Table 2 Comparation of PVTX-405 (16a), 16b and DKY709

CRBN binding^a

IC₅₀ (nM)

496

99

1335

IKZF2 degradation^b

DC₅₀ (D_max)

1.5 nM (73%)

0.7 nM (91%)

4.1 nM (89%)

IKZF1 degradation^b

DC₅₀ (D_max)

>10 µM (14%)

>10 µM (11%)

>10 µM (7%)

IKZF3 degradation^b

DC₅₀ (D_max)

>10 µM (20%)

>10 µM (17%)

>10 µM (9%)

SALL4 degradation^b

DC₅₀ (D_max)

4.9 nM (55%)

>1000 nM (33%)

>1000 nM (27%)

GSPT1 degradation^b

DC₅₀ (D_max)

>10 µM (16%)

>10 µM (14%)

>10 µM (13%)

CK1α degradation^b

DC₅₀ (D_max)

>10 µM (15%)

>10 µM (10%)

>10 µM (7%)

hERG inhibition^c

IC₅₀ (µM)

9.0

48

NT