In vitro potency of DAR4 ADCs.

ADC	LD	Dipeptide	DAR	K562 EC50/ug mL−1
				mTNF GREa	WT GREa
ADC1	LD1	Ala–Ala	3.8	0.92	>50
ADC2	LD2	Ala–Arg	3.6	0.74	>50
ADC3	LD3	Ala–Gln	3.7	0.95	>15
ADC4	LD4	Ala–Glu	3.3	0.84	>50
ADC5	LD5	Ala–Gly	3.7	0.72	>23
ADC6	LD6	Ala–His	3.5	0.82	>50
ADC7	LD7	Ala–Lys	2.4	0.51	>50
ADC8	LD8	Ala–Ser	4.2	0.44	>34
ADC9	LD12	Gly–Ala	3.8	1.49	>44
ADC10	LD13	Gly–Gln	3.7	0.60	>50
ADC11	LD14	Gly–Glu	3.2	1.40	>50
ADC12	LD15	Gly–Gly	3.6	0.54	>38
ADC13	LD16	Gly–Ser	3.7	0.81	>50
ADC14	LD17	Phe–Lys	3.7	0.78	>50
ADC15	LD18	Ser–Ala	3.8	1.05	>29
ADC16	LD19	Ser–Asn	3.5	0.80	>50
ADC17	LD20	Ser–Gln	3.6	1.08	>50
ADC18	LD21	Ser–Glu	3.5	1.69	>20
ADC19	LD22	Ser–Gly	3.7	1.03	>13
ADC20	LD23	Val–Ala	3.8	0.48	>26
ADC21	LD24	Val–Arg	3.4	0.86	>50
ADC22	LD25	Val–Cit	3.6	0.72	>50
ADC23	LD26	Val–Asn	3.5	0.53	>36
ADC24	LD27	Val–Gln	4.1	1.26	>19
ADC25	LD28	Val–Glu	3.4	0.79	>50
ADC26	LD29	Val–Gly	3.6	0.55	>19
ADC27	LD30	Val–Ser	3.7	0.55	>42

^aData is single point.