Table 1 Comparative study for compound activity in an ARE-Luciferase reporter assay for AR-driven transcription and compound activity in CETSA HT. Raw data is reported in Supplementary Table S1.

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

Compound Target and expected mode-of-action AR-driven transcription (ARE-Luciferase), 24 h, IC50 (µM) AR target engagement (CETSA HT), 2 h, IC50 (µM)
Enzalutamide AR antagonist 0.100 0.288
Hydroxyflutamide AR antagonist 0.135 0.046
MK-2866 AR antagonist 0.170 0.089
MI-136 Inhibitor of AR co-regulator Menin 7.4 >30
MI-503 Inhibitor of AR co-regulator Menin 11.0 >30
Danusertib Kinase inhibitor with activity against the AR co-regulator TrkA 2.6 >30
Entrectinib Kinase inhibitor with activity against the AR co-regulator TrkA 11.2 >30
Bayer inhibitor Kinase inhibitor with activity against the AR co-regulator TrkA 2.8 >30
JQ1 Inhibitor of AR co-regulator BRD4 0.302 >30
OTX-015 Inhibitor of AR co-regulator BRD4 0.214 >30
Onalespib Inhibitor of AR chaperone Hsp90 0.537 Reduces total AR
Tanespimycin Inhibitor of AR chaperone Hsp90 3.2 Reduces total AR
NVP-AUY-922 Inhibitor of AR chaperone Hsp90 0.089 Reduces total AR
Niclosamide AR downregulator 0.955 Reduces total AR
ACS-J9 AR downregulator >10 >30
Ailanthone Inhibitor of p23, mediator of AR-Hsp90 interaction 0.087 >30
WNT-974 Inhibitor of Tankyrase component of the WNT signalling pathway >30 >30
XAV-939 Inhibitor of Porcupine component of the WNT signalling pathway >30 >30
GSK-126, EPZ-6438, EED-226, A-395, GSK8814 Inhibitors of AR co-regulators EZH2/ATAD2 >30 >30
GSK2879522 Inhibitor of AR co-regulator LSD1 >30 >30
Abiraterone Inhibitor of CYP17A, a key component of nongonadal androgen synthesis >30 >30