Table 1 Best CDKi’s identified in this study for selective target engagement in live cells.

CDK2

NU6102

290 nM

ST^b

CDK3

RO-3306

200 nM

CDK7 (690 nM)

CDK4/6

Palbociclib

10 nM/2 nM

ST^b

CDK4/6

Ribociclib

29 nM/31 nM

ST^b

CDK7

THZ1

90 nM

CDK11a (300 nM)

CDK7

BS-181

470 nM

ST^b

CDK9

BAY-1251152

9 nM

ST^b

CDK9

Atuveciclib

150 nM

ST^b

CDK8/19

CCT251545

6 nM/6 nM

ST^b

CDK8/19

CCT251545 analog

6 nM/10 nM

ST^b

CDK8/19

BMS-265246

0.7 nM/1.5 nM

CDK3 (10 nM)

CDK8/19

K08361

3 nM/1.4 nM

CDK7 (63 nM)

CDK12

THZ531

770 nM

ST^b