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. 2023 Dec 7;39(1):2288810. doi: 10.1080/14756366.2023.2288810

Table 3.

Protein binding inhibition rate of each compound for MDM2 and MDMX.

Inline graphic
Compound R1 R2 R3 Protein binding inhibition at 1 μM(%) a
MDM2 MDMX
Nintedanib — — — 60.6 ± 3.1 76.5 ± 5.5
H1 H H OMe 31.4 ± 0.6 18.2 ± 2.7
H2 Cl H OMe 38.7 ± 1.0 21.3 ± 2.1
H3 H Cl OMe 72.8 ± 5.6 57.9 ± 6.1
H4 F H OMe 42.1 ± 3.3 15.4 ± 2.3
H5 H F OMe 56.8 ± 1.9 16.8 ± 3.1
H6 F Cl OMe 50.3 ± 2.5 13.1 ± 2.7
H7 H Cl graphic file with name IENZ_A_2288810_ILG0010_B.jpg 52.6 ± 2.1 34.1 ± 0.6
H8 H Cl graphic file with name IENZ_A_2288810_ILG0011_B.jpg 18.7 ± 0.8 25.6 ± 2.2
H9 H Cl graphic file with name IENZ_A_2288810_ILG0012_B.jpg 19.3 ± 1.5 21.2 ± 4.5
H10 H Cl graphic file with name IENZ_A_2288810_ILG0013_B.jpg 16.5 ± 2.8 23.8 ± 3.1
H11 H Cl graphic file with name IENZ_A_2288810_ILG0014_B.jpg 48.4 ± 4.6 15.4 ± 1.7
a

The protein binding inhibition at 1 μM of the compound was evaluated in a competitive fluorescence polarisation assay with the corresponding proteins in triplicate. Data are presented as mean ± SD.