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. 2021 Mar 3;12(4):555–562. doi: 10.1021/acsmedchemlett.0c00547

Table 3. In Vitro Potency Data for Compounds 42–52.

graphic file with name ml0c00547_0012.jpg

Compd R1R2N TAK1 IC50a
42 1-azetidinyl 2.6
43 1-piperidinyl 1.2
44 1-azepinyl 2.9
45 1-(2-methylpyrrolidinyl) 5.7
46 1-(3-methylpyrrolidinyl) 0.9
47 1-(3-fluoropyrrolidinyl) 1.2
48 1-(3-phenylpyrrolidinyl) 2.3
49 1-(3-(OMe)-pyrrolidinyl) >10
50 1-(3-(N-Ac)-pyrrolidinyl) >10
51 1-isoindolinyl 0.3
52 1-octahydro-1H-isoindolinyl 3.4
a

Biochemical Lanthascreen assay with TAK1–TAB1 fusion protein in the presence of 10 μM ATP, mean IC50 values in μM, n = 2.