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. 2021 Mar 30;6(14):9334–9343. doi: 10.1021/acsomega.0c06362

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)