Molecular decoration of lead compounds led to inhibitors exhibiting a potency, measured by the Thioflavin T fluorimetric assay, ranging from high to low micromolar IC50.
Efficacy study of CLX-103 in acute dextran sodium sulfate (DSS) mouse colitis model showed improved potency measured as Disease Activity Index (DAI) and histological scores in the colon as compared to sulfasalazine.
The summarized TTR-binding potency of the individual fractions was ca 50%% of the total TTR-binding potency measured in the unfractionated extract.
Using a classical PK/PD modelling approach, the cimicoxib efficacy (expressed as a percentage of return to control values) and the cimicoxib potency (measured by the plasma EC50/IC50) were determined.
For HL cytosol, expressed SULT1A1*1, SULT1A1*2, and SULT1E1, we investigated the relationship between inhibitory potency, measured at 0.1 μM 3-OH-BaP, and each of several physicochemical properties of the 4-OH-PCBs.
This activity scheme uses as its base dose potency measured as TD50 which after conversion into an inverse log scale, a decile scale, is adjusted by weighting factors that described other parameters of carcinogenic activity.
In close agreement with the high potency measured in the reporter assay, ISRIB significantly reduced SG formation even at concentrations as low as 2 nM in U2OS cells and as expected, an inactive analog, ISRIBinact, did not reduce their formation.
Holst et al. showed that the potency measured after lipogenesis for 2 h correlated poorly with the amount of analogue bound at the time where lipogenesis is measured ("equilibrium") but correlated strongly with the relative amounts of analogue bound within the first few minutes of incubation (50).
Briefly, we assigned each pesticide a hazard score based on two carcinogenicity measures (cancer class and potency) and two exposure potential measures (field volatilization flux and half-life).
