Table 5.

C-2 Diazaspiro[3.3]heptane Derivatives

Compd	R4	R3’, R5’	Kd (μM)a	ALogP	LipE
59		Me	0.012 ± 0.0020	6.92	1.02
60		Me	0.016 ± 0.0037	4.76	3.05
61		H	0.18 ± 0.003b	3.78	2.98
62		Me	0.012 ± 0.0008	4.53	3.38
63		H	0.036 ± 0.0055	3.56	3.88
64		Me	0.044 ± 0.0067	4.85	2.50
65		Me	0.009 ± 0.0017	5.12	2.91

Measurements are reported as the mean ± SD of two or more independent experiments, each conducted in duplicate.

^aEvaluated through displacement of fluorescent probe S3 (Supplementary Figure S2).

^bEvaluated through displacement of fluorescent probe S2 (Supplementary Figure S2).