell-free and cell-based assay data showed that both potency and selectivity changed with the change in zinc-binding group.

Collectively, these studies describe the synthesis, activity and binding mode of a new series of non-covalent proteasome inhibitors with unprecedented potency and selectivity for the β5 site, and which can discriminate between the constitutive proteasome and immunoproteasome in vitro and in cells.

A proposed protein ligand binding mode for this compound is also provided to rationalise the high levels of potency and selectivity over inhibition of related sodium channels.

While the mechanism for this distinction at mGlu7 is not known, it has been proposed that the enhanced potency and selectivity of LSP4-2022 at mGlu4 is generated by occupation of an additional binding pocket in the N-terminal domain.