TABLE 3

Prediction of intracellular KAT6A target exposure using two independent methods and comparison with biochemical potency measurements

Compound	IC_50,biochem (μM)	IC_50,cell (μM)	Fold Difference Relative to IC_50,biochem	Saturation Method^{^a}		Binding Method^{^b}
Compound	IC_50,biochem (μM)	IC_50,cell (μM)	Fold Difference Relative to IC_50,biochem	Cytosolic IC₅₀ (μM)	Fold Difference Relative to IC_50,biochem	Intracellular IC₅₀ (μM)	Fold Difference Relative to IC_50,biochem
WM-8014	0.005	0.10	20	0.001	4.0	0.006	1.1
WM-1119	0.005	0.03	5.7	0.013	2.7	0.005	1.0
Compound 1	0.48	7.8	16	0.12	3.8	0.009	55
Compound 2	0.085	8.52	100	0.13	1.6	0.46	5.4
Compound 3	0.075	12	158	0.20	2.7	0.053	1.4
Compound 4	0.088	4.9	57	0.59	6.8	0.39	4.5
Compound 5	0.017	3.8	220	0.17	9.9	0.097	5.6
Compound 6	0.061	0.12	2.1	0.017	3.5	0.010	6.1
Compound 7	0.026	1.0	40	0.046	1.7	0.045	1.7
Compound 8	0.006	1.6	260	0.010	1.6	0.003	2.3
Compound 9	0.59	0.92	1.5	0.029	21	0.006	105
Compound 10	0.17	0.22	1.3	0.032	5.3	0.004	45

↵^a For the prediction of cytosolic IC₅₀, the Kp_uu,cyto at the unbound IC_50,cell was used (eq. 16).
↵^b For the prediction of intracellular IC₅₀, the Kp_uu,cell,hom in the unsaturated state was used (eq. 15).