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. Author manuscript; available in PMC: 2017 Jan 27.
Published in final edited form as: Eur J Med Chem. 2015 Dec 15;108:505–528. doi: 10.1016/j.ejmech.2015.12.018

Table 2.

CAR inverse agonistic activities of CINPA1 and its 23 analogs from the first-round chemistry effort

graphic file with name nihms746925u2.jpg
Compound R1 R2 IC50 (nM)
11 (CINPA1) graphic file with name nihms746925t1.jpg graphic file with name nihms746925t2.jpg 687 ± 71
22 graphic file with name nihms746925t12.jpg 210 ± 10
23 graphic file with name nihms746925t13.jpg graphic file with name nihms746925t2.jpg
22 to 35 		3,050 ± 125
24 graphic file with name nihms746925t14.jpg 1,580 ± 88
25 graphic file with name nihms746925t15.jpg 620 ± 29
26 graphic file with name nihms746925t16.jpg 4,080 ± 162
27 graphic file with name nihms746925t17.jpg 1,410 ± 41
28 graphic file with name nihms746925t18.jpg 39,810 ± 4,384
29 graphic file with name nihms746925t19.jpg 37.0 ± 1.5
30 graphic file with name nihms746925t20.jpg 6,890 ± 350
31 graphic file with name nihms746925t21.jpg 24,490 ± 845
32 graphic file with name nihms746925t22.jpg 2,060 ± 163
33 graphic file with name nihms746925t23.jpg 2,430 ± 114
34 graphic file with name nihms746925t24.jpg 3,180 ± 131
35 graphic file with name nihms746925t25.jpg 70.8 ± 1.0
36 graphic file with name nihms746925t5.jpg
36 to 44 		graphic file with name nihms746925t26.jpg 2,320 ± 95
37 graphic file with name nihms746925t10.jpg 680 ± 31
38 graphic file with name nihms746925t27.jpg 1,030 ± 38
39 graphic file with name nihms746925t28.jpg 14,420 ± 742
40 graphic file with name nihms746925t29.jpg 4,930 ± 146
41 graphic file with name nihms746925t30.jpg 12,970 ± 183
42 graphic file with name nihms746925t31.jpg 13,990 ± 318
43 graphic file with name nihms746925t32.jpg 19,090 ± 1,397
44 graphic file with name nihms746925t33.jpg 18,790 ± 1,585