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While a handful of leads have been discovered with potencies in the nanomolar range, there is typically limited selectivity over the human homologue, and host cell toxicity effects are variable.
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The D2/D3 agonist radioligand [11C]--PHNO is currently the most suitable D3 imaging agent available, despite its limited selectivity for the D3 over the D2.
Various agents have been synthesized and proved useful for the National Cancer Institute's anticancer testing as potential new drugs, but most agents suffer side effects from their limited selectivity against cancer cells over healthy ones.
Given the limited selectivity of current small molecule tyrosine kinase inhibitors, studies of more selective antagonists are underway.
At the best they are permitted a limited selectivity as consumers.
While over the last years, inhibition of phosphorylation has evolved into a key strategy in targeted therapies, the development of clinically relevant phosphatase inhibitors still faces major bottlenecks and is often plagued by limited selectivity and unfavorable pharmacokinetics.
Cell membrane permeability and limited selectivity highlight their advantages and disadvantages, respectively.
Consistent with these views, other studies performed in vivo with these compounds have also shown limited selectivity [31].
Quinoxalinediones such as CNQX and NBQX show limited selectivity between AMPA and kainate receptors.
A drawback of the dosimeter used in this study is the limited selectivity to differentiate between the three frequency ranges.
Compound 6 (Cdk1/2 inhibitor III) was the most selective (18-fold) for PKN2 over PKN1 with only minimal selectivity over PKN3.
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