Table 1. Selected SERD Properties.
agonist/antagonist
profile |
|||||||
---|---|---|---|---|---|---|---|
molecular type | DC50 MCF-7 | Dmax MCF-7 | IC50 (antiproliferation) MCF-7 | breast | uterus (% of control w. wt) | bone | references |
Steroidal | |||||||
ICI 164,383 | >95% | 39 nM | antagonist | 40–50% | antagonist | (3c, 5a, 22a) | |
ICI 182,780 | 0.4 nM | >95% | 0.6 nM | antagonist | 42% | antagonist | (5a, 5b, 12a, 12c) |
Acrylic Acids | |||||||
GW5638/GW7604 | 390 nM/1.7 nM | 82%/86% | 985 nM/5 nM | antagonist | weak antagonist | agonist | (12a) |
GDC-0810 | 0.7 nM | 87% | 2.5 nM | antagonist | weak antagonist | agonist | (12a) |
AZD9496 | 0.14 nM | >95% | 0.04 nM | antagonist | weak agonist | unknown | (12b, 12c) |
Basic Side Chain | |||||||
RAD1901 | 1.5 nM | ∼70% | 8.9 nM | antagonist/agonist | weak agonist | unknown | (15b, 22b) |
bazedoxifene | 10 nM | ∼70% | 0.24 nM | antagonist | weak agonist | agonist | (15c, 16) |
GDC-0927 | 0.3 nM | 97% | 0.2 nM | antagonist | ∼60% | unknown | (22c, 22d) |
GDC-9545 | 0.04 nM | 84% | 0.26 nM | antagonist | ∼50% | unknown | (23a) |
AZD9833 | 0.16 nM | 99% | 5.0 nM | antagonist | not reported | unknown | (19b) |
PROTACs | |||||||
ARV-471 | 0.9 nM | >95% | not reported | antagonist | ∼45% | unknown | (23b) |
ERD-308 | 0.17 nM | >99% | 0.77 nM | antagonist | not reported | unknown | (23c) |