Assay Detail
Binding
CHEMBL3578508
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Inhibition of recombinant his-tagged methicillin-resistant Staphylococcus aureus pyruvate kinase expressed in Escherichia coli BL-21(DE3) using PEP as substrate after 5 mins by L-LDH coupled assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Staphylococcus aureus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthetic analogues of the marine bisindole deoxytopsentin: potent selective inhibitors of MRSA pyruvate kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.56 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3576887 | — | — | 1 | 8.82 |
| CHEMBL465609 | DIBROMODEOXYTOPSENTIN | — | 1 | 8.68 |
| CHEMBL3576888 | — | — | 1 | 8.48 |
| CHEMBL3576889 | — | — | 1 | 8.19 |
| CHEMBL541209 | CIS-3,4-DIHYDROHAMACANTHIN B | — | 1 | 7.80 |
| CHEMBL3576886 | — | — | 1 | 7.62 |
| CHEMBL198814 | BROMODEOXYTOPSENTIN | — | 1 | 7.22 |
| CHEMBL372191 | DEOXYTOPSENTIN | — | 1 | 6.62 |
| CHEMBL3576890 | — | — | 1 | 4.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3576887 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL465609 | DIBROMODEOXYTOPSENTIN | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3576888 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3576889 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL541209 | CIS-3,4-DIHYDROHAMACANTHIN B | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3576886 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL198814 | BROMODEOXYTOPSENTIN | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL372191 | DEOXYTOPSENTIN | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3576890 | — | IC50 | = | 26000.0 | nM | 4.58 |