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. 2018 Mar 26;8:5205. doi: 10.1038/s41598-018-23482-4

Table 1.

In vitro inhibitory potencies of synthesized benzylidenebarbituric acid derivatives.

Compound IC50 (nM)a against mPGES-1 COX-1/2 Inhibition (%) at 100 µMb
ID X Human mPGES-1 Mouse mPGES-1
4a H 622 ± 121 7080 ± 627 0 ± 15
4b Cl 33 ± 3 157 ± 31 4.3 ± 6.0
4c Br 45 ± 8 917 ± 321 63 ± 0.8
4d Me 82 ± 10 18900 ± 4080 9.1 ± 6.6
4e OH 116 ± 17 2900 ± 293 68 ± 3.4
4f OMe 121 ± 20 146 ± 209 28 ± 3.6
4g OEt 186 ± 26 2410 ± 339 0 ± 15.1
4h NO2 67 ± 20 698 ± 97 43 ± 3.2
4i 87 ± 27 19100 ± 3490 56 ± 3.7
6 69 ± 16 292 ± 47 17 ± 4.6

aData are expressed as the Mean ± SD of measurements in triplicate. bThe % inhibition of the compound at a concentration of 100 µM against the COX-1/2 (with equal amounts of COX-1 and COX-2 in terms of the enzyme activities).