. Author manuscript; available in PMC: 2024 Jun 8.

Published in final edited form as: J Med Chem. 2023 May 17;66(11):7454–7474. doi: 10.1021/acs.jmedchem.3c00176

Table 2.

Structures and DC₅₀ Values for PTD10 Analogs with Modifications to the E3 Ligase Ligand and Linker Attachment Site



Compounds	CRBN E3 Ligase Ligand	DC₅₀ (nM) Ramos cells^a	D_max (%) Ramos cells^a	DC₅₀ (nM) JeKo-1 cells^a	D_max (%) JeKo-1 cells^a
PTD12		3.6 ± 1.2	89.8	4.6 ± 1.4	89.2
PTD13		>3000	30.1	>3000	30
PTD14		1.7 ± 0.4	96.2	3.1 ± 0.6	97
PTD16		0.9 ± 0.2	97.3	0.8 ± 0.2	97.6

Cells were treated with PROTACs at concentrations from 3000 nM to 0.15 nM (3-fold dilutions) for 17 h. Western blots were used to quantify BTK levels by normalizing to β-actin. DC₅₀ values are reported as the mean ± standard deviation from two independent experiments.