. Author manuscript; available in PMC: 2022 Sep 23.

Published in final edited form as: J Med Chem. 2021 Sep 13;64(18):13902–13917. doi: 10.1021/acs.jmedchem.1c01294

Table 1:

SAR with aliphatic pyridazinones and BPTF


	R	BPTF AlphaScreen IC₅₀ (μM)	L.E.

GSK 4027		1.5 ± 0.2³⁶	0.35

1		10 ± 2³⁶	0.45

2		31³⁶	0.41

3		19³⁶	0.38

4		8.7	0.49

5		7.7	0.41

AlphaScreen values were an average of two technical replicates with N = 1, except for GSK4027 and 1 which were averages of six and three experimental replicates, respectively. Binding isotherms shown in Figure S2.