Figure 1
From: ML290 is a biased allosteric agonist at the relaxin receptor RXFP1

ML290 and binding of 125I-H2 relaxin to RXFP1 stably expressed in HEK293 cells. In (A) co-incubation with ML290 (90 min), increased total binding of 125I-H2 relaxin to RXFP1 in a concentration-dependent manner (n = 6). In (B) ML290 (1 μM) had no significant effect on competition by H2 relaxin for 125I-H2 relaxin binding (n = 8). In kinetic studies, ML290 (1 μM) had no significant effect on (C) dissociation (n = 3) or (D) association rate (n = 6–7) of 125I-H2 relaxin from RXFP1. Data are mean ± SEM of ‘n’ experiments.