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. 2021 Feb 11;12(3):380–388. doi: 10.1021/acsmedchemlett.0c00532

Figure 2.

Figure 2

Brain (A) and blood (B) exposure of 12 following oral gavage of compounds to C57/BL6 mice (10, 30, and 100 mg/kg). Left Y axis indicates the measured exposure in the matrix (determined by LC-MS/MS). Right Y axis indicates estimated free exposure, scaled based on fu values returned in each matrix in vitro. Class IIa cellular IC50 is shown by the red arrowhead; class I/IIb cellular IC50 is shown by the blue arrowhead. Affinity measures for other binding targets identified by the Cerep Diversity panel (KD range for M1–M4 receptors) indicated by the purple bar, and KD for HERG channels (IonWorks) indicated by the green arrowhead (SI Table 3).