Assay Detail
Binding
CHEMBL3373164
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Inhibition of Escherichia coli GyrB A2B2 subunits assessed reduction in DNA supercoiling activity by malachite green dye based by spectrophotometry
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Pyridine-3-carboxamide-6-yl-ureas as novel inhibitors of bacterial DNA gyrase: structure based design, synthesis, SAR and antimicrobial activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 5.88 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3329317 | — | — | 1 | 7.55 |
| CHEMBL3329318 | — | — | 1 | 7.44 |
| CHEMBL3329312 | — | — | 1 | 7.41 |
| CHEMBL3329307 | — | — | 1 | 7.40 |
| CHEMBL3329319 | — | — | 1 | 7.34 |
| CHEMBL3329316 | — | — | 1 | 7.03 |
| CHEMBL3329292 | — | — | 1 | 7.01 |
| CHEMBL3329291 | — | — | 1 | 7.00 |
| CHEMBL3329311 | — | — | 1 | 6.96 |
| CHEMBL3329308 | — | — | 1 | 6.85 |
| CHEMBL3329313 | — | — | 1 | 6.82 |
| CHEMBL3329309 | — | — | 1 | 6.82 |
| CHEMBL3329310 | — | — | 1 | 6.77 |
| CHEMBL3329287 | — | — | 1 | 6.38 |
| CHEMBL3329221 | — | — | 1 | 6.37 |
| CHEMBL3329297 | — | — | 1 | 6.26 |
| CHEMBL3329298 | — | — | 1 | 6.25 |
| CHEMBL3329305 | — | — | 1 | 6.18 |
| CHEMBL3329302 | — | — | 1 | 6.09 |
| CHEMBL3329288 | — | — | 1 | 6.02 |
| CHEMBL3329299 | — | — | 1 | 5.95 |
| CHEMBL3329274 | — | — | 1 | 5.80 |
| CHEMBL3329314 | — | — | 1 | 5.70 |
| CHEMBL3329275 | — | — | 1 | 5.68 |
| CHEMBL3329304 | — | — | 1 | 5.67 |
| CHEMBL3329303 | — | — | 1 | 5.53 |
| CHEMBL3329277 | — | — | 1 | 5.52 |
| CHEMBL3329300 | — | — | 1 | 5.52 |
| CHEMBL3329276 | — | — | 1 | 5.48 |
| CHEMBL3329278 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3329317 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3329318 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3329312 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3329307 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3329319 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3329316 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3329292 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3329291 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3329311 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3329308 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3329313 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3329309 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3329310 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3329287 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3329221 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3329297 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3329298 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3329305 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3329302 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3329288 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3329299 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL3329274 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3329314 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3329275 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3329304 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL3329303 | — | IC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL3329300 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL3329277 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3329276 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3329278 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3329284 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3329279 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3329306 | — | IC50 | = | 4810.0 | nM | 5.32 |
| CHEMBL3329315 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3329293 | — | IC50 | = | 5140.0 | nM | 5.29 |
| CHEMBL3329285 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3329294 | — | IC50 | = | 5660.0 | nM | 5.25 |
| CHEMBL3329272 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3329282 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3329301 | — | IC50 | = | 7270.0 | nM | 5.14 |
| CHEMBL3329283 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3329273 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL3706672 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL3329286 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3329295 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3329289 | — | IC50 | = | 23100.0 | nM | 4.64 |
| CHEMBL3329280 | — | IC50 | = | 24500.0 | nM | 4.61 |
| CHEMBL3329296 | — | IC50 | = | 33200.0 | nM | 4.48 |
| CHEMBL3329281 | — | IC50 | = | 40400.0 | nM | 4.39 |
| CHEMBL3094347 | — | IC50 | < | 750.0 | nM | - |