BI-1230

BI-1675

Jump to DiscoverX top

BI-1230

Cellular agonist effect was calculated as a % of control response to a known reference agonist for each target and cellular antagonist effect was calculated as a % inhibition of control reference agonist response for each target. Results showing an inhibition higher than 50 % are considered to represent significant effects of the probe. The results are expressed as a percent of control agonist response: (measured response/ control response ) * 100 or as a percent inhibition of control agonist response 100-((measured response/ control response) * 100).

Conclusion: Off target inhibition of Human PAR1 in a cell based antagonist effect assay at 10 µM is 59.6 %.

BI-1230

Results showing an inhibition higher than 50 % are considered to represent significant effects of the probe. The results are expressed as a percent inhibition of control specific activity 100-((measured specific activity/ control specific activity) * 100). Low to moderate negative values have no real meaning and are attributable to variability of the signal around the control level. High negative values (≥ 50 %) that are sometimes obtained with high concentrations of test compounds are generally attributable to nonspecific effects of the test compounds in the assays. The following proteases were also tested but the probe interferes with the detection method: ACE (h), ACE-2 (h), BACE-1 (h) (β-secretase), MMP-1 (h), MMP-2 (h), MMP-3 (h), MMP-7 (h), MMP-8 (h), MMP-9 (h), MMP-12 (h), MMP-13 (h), MT1-MMP (h) (MMP-14), TACE (h). (INTER: Test compound interferes with the assay detection method.

Conclusion: The only hit found for BI-1230 within the tested human serine proteases is cathepsin G at 63% inhibition. The Eurofins-Cerep panel for non-serine proteases tested at 10 µM is clean. The control was not tested.