Table 1 In vitro inhibition constants of PDFIs against PDFs from S. agalactiae, E. coli and A. thaliana.
From: A unique peptide deformylase platform to rationally design and challenge novel active compounds
PDF-In | SaPDF | EcPDF | AtPDF1B | ||||||
|---|---|---|---|---|---|---|---|---|---|
KI (nM) | KI*app (nM) | KI/KI*app | KI (nM) | KI*app (nM) | KI/KI*app | KI (nM) | KI*app (nM) | KI/KI*app | |
Actinonin | 64 ± 5 | 1.0 ± 0.1 | 64 | 185 ± 15 | 1.7 ± 0.5 | 109 | 82 ± 10 | 3.5 ± 0.3 | 23 |
Indole serie | |||||||||
AB47 | 62 ± 3 | 73 ± 5 | 1 | 47 ± 2 | 39 ± 2 | 1 | 455 ± 89 | 400 ± 35 | 1 |
SMP195 | 285 ± 18 | 250 ± 17 | 1 | 29 ± 4 | 20 ± 3 | 1 | 909 ± 118 | 833 ± 53 | 1 |
SMP289 | 909 ± 64 | 714 ± 72 | 1 | 769 ± 30 | 625 ± 75 | 1 | 1000 ± 78 | 1,428 ± 126 | 1 |
Peptide serie | |||||||||
RAS358 | 1428 ± 125 | 454 ± 29 | 3 | 833 ± 30 | 164 ± 40 | 5 | 2000 ± 150 | 400 ± 37 | 5 |
Oxadiazole serie | |||||||||
AT002 | 13 ± 1 | 4.0 ± 0.5 | 3 | 31 ± 7 | 5 ± 2 | 6 | 58 ± 4 | 53 ± 3 | 1 |
AT008 | 75 ± 4 | 81 ± 5 | 1 | 80 ± 10 | 18 ± 3 | 4 | 909 ± 78 | 666 ± 29 | 1 |
AT011 | 400 ± 20 | 430 ± 39 | 1 | — | 333 ± 13 | — | — | 5,000 ± 500 | — |
AT012 | — | 400 ± 35 | — | — | 70 ± 8 | — | — | 625 ± 30 | — |
AT013 | 70 ± 5 | 51 ± 3 | 1 | 73 ± 12 | 80 ± 10 | 1 | — | 303 ± 12 | — |
AT014 | 84 ± 6 | 65 ± 10 | 1 | — | 66 ± 3 | — | — | 909 ± 32 | — |
AT015 | 166 ± 12 | 122 ± 13 | 1 | 35 ± 5 | 10 ± 2 | 3 | — | 1,100 ± 115 | — |
AT016 | 67 ± 7 | 55 ± 5 | 1 | 25 ± 3 | 26 ± 5 | 1 | — | — | — |
AT017 | — | 85 ± 8 | — | — | 41 ± 3 | — | — | — | — |
AT018 | 38 ± 6 | 18 ± 1 | 2 | 49 ± 3 | 12 ± 1 | 4 | 1111 ± 100 | 833 ± 10 | 1 |
AT021 | — | 200 ± 10 | — | — | 76 ± 5 | — | — | ~10 μM | — |
AT019 | 65 ± 6 | 7.5 ± 2 | 9 | 76 ± 4 | 1.1 ± 0.3 | 69 | 263 ± 26 | 54 ± 2 | 5 |
AT020 | 63 ± 3 | 8.5 ± 3 | 7 | 80 ± 3 | 1.9 ± 0.2 | 42 | 238 ± 30 | 123 ± 5 | 2 |
