With the growing interest in developing PPARγ inverse agonists for bladder cancer therapeutics, including a covalent analog that is currently in phase 1 clinical trials40,41, our findings demonstrate a platform that can assess, explain, and potentially predict the cellular transcriptional activity of PPARγ compounds ranging from agonism to inverse agonism via biochemical and NMR-detected structural biology studies focused on the PPARγ LBD. The gene discussed is PPARG; the disease is urinary bladder cancer.