Assay Detail
Functional
CHEMBL680694
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]tetracycline uptake into everted membrane vesicles, prepared from tetracycline resistant Escherichia coli D1-209
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Inhibition of the tetracycline efflux antiport protein by 13-thio-substituted 5-hydroxy-6-deoxytetracyclines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.77 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL339030 | — | — | 1 | 6.52 |
| CHEMBL333888 | — | — | 1 | 6.52 |
| CHEMBL122262 | — | — | 1 | 6.40 |
| CHEMBL331492 | — | — | 1 | 6.40 |
| CHEMBL420159 | — | — | 1 | 6.30 |
| CHEMBL339999 | — | — | 1 | 6.22 |
| CHEMBL421456 | — | — | 1 | 6.22 |
| CHEMBL123933 | — | — | 1 | 6.16 |
| CHEMBL124794 | — | — | 1 | 6.16 |
| CHEMBL125490 | — | — | 1 | 6.16 |
| CHEMBL338009 | — | — | 1 | 6.16 |
| CHEMBL122174 | — | — | 1 | 6.10 |
| CHEMBL334080 | — | — | 1 | 6.00 |
| CHEMBL339135 | — | — | 1 | 5.92 |
| CHEMBL124531 | — | — | 1 | 5.85 |
| CHEMBL332525 | — | — | 1 | 5.85 |
| CHEMBL125290 | — | — | 1 | 5.82 |
| CHEMBL121816 | — | — | 1 | 5.80 |
| CHEMBL125115 | — | — | 1 | 5.68 |
| CHEMBL249837 | METHACYCLINE | 4.0 | 1 | 5.60 |
| CHEMBL1434 | MINOCYCLINE | 4.0 | 1 | 5.58 |
| CHEMBL125158 | — | — | 1 | 5.33 |
| CHEMBL338161 | — | — | 1 | 5.33 |
| CHEMBL338028 | — | — | 1 | 5.28 |
| CHEMBL338852 | — | — | 1 | 5.24 |
| CHEMBL334155 | — | — | 1 | 5.16 |
| CHEMBL123848 | — | — | 1 | 5.10 |
| CHEMBL338688 | — | — | 1 | 4.95 |
| CHEMBL1440 | TETRACYCLINE | 4.0 | 1 | 4.88 |
| CHEMBL332172 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL339030 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL333888 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL122262 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL331492 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL420159 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL339999 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL421456 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL123933 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL124794 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL125490 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL338009 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL122174 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL334080 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL339135 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL124531 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL332525 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL125290 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL121816 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL125115 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL249837 | METHACYCLINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1434 | MINOCYCLINE | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL125158 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL338161 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL338028 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL338852 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL334155 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL123848 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL338688 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL1440 | TETRACYCLINE | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL332172 | — | IC50 | = | 43200.0 | nM | 4.37 |