From: Development of 4H-pyridopyrimidines: a class of selective bacterial protein synthesis inhibitors
Compound | IC50 (μM) | E. fae*(μg/ml) | M. cat(μg/ml) | H. flu(μg/ml) | S. pneumo(μg/ml) | S. aureus(μg/ml) | E. coli tolC(μg/ml) | E. coli + PMBP (μg/ml) |
---|---|---|---|---|---|---|---|---|
321376 | > 300 | N/D | N/D | N/D | N/D | > 128 | > 128 | N/D |
321578 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
321386 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
321388 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
321521 | 2.4 | 16 | 0.5 | 4 | 16 | 128 | 16 | 64 |
321522 | 2.6 | 16 | 1 | 2 | 16 | 128 | 32 | 64 |
321524 | 2.0 | 16 | 1 | 4 | 16 | 128 | 16 | 64 |
321526 | 3.5 | > 128 | 64 | > 128 | > 128 | > 128 | > 128 | > 128 |
321527 | 1.8 | 64 | 2 | 16 | 32 | > 128 | 64 | > 128 |
321529 | 2.6 | 128 | 2 | 8 | 32 | > 128 | 32 | 128 |
323191 | > 300 | 128 | 4 | 32 | 32 | > 128 | 128 | 64 |
323192 | > 300 | 128 | 4 | 64 | 32 | > 128 | 128 | 64 |
323193 | 4.1 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323194 | 3.4 | 64 | 1 | 8 | 8 | 64 | 16 | 16 |
323195 | 1.5 | 64 | 2 | 16 | 32 | 64 | 32 | 16 |
323196 | 1.6 | 32 | 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323197 | 4.4 | > 128 | 16 | 32 | 128 | > 128 | > 128 | > 128 |
323198 | 2.7 | > 128 | 1 | 8 | 16 | > 128 | 32 | 64 |
323199 | 1.1 | 128 | 1 | 16 | 16 | 128 | 32 | 32 |
323200 | 0.4 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323201 | 2.1 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323202 | 4.3 | 32 | 0.25 | 4 | 4 | 16 | 8 | 32 |
323203 | 2.0 | 64 | 1 | 8 | 4 | 16 | 8 | 16 |
323204 | 2.1 | > 128 | 64 | 32 | 128 | > 128 | > 128 | > 128 |
323205 | > 300 | 128 | 4 | 16 | 32 | > 128 | 64 | 64 |
323206 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323207 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323208 | 2.7 | > 128 | 4 | 64 | 32 | > 128 | 64 | 64 |
323209 | 1.5 | > 128 | 4 | 64 | 32 | > 128 | 64 | 64 |
323210 | 3.2 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323211 | 1.6 | > 128 | 64 | > 128 | > 128 | > 128 | > 128 | > 128 |
323212 | 3.4 | 128 | 1 | > 128 | 4 | 64 | 8 | 16 |
323213 | 2.4 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323214 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323215 | 2.1 | > 128 | 128 | 64 | > 128 | > 128 | > 128 | > 128 |
323216 | 1.1 | 32 | ≤0.12 | 2 | 4 | 16 | 8 | 8 |
323217 | 4.8 | > 128 | 32 | 32 | > 128 | > 128 | > 128 | > 128 |
323218 | 0.24 | > 128 | 4 | 16 | 32 | > 128 | 128 | 64 |
323219 | 3.0 | 32 | ≤0.12 | 4 | 4 | 16 | 8 | 16 |
323220 | 2.1 | 32 | ≤0.12 | 2 | 4 | 16 | 8 | 8 |
323221 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323222 | > 300 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323223 | 14.7 | > 128 | 4 | 32 | 32 | > 128 | 128 | 64 |
323224 | 4.9 | > 128 | 16 | 8 | > 128 | > 128 | > 128 | 128 |
323225 | 17.1 | > 128 | 2 | 8 | 128 | > 128 | > 128 | > 128 |
323226 | 8.0 | > 128 | 64 | > 128 | > 128 | > 128 | > 128 | > 128 |
323227 | 0.37 | > 128 | 8 | 32 | 64 | > 128 | 64 | > 128 |
323228 | 0.30 | 64 | 0.5 | 4 | 8 | 31 | 16 | 16 |
323229 | 0.53 | 64 | 0.5 | 8 | 8 | 64 | 16 | 16 |
323230 | 2.0 | 32 | 0.5 | 8 | 8 | 32 | 16 | 16 |
323231 | 5.9 | 128 | 128 | 128 | 128 | > 128 | > 128 | > 128 |
323232 | 3.2 | > 128 | 8 | > 128 | > 128 | > 128 | 128 | > 128 |
323233 | > 300 | 128 | 4 | 16 | 32 | > 128 | 64 | 64 |
323234 | 5.8 | 128 | 16 | 128 | 128 | > 128 | > 128 | 64 |
323235 | 37.9 | > 128 | 8 | 64 | 64 | > 128 | 128 | 128 |
323236 | 7.8 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323237 | 2.8 | 64 | 0.5 | 4 | 8 | 32 | 8 | 16 |
323238 | 2.1 | > 128 | 16 | 32 | > 128 | > 128 | > 128 | > 128 |
323239 | 3.0 | 64 | 8 | 64 | > 128 | > 128 | 64 | 128 |
323338 | 64.4 | 16 | ≤0.12 | 2 | 4 | 16 | 4 | 8 |
323339 | 19.0 | 64 | ≤0.12 | 8 | 4 | 32 | 2 | 2 |
323340 | > 300 | 16 | ≤0.12 | 1 | 2 | 4 | 1 | 2 |
323341 | 41.4 | 32 | ≤0.12 | 2 | 4 | 16 | 8 | 16 |
323342 | 28.9 | 32 | ≤0.12 | 2 | 2 | 32 | 4 | 16 |
323343 | 8.24 | 32 | ≤0.12 | 1 | 2 | 8 | 4 | 2 |
323344 | 11.6 | 32 | ≤0.12 | 4 | 2 | 8 | 1 | 4 |
323345 | > 300 | > 128 | 32 | 64 | 128 | > 128 | 128 | 128 |
323353 | 1.7 | > 128 | 8 | 32 | 128 | > 128 | 128 | 128 |
323354 | 21.6 | > 128 | 16 | > 128 | > 128 | > 128 | > 128 | > 128 |
323355 | 32.1 | > 128 | 4 | 64 | 64 | 128 | 64 | 64 |
323356 | > 300 | 128 | 8 | 64 | 128 | > 128 | 128 | > 128 |
323365 | 2.27 | 16 | ≤0.12 | 4 | 4 | 8 | 4 | 4 |
323366 | 2.47 | 8 | ≤0.12 | 4 | 2 | 8 | 4 | 2 |
323367 | 1.89 | 4 | ≤0.12 | 1 | 2 | 8 | 2 | 8 |
323368 | 0.47 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
323369 | 2.01 | 64 | 4 | 16 | 64 | 128 | 64 | 32 |
323370 | 0.28 | 16 | ≤0.12 | 2 | 4 | 16 | 8 | 8 |
332052 | > 300 | > 128 | 32 | > 64 | > 128 | > 128 | > 128 | > 128 |
332053 | > 300 | > 128 | > 128 | > 64 | > 128 | > 128 | > 128 | > 128 |
332054 | 7.4 | 8 | ≤0.12 | 1 | 2 | 4 | 2 | 1 |
332055 | 16.4 | 64 | 32 | 16 | 128 | > 128 | 128 | 64 |
332057 | 101 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 | > 128 |
332058 | 0.56 | 16 | ≤0.12 | 0.5 | 2 | 16 | 4 | 4 |