The biochemical half maximal inhibitory concentration (IC50) is the most commonly used metric for on-target activity in lead optimization. It is used to guide lead optimization, build large-scale chemogenomics analysis, off-target activity and toxicity models based on public data. However, the use of public biochemical IC50 data is problematic, because they are assay specific and comparable onl...

This paper proposes an effective methodology for the determination of the half maximal (50%) inhibitory concentration (IC50) by using microfluidic device that generates logarithmic concentration gradients. Dose-response curve is obtained with respect to the concentrations in a logarithmic scale. Although we have presented a high-throughput analysis of ATP binding cassette transporter (ABC-trans...

Theunit ofACE inhibitory activity of identified substances in the Abstract, Results and Discussion, and Table 3 should be corrected to (IC50, μM). The correct ACE inhibitory activities are as follows: Ala-Trp, IC50=10 μM;Gly-Trp, IC50=30 μM;Ala-Tyr, IC50= 48 μM; Ser-Tyr, IC50= 67 μM;Gly-Tyr, IC50= 97 μM; Ala-Phe, IC50=190 μM;Val-Pro, IC50=480 μM;Ala-Ile, IC50=690 μM; Val-Gly, IC50 = 1100 μM; an...

Phenoxyacetohydrazide Schiff base analogs 1-28 have been synthesized and their in vitro β-glucouoronidase inhibition potential studied. Compounds 1 (IC50=9.20±0.32 µM), 5 (IC50=9.47±0.16 µM), 7 (IC50=14.7±0.19 µM), 8 (IC50=15.4±1.56 µM), 11 (IC50=19.6±0.62 µM), 12 (IC50=30.7±1.49 µM), 15 (IC50=12.0±0.16 µM), 21 (IC50=13.7±0.40 µM) and 22 (IC50=22.0±0.14 µM) showed promising β-glucuronidase inhi...

The effects of various inhibitors on crude, commercial and partially purified commercial mushroom tyrosinase were examined by comparing IC(50) values. Kojic acid, salicylhydroxamic acid, tropolone, methimazole, and ammonium tetrathiomolybdate had relatively similar IC(50) values for the crude, commercial and partially purified enzyme. 4-Hexylresorcinol seemed to have a somewhat higher IC(50) va...

The leaves from Aglaia andamanica were determined for their anti-allergic and anti-inflammatory effects using RBL2H3 and RAW264.7 cells, respectively. Among the isolated compounds, 24-epi-piscidinol A (5) exhibited the highest antiallergic activity against -hexosaminidase release with an IC50 value of 19.8 M, followed by (-)-yangambin (3, IC50 = 33.8 M), pyramidaglain A (8, IC50 = 37.1 M), ...