Assay Detail
Binding
CHEMBL863389
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Inhibitory activity against FabH from Mycobacterium tuberculosis H37Rv
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mycobacterium tuberculosis |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Mycobacterial beta-ketoacyl-[acyl-carrier-protein] synthase III (CHEMBL3640) ↗| Type | SINGLE PROTEIN |
| Organism | Mycobacterium tuberculosis |
Publication
Structure-activity relationships at the 5-position of thiolactomycin: an intact (5R)-isoprene unit is required for activity against the condensing enzymes from Mycobacterium tuberculosis and Escherichia coli.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 4.12 | 4.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL199542 | — | — | 1 | 4.30 |
| CHEMBL199976 | — | — | 1 | 4.19 |
| CHEMBL199516 | — | — | 1 | 4.12 |
| CHEMBL200655 | — | — | 1 | 4.10 |
| CHEMBL200803 | — | — | 1 | 4.10 |
| CHEMBL399043 | THIOLACTOMYCIN | — | 1 | 4.06 |
| CHEMBL372341 | — | — | 1 | 4.00 |
| CHEMBL198344 | — | — | 1 | - |
| CHEMBL381463 | — | — | 1 | - |
| CHEMBL333571 | — | — | 1 | - |
| CHEMBL199463 | — | — | 1 | - |
| CHEMBL201227 | — | — | 1 | - |
| CHEMBL202928 | — | — | 1 | - |
| CHEMBL200363 | — | — | 1 | - |
| CHEMBL202817 | — | — | 1 | - |
| CHEMBL200281 | — | — | 1 | - |
| CHEMBL200101 | — | — | 1 | - |
| CHEMBL199436 | — | — | 1 | - |
| CHEMBL199428 | — | — | 1 | - |
| CHEMBL383537 | — | — | 1 | - |
| CHEMBL380904 | — | — | 1 | - |
| CHEMBL203154 | — | — | 1 | - |
| CHEMBL432983 | — | — | 1 | - |
| CHEMBL333467 | — | — | 1 | - |
| CHEMBL201711 | — | — | 1 | - |
| CHEMBL199810 | — | — | 1 | - |
| CHEMBL123184 | — | — | 1 | - |
| CHEMBL436318 | — | — | 1 | - |
| CHEMBL382958 | — | — | 1 | - |
| CHEMBL373005 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL199542 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL199976 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL199516 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL200655 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL200803 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL399043 | THIOLACTOMYCIN | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL372341 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL201423 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL200281 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL199900 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL200240 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL196776 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL383601 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL381463 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL199436 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL200101 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL199977 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL381684 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL201261 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL379235 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL371660 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL381712 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL201541 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL201752 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL381559 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL383600 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL380904 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL373005 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL382958 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL436318 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL123184 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL199810 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL201711 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL333467 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL432983 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL203154 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL202817 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL383537 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL199428 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL198344 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL333571 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL199463 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL201227 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL202928 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL200363 | — | IC50 | > | 100000.0 | nM | - |