Assay Detail
Binding
CHEMBL661928
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Inhibition of class A TEM-1 beta-lactamase derived from Enterobacter cloacae
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Enterobacter cloacae |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.22 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL433726 | — | — | 1 | 8.22 |
| CHEMBL355558 | — | — | 1 | 7.85 |
| CHEMBL169392 | — | — | 1 | 7.70 |
| CHEMBL353422 | — | — | 1 | 7.16 |
| CHEMBL167539 | — | — | 1 | 7.16 |
| CHEMBL353613 | — | — | 1 | 7.05 |
| CHEMBL355165 | — | — | 1 | 6.70 |
| CHEMBL1439 | TAZOBACTAM SODIUM | 4.0 | 1 | 6.50 |
| CHEMBL353978 | — | — | 1 | 6.16 |
| CHEMBL422212 | — | — | 1 | 6.10 |
| CHEMBL353694 | — | — | 1 | 6.05 |
| CHEMBL355288 | — | — | 1 | 5.63 |
| CHEMBL169373 | — | — | 1 | 5.60 |
| CHEMBL171999 | — | — | 1 | 5.60 |
| CHEMBL354754 | — | — | 1 | 5.54 |
| CHEMBL169550 | — | — | 1 | 5.25 |
| CHEMBL354758 | — | — | 1 | 4.98 |
| CHEMBL169303 | — | — | 1 | 4.76 |
| CHEMBL167311 | — | — | 1 | 4.17 |
| CHEMBL171049 | — | — | 1 | - |
| CHEMBL172564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL433726 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL355558 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL169392 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL353422 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL167539 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL353613 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL355165 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1439 | TAZOBACTAM SODIUM | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL353978 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL422212 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL353694 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL355288 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL169373 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL171999 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL354754 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL169550 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL354758 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL169303 | — | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL167311 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL171049 | — | IC50 | = | 260000.0 | nM | - |
| CHEMBL172564 | — | IC50 | = | 311000.0 | nM | - |