Table 1

JAKinib IC₅₀ values in CD4+ T-cells, monocytes and NK cells from whole blood assays

Stimulation/pSTAT	CD4+ T-cells					Monocytes					NK cells
	BARI	FIL	MET	TOFA	UPA	BARI	FIL	MET	TOFA	UPA	BARI	FIL	MET	TOFA	UPA
	IC₅₀, nM
JAK2/JAK2 or JAK2/TYK2-dependent cytokines
G-CSF/pSTAT3	NS					81	4977	50 215	292	81	NS
GM-CSF/pSTAT5	NS					127	9916	102 910	510	74	NS
IL-12/pSTAT4	NS					NS					269	10 351	221 777	1216	364
JAK1/JAK2/TYK2-dependent cytokines
IFNα/pSTAT1	50	1096	17 161	98	30	192	4560	91 078	393	83	131	2440	41 161	256	117
IFNα/pSTAT3	39	871	12 644	80	24	40	991	15 793	86	17	30	675	8620	60	25
IFNα/pSTAT5	28	638	9587	49	17	25	613	9518	51	11	34	507	7484	50	26
IFNγ/pSTAT1	NS					74	4138	62 374	228	58	NS
IL-6/pSTAT1	29	783	5637	63	27	39	1011	10 019	84	22	NS
IL-6/pSTAT3	274	5435	62 680	644	225	161	3527	49 109	368	100	NS
JAK1/JAK3-dependent cytokines
IL-2/pSTAT5	40	988	14 079	40	21	NS					80	2153	23 824	87	56
IL-4/pSTAT6	73	1458	39 420	77	36	53	1337	36 537	116	32	40	869	20 984	45	25
IL-15/pSTAT5	38	967	14 326	39	21	NS					83	2044	27 540	93	58

G-CSF, GM-CSF, IFNα, IFNγ, IL-6, IL-2, IL-4 and IL-15 reported IC₅₀ values are based on the average of duplicates from 7–10 healthy volunteer whole blood.
BARI, baricitinib; FIL, filgotinib; G-CSF, granulocyte colony stimulating factor; GM-CSF, granulocyte-macrophage colony stimulating factor; IC₅₀, half maximum inhibitory concentration; IFN, interferon; IL, interleukin; JAK, Janus kinase; JAKinib, Janus kinase inhibitor; MET, major metabolite of filgotinib (GS-829845); NK, natural killer cell; NS, not sampled; pSTAT, phosphorylated signal transducer and activator of transcription; TOFA, tofacitinib; TYK2, tyrosine kinase 2; UPA, upadacitinib.