AR construct | IC50 of VPC-13566 Inhibition (μM) | EC50 of DHT activation (nM) | EC50 of estradiol activation (nM) | EC50 of progesterone activation (nM) | EC50 of hydrocortisone activation (nM) |
---|---|---|---|---|---|
WT | 1.73 | 0.05 | >500 | 104.0 | >500 |
L702H | 6.13 | 8.00 | >500 | 172.0 | 25.0 |
V716M | 1.06 | 0.14 | >500 | 329 .0 | >500 |
V731M | 0.99 | 0.09 | >500 | 115.0 | >500 |
W742L | 2.29 | 33.60 | >500 | >500 | >500 |
W742C | 3.43 | 4.74 | >500 | 293.0 | >500 |
H875Y | 1.34 | 0.14 | 68.0 | 10.20 | >500 |
H875Q | 0.79 | 0.43 | >500 | >500 | >500 |
F877L | 0.37 | 0.08 | >500 | >500 | >500 |
T878A | 2.56 | 0.06 | 144.0 | 0.57 | >500 |
T878S | 0.43 | 0.02 | 100.0 | 0.53 | >500 |
D880E | 1.14 | 0.11 | >500 | 177.0 | >500 |
L882I | 0.84 | 0.20 | >500 | >500 | >500 |
S889G | 10.48 | 0.37 | 230.0 | 17.20 | >500 |
D891H | 2.35 | 0.12 | 173.0 | 31.0 | >500 |
E894K | 1.20 | 0.25 | >500 | 143.0 | >500 |
M896V | 0.59 | 4.50 | >500 | >500 | >500 |
M896T | 0.10 | >500 | >500 | >500 | >500 |
E898G | 1.24 | 0.45 | >500 | >500 | >500 |
T919S | 1.29 | 0.03 | >500 | 123.0 | >500 |
H875Q/T919S | 0.63 | 0.18 | >500 | >500 | >500 |
T878A/S889G | 13.20 | 0.12 | 94.0 | 0.36 | >500 |
T878A/D891H | 13.40 | 0.40 | 100.0 | 0.49 | >500 |
H875Y/T878A | 10.80 | 1.26 | 63.0 | 0.66 | 105.0 |
F877L/ T878A | 11.70 | 0.81 | >500 | 5.70 | >500 |