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. 2020 Feb 27;477(4):787–800. doi: 10.1042/BCJ20190826

Table 1. Kd and IC50 values for series of inhibitors (4–10) and SAH against PRMT1 and CARM1 measured using ITC and enzyme activity assays, respectively.

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Inhibitor Kd ± standard error (µM) IC50 (95% confidence interval) (µM)
PRMT1 CARM1 PRMT1 CARM1
4 10.2 ± 0.996 3.32 ± 0.335 7.2 (3.5–15.0) 2.3 (1.8–3.0)
5 4.02 ± 0.453 7.18 ± 0.557 11.8 (9.0–15.5) 8.7 (6.9–10.8)
6 9.99 ± 1.89 9.80 ± 1.83 11.6 (4.9–27.2) 17.7 (13.5–23.2)
7 32.2 ± 3.531 38.1 ± 9.61 22.0 (14.4–33.5) 24.1 (15.4–37.6)
8 10.2 ± 4.21 2.30 ± 0.162 22.0 (15.7–30.8) 0.7 (0.5–1.0)
9 15.3 ± 1.57 1.14 ± 0.411 11.1 (5.6–21.8) 0.3 (0.1–1.1)
10 43.7 ± 14.92 1.11 ± 0.132 25.3 (17.3–37.0) 0.8 (0.6–1.0)
SAH 0.709 ± 0.057 0.775 ± 0.111 0.5 (0.2–1.0) 0.2 (0.1–0.4)
1

Stoichiometry fixed to 0.5.

2

This Kd is derived from a competition experiment with SAH as the Kd was not accessible through direct titration.