Assay Detail
Binding
CHEMBL4275017
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Inhibition of Escherichia coli GyrB (1 to 220 residues) expressed in Escherichia coli BL21(DE3)
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.28 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4283208 | — | — | 1 | 8.70 |
| CHEMBL4286573 | — | — | 1 | 8.70 |
| CHEMBL4294536 | — | — | 1 | 8.52 |
| CHEMBL4295081 | — | — | 1 | 8.52 |
| CHEMBL4291061 | — | — | 1 | 8.40 |
| CHEMBL4286625 | — | — | 1 | 8.40 |
| CHEMBL4290062 | — | — | 1 | 8.30 |
| CHEMBL4293447 | — | — | 1 | 8.22 |
| CHEMBL4294467 | — | — | 1 | 8.22 |
| CHEMBL4281775 | — | — | 1 | 8.22 |
| CHEMBL3235085 | — | — | 1 | 8.22 |
| CHEMBL4279382 | — | — | 1 | 8.15 |
| CHEMBL4278317 | — | — | 1 | 8.10 |
| CHEMBL4279313 | — | — | 1 | 8.10 |
| CHEMBL4289650 | — | — | 1 | 8.05 |
| CHEMBL4289998 | — | — | 1 | 8.05 |
| CHEMBL4286232 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4283208 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4286573 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4294536 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4295081 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4291061 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4286625 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4290062 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4293447 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4294467 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4281775 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3235085 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4279382 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4278317 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4279313 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4289650 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4289998 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4286232 | — | IC50 | = | 14.0 | nM | 7.85 |