Table 2. Hit Rates in the Primary High-Throughput Screen (HTS).
% of GCPII Bindinga | mP | Number of hits at 1 μMb | Number of hits at 60 μMc | Autofluorescent Compoundsd |
---|---|---|---|---|
>90% | <88 | 0 | 6 | 3 |
>75% | <130 | 0 | 12 | 5 |
>50% | <215 | 10 | 65 | 19 |
>30% | <281 | 15 | 119 | 28 |
>25% | <300 | 18 | 166 | 30 |
A library of nearly 20 000 compounds was screened and data were normalized with the b-score algorithm. GCPII, glutamate carboxypeptidase II.
Hits were identified using different cutoffs based on the percentage of probe displacement from the GCPII protein according to mP values.
Number of hits in the 1-μM screen.
Number of hits in the 60-μM screen.
Number of active compounds in the HTS showing at least 5 times higher autofluorescence than the background.