Table 3.

CAR inverse agonistic activities of CINPA1 and its novel 20 analogs from the second-round chemistry effort

Compound	R1	R2	IC50 (nM)
11 (CINPA1)			687 ± 71
53			6,400 ± 124
54		53 to 64	116.4 ± 8.6
55			249.0 ± 16.6
56			20.9 ± 2.6
57			11,350 ± 670
58			60.1 ± 3.4
59			35.3 ± 4.8
60			21.2 ± 1.9
61			81.5 ± 7.4
62			37.6 ± 2.8
63			19.5 ± 1.5
64			24.1 ± 1.4
65		65 to 68	152.9 ± 11.1
66			216.2 ± 15.6
67			116.0 ± 7.3
68			31.9 ± 2.2
69	69 to 72		22.1 ± 1.3
70			20.1 ± 2.8
71			13.9 ± 0.9
72			11.7 ± 0.8