Assay Detail
Functional
CHEMBL2344963
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Antitubercular activity against Mycobacterium tuberculosis H37Rv by BacTiter-Gl Microbial Cell Viability assay
54
Total Activities
20
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mycobacterium tuberculosis |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines acting as antimycobacterial agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 5.34 | 7.70 |
| EC90 | 20 | - | - |
| MIC | 14 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374478 | RIFAMPIN | 4.0 | 3 | 7.70 |
| CHEMBL177 | AMIKACIN | 4.0 | 3 | 7.16 |
| CHEMBL64 | ISONIAZID | 4.0 | 3 | 6.89 |
| CHEMBL44884 | ETHAMBUTOL | 4.0 | 3 | 5.82 |
| CHEMBL2331869 | — | — | 3 | 5.66 |
| CHEMBL2331856 | — | — | 3 | 5.49 |
| CHEMBL2331868 | — | — | 3 | 5.20 |
| CHEMBL2331857 | — | — | 3 | 5.07 |
| CHEMBL2331865 | — | — | 2 | 5.02 |
| CHEMBL2331863 | — | — | 3 | 5.01 |
| CHEMBL2331860 | — | — | 2 | 5.00 |
| CHEMBL2331862 | — | — | 3 | 4.94 |
| CHEMBL2331861 | — | — | 3 | 4.87 |
| CHEMBL2331866 | — | — | 2 | 4.75 |
| CHEMBL2331864 | — | — | 2 | 4.72 |
| CHEMBL2331859 | — | — | 3 | 4.68 |
| CHEMBL771 | CYCLOSERINE | 4.0 | 3 | 4.63 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 3 | 4.62 |
| CHEMBL2331858 | — | — | 2 | 4.19 |
| CHEMBL2331867 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374478 | RIFAMPIN | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL177 | AMIKACIN | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL64 | ISONIAZID | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL44884 | ETHAMBUTOL | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2331869 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2331856 | — | EC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL2331868 | — | EC50 | = | 6270.0 | nM | 5.20 |
| CHEMBL2331857 | — | EC50 | = | 8510.0 | nM | 5.07 |
| CHEMBL2331865 | — | EC50 | = | 9560.0 | nM | 5.02 |
| CHEMBL2331863 | — | EC50 | = | 9870.0 | nM | 5.01 |
| CHEMBL2331860 | — | EC50 | = | 10060.0 | nM | 5.00 |
| CHEMBL2331862 | — | EC50 | = | 11510.0 | nM | 4.94 |
| CHEMBL2331861 | — | EC50 | = | 13430.0 | nM | 4.87 |
| CHEMBL2331866 | — | EC50 | = | 17750.0 | nM | 4.75 |
| CHEMBL2331864 | — | EC50 | = | 18850.0 | nM | 4.72 |
| CHEMBL2331859 | — | EC50 | = | 20740.0 | nM | 4.68 |
| CHEMBL771 | CYCLOSERINE | EC50 | = | 23550.0 | nM | 4.63 |
| CHEMBL36 | PYRIMETHAMINE | EC50 | = | 24270.0 | nM | 4.62 |
| CHEMBL2331858 | — | EC50 | = | 64460.0 | nM | 4.19 |
| CHEMBL2331868 | — | MIC | = | 50000.0 | nM | - |
| CHEMBL2331869 | — | MIC | = | 12500.0 | nM | - |
| CHEMBL2331856 | — | MIC | = | 50000.0 | nM | - |
| CHEMBL2331857 | — | MIC | = | 50000.0 | nM | - |
| CHEMBL44884 | ETHAMBUTOL | MIC | = | 6250.0 | nM | - |
| CHEMBL2331861 | — | MIC | = | 100000.0 | nM | - |
| CHEMBL2331862 | — | MIC | = | 100000.0 | nM | - |
| CHEMBL2331863 | — | MIC | = | 100000.0 | nM | - |
| CHEMBL771 | CYCLOSERINE | MIC | = | 100000.0 | nM | - |
| CHEMBL64 | ISONIAZID | MIC | = | 310.0 | nM | - |
| CHEMBL374478 | RIFAMPIN | MIC | = | 40.0 | nM | - |
| CHEMBL177 | AMIKACIN | MIC | = | 160.0 | nM | - |
| CHEMBL36 | PYRIMETHAMINE | MIC | = | 100000.0 | nM | - |
| CHEMBL2331859 | — | MIC | = | 100000.0 | nM | - |
| CHEMBL2331867 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL2331867 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL2331868 | — | EC90 | = | 29.62 | uM | - |
| CHEMBL2331869 | — | EC90 | = | 10.76 | uM | - |
| CHEMBL2331856 | — | EC90 | = | 12.29 | uM | - |
| CHEMBL2331857 | — | EC90 | = | 26.08 | uM | - |
| CHEMBL2331858 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL2331859 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL2331860 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL2331861 | — | EC90 | = | 62.37 | uM | - |
| CHEMBL2331862 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL2331863 | — | EC90 | = | 55.34 | uM | - |
| CHEMBL2331864 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL2331865 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL2331866 | — | EC90 | > | 100.0 | uM | - |
| CHEMBL64 | ISONIAZID | EC90 | = | 0.2 | uM | - |
| CHEMBL771 | CYCLOSERINE | EC90 | = | 26.38 | uM | - |