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. Author manuscript; available in PMC: 2019 Dec 20.
Published in final edited form as: J Med Chem. 2019 Aug 1;62(16):7557–7574. doi: 10.1021/acs.jmedchem.9b00869

Table 1.

Effects of Modifications to the Triazine Core on Allosteric Activityb

graphic file with name nihms-1062982-t0002.jpg
compd R1 R2 Log (α) Log (β) −Log (KB) Log (αβ/KB) Δ
1 H H 0.60 ± 0.10 0.36 ± 0.07 4.35 ± 0.12 5.31 ± 0.05 0.00
5 H Me 0.48 ± 0.10 0.37 ± 0.16 4.51 ± 0.07 5.36 ± 0.06 0.05
6 H Et 0.47 ± 0.12 0.25 ± 0.13 4.63 ± 0.17 5.34 ± 0.09 0.03
7 Me Me Inactive
10a graphic file with name nihms-1062982-t0003.jpg Weak PAM
a

The structure of 10 is shown.

b

Values represent means ± standard error of the mean (SEM) from a minimum of three independent assays, each in triplicate or quadruplicate. Δ stands for the difference of Log(αβ/KB) from that of 1, positive values indicated increased allosteric activity and negative values indicated reduced allosteric activity. Proton concentration-response curves are shown in Supporting Figure 1.