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. 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 3:

SAR with aromatic pyridazinones containing different basic groups substitutions for binding to BPTF

graphic file with name nihms-1794605-t0023.jpg
R BPTF
AlphaScreen
IC50 (μM)
L.E.

10 graphic file with name nihms-1794605-t0024.jpg 0.29 ± 0.08 0.50

11 graphic file with name nihms-1794605-t0025.jpg 0.31 0.44

12 graphic file with name nihms-1794605-t0026.jpg 0.25 0.45

13 graphic file with name nihms-1794605-t0027.jpg 0.37 0.44

14 graphic file with name nihms-1794605-t0028.jpg 3.9 0.37

15 graphic file with name nihms-1794605-t0029.jpg 0.80 0.46

16 graphic file with name nihms-1794605-t0030.jpg 0.22 0.50

17 graphic file with name nihms-1794605-t0031.jpg 0.97 0.39

AlphaScreen values were an average of two technical replicates with N = 1, except for 10 where it was an average of three experimental replicates. Binding isotherms shown in Figure S3.