Assay Detail
Binding
CHEMBL4186232
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Inhibition of recombinant Caulobacter vibrioides cell cycle histidine kinase CckA deltaTM mutant DHp domain (70 to 691 residues) expressed in Escherichia coli in presence of varying levels of ATP measured every 60 secs for 2 hrs by PK/LDH enzyme coupled assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Caulobacter vibrioides |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Cell cycle histidine kinase CckA (CHEMBL4295627) ↗| Type | SINGLE PROTEIN |
| Organism | Caulobacter vibrioides |
Publication
Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.64 | 5.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL252164 | LUMINESPIB | 2.0 | 1 | 5.14 |
| CHEMBL191074 | — | — | 1 | 4.95 |
| CHEMBL371380 | — | — | 1 | 4.91 |
| CHEMBL364882 | — | — | 1 | 4.76 |
| CHEMBL4218027 | — | — | 1 | 4.73 |
| CHEMBL399530 | — | — | 1 | 4.55 |
| CHEMBL4217100 | — | — | 1 | 4.49 |
| CHEMBL191228 | — | — | 1 | 4.49 |
| CHEMBL4204469 | — | — | 1 | 4.47 |
| CHEMBL192894 | — | — | 1 | 4.34 |
| CHEMBL1551662 | — | — | 1 | 4.25 |
| CHEMBL414883 | RADICICOL | — | 1 | - |
| CHEMBL4217220 | — | — | 1 | - |
| CHEMBL2419346 | CUDC-305 | 1.0 | 1 | - |
| CHEMBL200102 | PU-H71 | 2.0 | 1 | - |
| CHEMBL467399 | BIIB021 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL252164 | LUMINESPIB | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL191074 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL371380 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL364882 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL4218027 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL399530 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4217100 | — | IC50 | = | 32700.0 | nM | 4.49 |
| CHEMBL191228 | — | IC50 | = | 32300.0 | nM | 4.49 |
| CHEMBL4204469 | — | IC50 | = | 33600.0 | nM | 4.47 |
| CHEMBL192894 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL1551662 | — | IC50 | = | 56900.0 | nM | 4.25 |
| CHEMBL414883 | RADICICOL | IC50 | = | 184000.0 | nM | - |
| CHEMBL4217220 | — | IC50 | - | — | - | |
| CHEMBL2419346 | CUDC-305 | IC50 | - | — | - | |
| CHEMBL200102 | PU-H71 | IC50 | - | — | - | |
| CHEMBL467399 | BIIB021 | IC50 | - | — | - |