OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism[1]. IC50: 29 nM (GR)[1]
OP-3633 exhibits low progesterone receptor (PR) agonism with an EC50 higher than 2500 nM[1]. OP-3633 exhibits low androgen receptor (PR) antagonism, with an IC50 of 1135 nM[1].
[1]. Du X, et al. Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633). J Med Chem. 2019 Jul 25;62(14):6751-6764.