If the topic of your question is strictly to determine if a drug has an effect on a defined target you should isolate that target (most probably a protein?!) and do some biochemical activity assay (if it is an enzyme) or binding assay in absence or presence of your drug. If it has an effect on the activity of your target or at least binds to it you may think about the next step and find out whether the in-vitro effect translates in an phenotypic effect in cells (e.g. proliferation).
One could isolate the target by IP (if antibodies are available) for the first step, or isolate the cDNA and express it recombinantly.
If you have a clear idea about your target some more details would be helpful to give a more precise answer.