Table 2uHTS campaign summary and results

StepScreen typeTargetNumber of compounds testedSelection criteriaNumber of selected compoundsPubChem AIDcAssay statistics
Z′S/B
1Primary screenSTAT3194698%Inha>43.4%17238620.846.22
2ConfirmationSTAT31215%Inhb>43.4%54412650.888.04
3aSelectivityNF-kB544Inactive in both the NF-κB and STAT1 assays10513080.8717.60
3bSTAT11058713170.877.29
4aTitrationSTAT3122Active in the STAT3 assay and inactive in the STAT1 assay11613990.826.88
4bSTAT114110.8614.58
a

The primary screen hit-cutoff was calculated at the average percent activation of all test compounds plus three times the standard deviation.

b

The hit-cutoff calculated for the primary run was also applied to the confirmation run.

c

PubChem AIDs are accessible on-line at http://www​.ncbi.nlm.nih​.gov/sites/entrez?db​=pcassay&term=xxxx, where xxxx represents the PubChem AID number listed in the table.

From: Modulators of STAT Transcription Factors for the Targeted Therapy of Cancer (STAT3 Inhibitors)

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

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