Assay Detail
Functional
CHEMBL5154110
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in human A-THP1 macrophages assessed as viability of infected macrophages incubated for 96 hrs by fluorescence microplate assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mycobacterium tuberculosis |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.38 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376488 | BEDAQUILINE | 4.0 | 1 | 7.47 |
| CHEMBL374478 | RIFAMPIN | 4.0 | 1 | 7.04 |
| CHEMBL64 | ISONIAZID | 4.0 | 1 | 6.69 |
| CHEMBL5186518 | — | — | 1 | 6.44 |
| CHEMBL5201484 | — | — | 1 | 6.34 |
| CHEMBL5202255 | — | — | 1 | 5.62 |
| CHEMBL5182198 | — | — | 1 | 5.09 |
| CHEMBL5196810 | — | — | 1 | - |
| CHEMBL5206556 | — | — | 1 | - |
| CHEMBL5171834 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376488 | BEDAQUILINE | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL374478 | RIFAMPIN | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL64 | ISONIAZID | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL5186518 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5201484 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5202255 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5182198 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL5196810 | — | IC50 | - | — | - | |
| CHEMBL5206556 | — | IC50 | - | — | - | |
| CHEMBL5171834 | — | IC50 | - | — | - |