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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 5:

Aromatic pyridazinones with 2-position N-alkyl substituents

graphic file with name nihms-1794605-t0038.jpg
R’’ BPTF
AlphaScreen
IC50 (μM)		 BRD4(1)
AlphaScreen
IC50 (μM)
10 CH3 0.29 42
23 graphic file with name nihms-1794605-t0039.jpg 0.55 35
24 graphic file with name nihms-1794605-t0040.jpg 0.38 71
25 graphic file with name nihms-1794605-t0041.jpg 0.79 NB

AlphaScreen values were an average of two technical replicates with N =1. NB indicates that the compound was non-binding up to 250 μM. Binding isotherms shown in Figure S4–5.