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. 2019 Apr 15;29(8):995–1000. doi: 10.1016/j.bmcl.2019.02.011

Table 2.

1,2,4-oxadiazol-3-yl benzoic acid derivatives in RAR α, β and γ transactivation assays.aInline graphic

Compd X β EC50 nMa α EC50 nMa Fold selectivity for β over αb γ EC50 nMa Fold selectivity for β over γb cLogPd
ATRA - 1.9 1.2 0.9 0.6 0.5
5 graphic file with name fx9.gif 1.5 18c 28 12 19 5.1
8 graphic file with name fx10.gif 4200 18 17 0.0043 0.0041 7.2
9 graphic file with name fx11.gif 1.4 4 3 2.8 2.1 7.2
10 graphic file with name fx12.gif 1.9 26 11 13 5.6 5.3
11 graphic file with name fx13.gif 2.5 19 5.3 7.6 2 5.3
12 graphic file with name fx14.gif 3.4 30 6.3 9 2 5.8
13 graphic file with name fx15.gif 11 114 83 10 7.5 4.1
a–d

See Table 1.