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. Author manuscript; available in PMC: 2026 Sep 13.
Published in final edited form as: Eur J Med Chem. 2025 Oct 4;301:118228. doi: 10.1016/j.ejmech.2025.118228

Table 1.

illustrates in vitro DMPK values for new TG2 PROTACs P374, P404, and P405 showing mouse microsomal stability, PAMPA permeability, and solubility. Compound MT4 was reported previously and is the small molecule TG2 inhibitor control. Compounds 7 and 11 are TG2 PROTACs we recently reported (29).
Microsomal Stability PAMPA Permeability Kinetic Solubility Equilibrium Solubility
Compound ID T1/2 (min) Clint (μl/min/mg) (10−6 cm*s−1) (μM) (μM)
MT4 15.2 46 2.60 54.96 0.76
Compound 7 12.4 56 0.00 1.19 0.24
Compound 11 18.4 38 0.90 9.95 0.17
P374 21.5 32 0.51 0.36 0.06
P404 11.6 60 0.63 0.63 0.01
P405 16.1 43 0.77 0.27 0.02