Table 3Summary of in vitro ADME properties of ML315

Aqueous Solubilitya

(μg/mL, μM)
Assay Media Solubilityb

(μg/mL, μM)
PAMPA Pec

(×10−6 cm/s) (@ Donor pH)
Plasma Protein Binding
(% Bound)
Plasma Stabilityd

Human/Mouse 1:1 Plasma:PBS
Hepatic Microsome Stabilitye

Human/Mouse
Hepatic Toxicityf

LC50 (μM)
Human
1μM/10μM
Mouse
1μM/10μM
0.43/1.150.64/1.712224 (5.0)
1355 (6.2)
1154 (7.4)
99.35/99.7899.49/99.4785.50/86.671.3/0.54>50
a

in 1× PBS, pH 7.4

b

in 25 mM Tris, 10 mM MgCl2, 0.5 mM EGTA, 2.5 mM DTT, 0.01% TritonX-100, pH 7.5)

c

in aqueous buffer (pION),; Donor compartment pH 5.0/6.2/7.4; Acceptor compartment pH 7.4 @ RT

d

% remaining at 3 hr @ 37°C

e

% remaining at 1 hr @ 37°C

f

towards Fa2N-4 immortalized human hepatocytes

From: Identification of selective inhibitors of cdc2-like kinases 1 and 4 (Clk1, Clk4)

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.