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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 4:

Aromatic pyridazinones with extended basic group

graphic file with name nihms-1794605-t0032.jpg
R R’ BPTF
Alpha
Screen
IC50 (μM)
L.E.

18
(BZ1)
graphic file with name nihms-1794605-t0033.jpg Cl 0.067 ± 0.01 0.51

19 graphic file with name nihms-1794605-t0034.jpg Cl 0.17 0.44

20 graphic file with name nihms-1794605-t0035.jpg Cl 10 0.32

21 graphic file with name nihms-1794605-t0036.jpg Br 0.036 ± 0.008 0.53

22 graphic file with name nihms-1794605-t0037.jpg Cl 0.056 ± 0.01 0.45

AlphaScreen values were an average of two technical replicates, with N = 1 except for 18 (BZ1) which was an average of seven experimental replicates and 21–22 which were averages of three experimental replicates. Binding isotherms shown in Figure S4.