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. 2021 Dec 11;229:114046. doi: 10.1016/j.ejmech.2021.114046

Table 3.

Inhibitory potency against SARS-CoV-2 3CLpro. Optimization of R3.

Entry Cmpd R1 R3 R4 Inhibition (%)a IC50 (μM)
1 11c Image 60 Image 61 cHex 22 ± 8 ndb
2 11d Image 62 Image 63 cHex 18 ± 8 ndb
3 11e Image 64 Image 65 cHex <5 ndb
4 11f Image 66 Image 67 cHex 19 ± 8 ndb
5 11g Image 68 Image 69 cHex 38 ± 8 ndb
6 11h Image 70 Image 71 cHex <5 ndb
7 11i Image 72 Image 73 cHex 24 ± 8 ndb
8 8c Image 74 Image 75 tBu 24 ± 8 ndb
9 16d Image 76 Image 77 cHex 22 ± 11 ndb
10 16e Image 78 Image 79 cHex >95 0.84 ± 0.30
11 16f Image 80 Image 81 cHex >95 0.98 ± 0.35
12 13e Image 82 Image 83 cHex >95 5.0 ± 2.3
13 13f Image 84 Image 85 cHex 80 ± 10 ndb,c
14 13g Image 86 Image 87 cHex 54 ± 15 ndb
15 13h Image 88 Image 89 cHex 57 ± 6 ndb
16 13i Image 90 Image 91 cHex 10 ± 10 ndb
17 13j Image 92 Image 93 cHex 19 ± 5 ndb

3.