Assay Detail
Binding
CHEMBL3879300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Rickettsia prowazekii str. Madrid E N-terminal His-tagged methionine aminopeptidase 1A expressed in Escherichia coli BL21(DE3) Rosetta cells using Met-AMC as substrate preincubated for 1 hr followed by substrate addition measured after 30 mins for 90 mins in presence of MnCl2 by fluorescence assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rickettsia prowazekii str. Madrid E |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 26 | 5.11 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200377 | — | — | 1 | 6.30 |
| CHEMBL200238 | — | — | 1 | 6.22 |
| CHEMBL370437 | — | — | 1 | 6.22 |
| CHEMBL225164 | CLOXYQUIN | 2.0 | 1 | 6.05 |
| CHEMBL310555 | OXYQUINOLINE | -1.0 | 1 | 6.05 |
| CHEMBL3903463 | — | — | 1 | 6.05 |
| CHEMBL316892 | 8-HYDROXY QUINALDINE | — | 1 | 6.00 |
| CHEMBL1454910 | NITROXOLINE | 4.0 | 1 | 5.89 |
| CHEMBL2407096 | — | — | 1 | 5.85 |
| CHEMBL2407599 | — | — | 1 | 5.60 |
| CHEMBL1313880 | — | — | 1 | 5.18 |
| CHEMBL569750 | — | — | 1 | 5.11 |
| CHEMBL2407595 | — | — | 1 | 4.85 |
| CHEMBL1367401 | — | — | 1 | 4.82 |
| CHEMBL2407604 | — | — | 1 | 4.80 |
| CHEMBL568651 | — | — | 1 | 4.64 |
| CHEMBL3985041 | — | — | 1 | 4.58 |
| CHEMBL569683 | — | — | 1 | 4.55 |
| CHEMBL3925290 | — | — | 1 | 4.52 |
| CHEMBL200666 | — | — | 1 | 4.43 |
| CHEMBL3924359 | — | — | 1 | 4.34 |
| CHEMBL3968454 | — | — | 1 | 4.24 |
| CHEMBL3920098 | — | — | 1 | 4.22 |
| CHEMBL2407601 | — | — | 1 | 4.14 |
| CHEMBL3951007 | — | — | 1 | 4.13 |
| CHEMBL1408131 | — | — | 1 | 4.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200377 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL200238 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL370437 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL225164 | CLOXYQUIN | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL310555 | OXYQUINOLINE | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3903463 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL316892 | 8-HYDROXY QUINALDINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1454910 | NITROXOLINE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2407096 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2407599 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1313880 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL569750 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL2407595 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1367401 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2407604 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL568651 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3985041 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL569683 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3925290 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL200666 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL3924359 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL3968454 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL3920098 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL2407601 | — | IC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL3951007 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL1408131 | — | IC50 | = | 77000.0 | nM | 4.11 |