Table 2.

Biochemical IC₅₀s on CDKs of TMX-2039 analogs.

Compound	CDK1[a] IC50 (nM)	CDK2[b] IC50 (nM)	CDK5[c] IC50 (nM)	CDK4[d] IC50 (nM)	CDK6[d] IC50 (nM)
TMX-2075	365.0	75.3	154.0	124	127.0
TMX-2076	105.0	17.8	32.4	981	487.0
TMX-2099	3.7	0.6	<0.5	10.2	4.9
TMX-2105	1600.0	530.0	530.0	140.0	5100.0
TMX-2106	369.0	33.2	57.0	33.4	546.0
TMX-3013	0.9	<0.5	0.5	24.5	15.6
TMX-3010	1.2	0.7	0.9	135.0	84.1
TMX-3012	0.8	0.7	0.6	79.6	24.0

^[a]w/cyclin B.

^[b]w/cyclin A.

^[c]w/p25.

^[d]w/cyclin D1. All the IC₅₀ values were tested in duplicate, value ranges are shown in Table S2 in the Supporting Information.