. 2019 Oct 16;29(23):126717. doi: 10.1016/j.bmcl.2019.126717

Table 4.

CypD SAR of optimized amides derived from fragment linking of fragment hits 3 or 4 with fragment hit 7.

#	Structure	Biochemical CypD FP assay		Biochemical PPIase assay IC₅₀ (µM)^c	SPR binding CypD
#	Structure	IC₅₀ (µM)^a	LE^b	Biochemical PPIase assay IC₅₀ (µM)^c	K_D (µM)^d	LE^e
34		80	0.18	nt	ND
35		ND		nt	>6000
36		2.8	0.32	28	4.9	0.29
37		490	0.18	nt	>200
38		1.35	0.30	0.6	1.6	0.28
39		1.7	0.26	nt	0.660	0.26
40		0.735	0.27	nt	1.2	0.25

^a,bCypD biochemical FP and PPIase assays. ^c,eLigand binding efficiencies (LE) based on biochemical FP IC₅₀s or SPR K_Ds. ^dCypD SPR binding assay. nt = not tested, ND = not detected.