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. Author manuscript; available in PMC: 2019 Feb 19.
Published in final edited form as: Bioorg Med Chem. 2018 Mar 19;26(11):2984–2991. doi: 10.1016/j.bmc.2018.03.030

Figure 3.

Figure 3

Screening of AMI analogues for binding and catalytic inhibition of KDM5A. (A) AlphaScreen assay for H3K4me3 and His-KDM5A(PHD3) interactions. (B) Normalised dose-response inhibition curves for displacement of H3K4me3-Bn from KDM5A(PHD3) by representative AMI derivatives. Average ± StdDev (N ≥ 3 independent replicates). (C, D) Dose-response inhibition curves of H3K4me3 demethylation activity by AMI derivatives for KDM5A using a MALDI-TOF MS-based assay. AMI derivatives were tested against two active KDM5A constructs, KDM5A_c1 (M1-L801), and KDM5A_c2 (ΔARID/PHD1, L88-G353). KDOAM25a is a small molecule JmjC-domain inhibitor of KDM5.