Figure 2 | Scientific Reports

Figure 2

From: Determining direct binders of the Androgen Receptor using a high-throughput Cellular Thermal Shift Assay

Figure 2

Cellular target engagement of AR agonists or antagonists by CETSA HT. (a) An in-cell CETSA HT thermal melt curve confirming thermal stabilisation of AR upon addition of the agonist dihydrotestosterone (DHT), but no stabilisation in the presence of the antagonist Enzalutamide. Data is the mean ± SD of one replicate, n = 4. (b) ITDRFCETSA experiments at 46 °C to determine the potency of agonist target engagement. R1881 EC50 = 1.2 nM, Testosterone EC50 = 1.7 nM, Andrenosterone EC50 = 50.6 nM. Data is the mean ± SD of two technical replicates. (c) ITDRFCETSA experiments at 46 °C in the presence of 1 nM DHT to determine the potency of antagonist target engagement. Enzalutamide IC50 = 666.8 nM, ARN-509 IC50 = 20.6 nM. Data is the mean ± SD of one replicate, n = 6.