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Aiming to establish an increased potency, the bioassay results were matched to those of 1,3,4-oxadiazoles, utilized previously.
Other pro-inflammatory mediators like interleukin-1β and tumor necrosis factor-α (TNF-α) were associated with an enhanced sensitivity to the opioid analgesic effect (IL-1β, P = 0.0218; TNF-α, P = 0.0276 .Nocturnal hypoxemia in subjects at high risk for OSA was associated with an increased potency of opioid analgesia.
One of the gem-chlorines on the fused cyclopropane moiety of 2 was eliminated to produce 3, which showed reduced potency for iNOS inhibition, as well as 4 with an increased potency.
Collectively, these experiments support the hypothesis that there is an increased potency and selectivity to be gained in the design of G-quadruplex-stabilizing agents that incorporate multiple interactions.
Similarly, PDGF demonstrated an increased potency toward quiescent SMC migration.
When the targeted agents were used together, an increased potency of the inhibitors was observed.
Similar(46)
On the other hand, 3h demonstrated a significantly increased potency compared to diclofenac in this assay (IC50 = 0.13 μM).
None of them, however, have improvements comparable to WT 331Δ, which has a significantly increased potency (EC50 ratio 2.6, p<0.05 compared to WT).
Compared to currently approved anti-VEGF compounds, DARPins display a significantly increased potency in functional models of angiogenesis.
4-hydroxy tamoxifen has at least 100-fold greater affinity for the ER than tamoxifen, and has a similarly increased potency in anti-proliferative action.
Its measured IC50 in HeLa cells was higher (1.5 μM [ 30]) than measured here in PC3 cells (450 nM; total HDAC activity) suggesting that MI192 may have a slightly increased potency in PC3 cells.
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