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It then addresses analog testing, including DC and AC parametric testing.
Advantages of adaptive error thresholds over constant or relative error thresholds in analog testing applications are discussed.
This knowledge will be applied to future Desert RATS field tests, and other Earth based analog testing for space exploration, to continue the evolution of manned space operations in preparation for human planetary exploration.
Analog testing identified CsA-related compounds with higher anti-HBV potency than CsA.
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This appeared to correlate with the agonistic potential of the analog tested, as CD40L and IFNγ were also induced with high doses of the weak adamantanoyl agonist (Figure 6B).
Furthermore, the oxidation state of the thioether group appears critical as no activity could be observed with the sulfone analog (tested at ≤30 μM, data not shown).
Six of the 23 analogs tested possessed an NPY Y2 IC50 ⩽ 15 nM.
Of all the analogs tested, 8d was stable in hamster, mouse and human liver microsomes but lost the efficacy with an IC50 of 6.42 μM.
We profiled the best tankyrase-inhibiting 2-PQs against a panel of tankyrase and Wnt-related kinases and most of the analogs tested were significantly more potent against tankyrases than kinases, while one analog, compound 42, showed similar inhibition of TNKS2 and CDK9 as well as Akt kinase.
By contrast, all analogs tested supported increased intracellular sialic acid production within 2 h establishing that esterase processing once the analogs are taken up by cells is not rate limiting.
Among these analogs tested, compound 1d possessing an isopropyl group at the amino terminal afforded an increased antimycobacterial activity with a MIC value of 8 μg/mL in comparison with SSA.
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