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. 2019 Aug 15;29(16):2440–2441. doi: 10.1016/j.bmcl.2019.05.058

Table 2.

1,2,4-Oxadiazol-3-yl benzoic acid derivatives in RAR α, β and γ transactivation assays.a

graphic file with name fx1.jpg

Compd X β EC50 nMa α EC50 nMa γ EC50 nMa Fold Selectivity for β over αb Fold Selectivity for β over γb cLog Pd
ATRA 1.9 1.2 0.9 0.6 0.5
5 graphic file with name fx2.gif 1.5 18c 28 12 19 5.1
8 graphic file with name fx3.gif 4200 18 17 0.0043 0.0041 7.2
9 graphic file with name fx4.gif 1.4 4 3 2.8 2.1 7.2
10 graphic file with name fx5.gif 1.9 26 11 13 5.6 5.3
11 graphic file with name fx6.gif 2.5 19 5.3 7.6 2 5.3
12 graphic file with name fx7.gif 3.4 30 6.3 9 2 5.8
13 graphic file with name fx8.gif 11 114 83 10 7.5 4.1
a–d

See Table 1.