Table 1.

In vitro PI3K Isoform Inhibition Data for ZSTK474 analogs.

IC50 (nM)a
COMPD	cLogPb	PI3Kα	PI3Kβ	PI3Kγ	PI3Kδ
ZSTK474	1.06	5.0 ± 0.8	15.2 ± 1.4	20.8 ± 0.6	3.9 ± 0.6
6a	0.96	9.9 ± 1.2	71 ± 8	54 ± 1	8.1 ± 1.7
6b	0.28	3.7 ± 1.0	74 ± 5.7	14.6 ± 1.4	9.9 ± 0.4
6c	1.72	20 ± 3	208 ± 15	64 ± 5	17 ± 1
6d	1.04	5.1 ± 1.1	136 ± 6.4	30.7 ± 0.9	8.9 ± 0.5
6e	1.25	148 ± 22	627 ± 174	869 ± 11	46.7 ± 3.3
6f	1.38	12.4 ± 0.7	787 ± 106	22.3 ± 0.7	60 ± 3.4
6g	0.92	20 ± 0.4	431 ± 83	67 ± 2.8	26 ± 4.9
6l	1.03	292 ± 31	2117 ± 444	771 ± 63	291 ± 32
6m	1.34	248 ± 24	2900 ± 375	681 ± 90	135 ± 19
6n	0.46	89.3 ± 9.5	1867 ± 245	502 ± 20	12.6 ± 1.0
6o	−0.22	10.9 ± 0.75	1085 ± 143	137 ± 21	8.6 ± 1.2
6p	0.92	16.6 ± 1.4	199 ± 12	54 ± 1.5	9.5 ± 2.4
6q	1.32	10.3 ± 1.0	404 ± 63	55.2 ± 11.5	11.7 ± 2.2

^aMean ± standard error (SEM) of 3 experiments each conducted in duplicate

^bcLogP data obtained using ChemDraw Professional (version 15.0.0.106)