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. 2020 Aug 1;10(21):9741–9766. doi: 10.7150/thno.46913

Table 2.

PAK1 inhibitors

No. Comd. Structure Classification PAK1 inhibition activity References
1 K-252a graphic file with name thnov10p9741i001.jpg ATP-competitive inhibitors 2.4 nM 172
2 KTD606 graphic file with name thnov10p9741i002.jpg ATP-competitive inhibitors 4.0 nM 174
3 CEP1347 graphic file with name thnov10p9741i003.jpg ATP-competitive inhibitors 2.5 nM 174
4 Staurosporine graphic file with name thnov10p9741i004.jpg ATP-competitive inhibitors 0.75 nM 175
5 Λ-FL172 graphic file with name thnov10p9741i005.jpg ATP-competitive inhibitors 130 nM 176
6 (R-1) graphic file with name thnov10p9741i006.jpg ATP-competitive inhibitors 83 nM 177
7 II-11 graphic file with name thnov10p9741i007.jpg ATP-competitive inhibitors 1.6 nM 179
8 PF-3758309 graphic file with name thnov10p9741i008.jpg ATP-competitive inhibitors 14 nM 180
9 FRAX597 graphic file with name thnov10p9741i009.jpg ATP-competitive inhibitors 7.7 nM 186
10 FRAX486 graphic file with name thnov10p9741i010.jpg ATP-competitive inhibitors 8.3 nM 187
11 G‑5555 graphic file with name thnov10p9741i011.jpg ATP-competitive inhibitors 3.7 nM 188
12 12 graphic file with name thnov10p9741i012.jpg ATP-competitive inhibitors 65 nM 189
13 13 graphic file with name thnov10p9741i013.jpg ATP-competitive inhibitors 5.0 nM 190
14 14 graphic file with name thnov10p9741i014.jpg ATP-competitive inhibitors 5 nM 191
15 15 graphic file with name thnov10p9741i015.jpg ATP-competitive inhibitors 288 nM 192
16 G-9791 graphic file with name thnov10p9741i016.jpg ATP-competitive inhibitors Ki=26 nM 193
17 17 graphic file with name thnov10p9741i017.jpg ATP-competitive inhibitors 0.73 μM 194
18 OSU-03012 graphic file with name thnov10p9741i018.jpg ATP-competitive inhibitors 1.03 μM 195
19 AK963 graphic file with name thnov10p9741i019.jpg ATP-competitive inhibitors - 196
20 ZMF-10 graphic file with name thnov10p9741i020.jpg ATP-competitive inhibitors 194 nM 197
21 IPA-3 graphic file with name thnov10p9741i021.jpg Allosteric inhibitors 2.5 μM 198
22 22 graphic file with name thnov10p9741i022.jpg Allosteric inhibitors 5 nM 199
23 23 graphic file with name thnov10p9741i023.jpg Allosteric inhibitors 18 nM 199
24 2-Mc-1,4-NHQ graphic file with name thnov10p9741i024.jpg Allosteric inhibitors - 200