ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound)
Methods employed in this study have been adapted from the scientific literature to maximize reliability and reproducibility.Reference standards were run as an integral part of each assay to ensure the validity of the results obtained. Assays were performed under conditions described in the accompanying "Methods" section of this report.Where presented, IC50 values were determined by a non-linear, more ..
Assay Provider: P Jeffrey Conn
Assay Provider Affiliation: Vanderbilt University
Methods employed in this study have been adapted from the scientific literature to maximize reliability and reproducibility.Reference standards were run as an integral part of each assay to ensure the validity of the results obtained. Assays were performed under conditions described in the accompanying "Methods" section of this report.Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (IDBusiness Solutions Ltd., UK). Where inhibition constants (Ki) are presented, the Ki values were calculated using the equation of Cheng and Prusoff (Cheng, Y., Prusoff, W.H., Biochem. Pharmacol. 22:3099-3108, 1973) using the observed IC50 of the tested compound, the concentration of radioligand employed in the assay, and the historical valuesfor the KD of the ligand (obtained experimentally at Eurofins Panlabs, Inc.). Where presented, the Hill coefficient (nH),defining the slope of the competitive binding curve, was calculated using MathIQTM. Hill coefficients significantly different than 1.0, may suggest that the binding displacement does not follow the laws of mass action with a single binding site.Where IC50, Ki, and/or nH data are presented without Standard Error of the Mean (SEM), data are insufficient to be quantitative, and the values presented (Ki, IC50, nH) should be interpreted with caution.
Panel Assay with Multiple Targets/Outcomes
§ Panel component ID.
Biochemical assay results are presented as the percent inhibition of specific binding or activity throughout the report. All other results are expressed in terms of that assay's quantitation method.1:For primary assays, only the lowest concentration with a significant response judged by the assays' criteria, is shown in this summary.2:Where applicable, either the secondary assay results with the lowest dose/concentration meeting the significance criteria or, if inactive, the highest dose/concentration that did not meet the significance criteria is shown.3:Unless otherwise requested, primary screening in duplicate with quantitative data (e.g., IC50 +/- SEM, Ki +/- SEM and nH)are shown where applicable for individual requested assays. In screening packages, primary screening in duplicate with semi-quantitative data (e.g., estimated IC50, Ki and nH) are shown where applicable (concentration range of 4 log units);available secondary functional assays are carried out (30 mM) and MEC or MIC determined only if active in primary assays >50% at 1 log unit below initial test concentration.Significant responses (>/= 50% inhibition or stimulation for Biochemical assays) were noted in the primary assays listed below: No Significant Results