Structures of the AGP and HSA Validation Set.

<p>Structures of the AGP and HSA Validation Set.</p

HSA and AGP IC₅₀ and K_d value comparisons for the 10-compound validation set.

<p>–: no activity exhibited.</p><p>NC: Ratio could not be calculated.</p>1<p>Based on literature.</p

Validation Set Testing.

<p>A) IC₅₀ and K_d values for the Validation Set in 1,536-well (▪), 96-well (▪), and protein coated bead (□) AGP assays; B) the corresponding results for the HSA assays.</p

AGP Assay Protocol for 1,536-well Format.

<p>AGP Assay Protocol for 1,536-well Format.</p

Top LOPAC¹²⁸⁰ Hits.

1<p>Top compound concentrations of 144 or 151 µM for the AGP and HSA assays, respectively.</p

LOPAC¹²⁸⁰ Screen.

<p>The robust AGP (•) and HSA (o) screen performance as represented by the reproducible high Z’-factor trend.</p

Fluorescence polarization assay.

<p>A) assay principle; B) structures of the fluorescent AGP and HSA probes Dipyridamole and Dansyl sarcosine, respectively.</p

HSA Assay Protocol for 1,536-well Format.

<p>HSA Assay Protocol for 1,536-well Format.</p

Structures of the top hits from the AGP and HSA LOPAC¹²⁸⁰ Screen.

<p>Structures of the top hits from the AGP and HSA LOPAC¹²⁸⁰ Screen.</p

HSA Assay Miniaturization to 1536-well Format.

<p>A) whole-plate scatter plot obtained from 10 µM HSA/3 µM Dansyl sarcosine mix (•) and 3 µM Dansyl sarcosine (○); B) concentration-response profiles of Naproxen (•) and Phenylbutazone (○) in 1536-well format.</p