Assay Detail
Binding
CHEMBL3879302
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Inhibition of recombinant full length human N-terminal GST/His6-tagged methionine aminopeptidase 2 expressed in baculovirus infected sf9 cells using methionylprolyl-p-nitroanilide as substrate preincubated for 20 mins followed by substrate addition measured for 20 mins in presence of MnCl2 by proline aminopeptidase coupled enzyme assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rickettsia prowazekii methionine aminopeptidase as a promising target for the development of antibacterial agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.28 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225164 | CLOXYQUIN | 2.0 | 1 | 7.26 |
| CHEMBL310555 | OXYQUINOLINE | -1.0 | 1 | 5.90 |
| CHEMBL316892 | 8-HYDROXY QUINALDINE | — | 1 | 5.69 |
| CHEMBL2407096 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225164 | CLOXYQUIN | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL310555 | OXYQUINOLINE | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL316892 | 8-HYDROXY QUINALDINE | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL2407096 | — | IC50 | > | 15000.0 | nM | - |