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Thus, a screening system for anti-SARS-CoV agents was developed, which evaluated compound potency, specificity and cytotoxicity at the initial screening phase.
After the initial screening, potential "hits" were optimized by medicinal chemistry and tested for potency, specificity, and toxicity.
However, none has reached the clinic due to lack of potency, specificity, bioavailability or easy access due to structural complexity [22], [23].
The potency, specificity and toxicity of the substances were compared.
In vitro the potency, specificity and species selectivity of CAT-354 was assayed in TF-1 cells, human umbilical vein endothelial cells and HDLM-2 cells.
Romidepsin has high potency specificity for HDAC1 and HDAC2, but there is no published data on the effect on latent HIV.
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A number of small molecules, which could inhibit the intrinsic tyrosine kinase activity of VEGFR, have been reported previously with a range of nanomolar potencies, specificities, and pharmacokinetic properties [ 15– 17].
Several CHK1 inhibitors, with different potencies, specificities and activities are currently undergoing clinical trial (reviewed in Ma et al, 2011) and ATR inhibition is likely to have different therapeutic activity compared with the CHK1 inhibitors.
They proved to be reasonably potent and fairly specific, with potency to specificity ratios of 7.98 and 6.42, respectively.
Among the purified malleins, the number 1 showed the best specific activity, with a potency to specificity ratio of 7.98, and the number 3 showed the worse specific activity, with a potency to specificity ratio of 2.63.
One must be wary of trading potency for specificity, as targeting very specific amino acid sequences in highly mutated tumors may result in killing only a subgroup of cells.
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