Table 1. Limited selectivity conditions... | American Society of Hematology

Table 1.

Limited selectivity conditions in 2 human kinome assays of BTKis

Reference	Reported selectivity (from high to low)	IC₅₀ (μM)	Ki∗ (μM)	BTKi in the assay (μM)	Selectivity conditions vs IC₅₀ vs Ki
Podoll et al¹⁴	Acalabrutinib ACP-5862† Zanubrutinib Ibrutinib	0.005 0.005 0.0005 0.0015	0.181 0.188 0.126 0.054	1 1 1 1	- - - - - - - -
Shadman et al¹³	Zanubrutinib Acalabrutinib Ibrutinib ACP-5862†	0.00071 0.0240 0.00032 0.0630	0.126 0.181 0.054 0.188	0.071 2.400 0.032 6.300	- √ - - - √ - -

Reference	Reported selectivity (from high to low)	IC₅₀ (μM)	Ki∗ (μM)	BTKi in the assay (μM)	Selectivity conditions vs IC₅₀ vs Ki
Podoll et al¹⁴	Acalabrutinib ACP-5862† Zanubrutinib Ibrutinib	0.005 0.005 0.0005 0.0015	0.181 0.188 0.126 0.054	1 1 1 1	- - - - - - - -
Shadman et al¹³	Zanubrutinib Acalabrutinib Ibrutinib ACP-5862†	0.00071 0.0240 0.00032 0.0630	0.126 0.181 0.054 0.188	0.071 2.400 0.032 6.300	- √ - - - √ - -

-, no; √, yes.

All from Podoll et al.¹⁴

Acalabrutinib active metabolite.