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It also demonstrates that SBCAMD is capable of improving potency of an inhibitor lead by nearly one order of magnitude, even for BoNTAe as one of the most challenging protein targets.
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Two distinct pathways of immuno-modulation improve potency of p53 immunization in rejecting established tumors.
Lehár, J. et al. Improved potency of cisplatin by hydrophobic ion pairing.
Molecular modeling was used to improve potency of the cyclohexylamine series.
In an effort to improve potency of the antagonists we synthesized over 200 derivatives and tested these derivatives in the 10T1/2 Super8xTOPflash reporter assay.
Structure activity relationship studies have subsequently attempted to improve potency of Lys-CoA and probe p300 catalysis.
A series of alkylaryl and sulfonylaryl groups, on the IDA basic scaffold, was investigated with the aim of improving potency and selectivity against MMPs involved in degenerative diseases.
To address this issue, we carried out a PET-specific structure activity relationship (SAR) effort with the goal of further improving potency while maintain other properties.
In a series of alkyl and electron withdrawing groups that had improved potency, introduction of trifluoromethyl and chloro groups meta and para, respectively, to the thiourea nitrogen was optimal (30, IC50 0.03 μg/mL).
None of the compounds showed improved potency over that of the parent compounds, with the relatively low potencies limiting the derivation of structure activity relationships.
Lacking insight into the binding mode, initial attempts to improve inhibitor potency failed to improve potency, and synthesis of analogs was further hampered by the presence of a C C bond between the pyrrolidine and pyridine.
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