Assay Detail
Functional
CHEMBL5370873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antileishmanial activity against promastigote stage of Leishmania braziliensis MHOM/BR/75/M2904 infected in human THP-1 cells assessed as parasite growth inhibition incubated for 72 hrs by microplate reader analysis
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Leishmania braziliensis |
| Cell Type | THP-1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Hit-to-lead optimization of a pyrazinylpiperazine series against Leishmania infantum and Leishmania braziliensis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 4.81 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267345 | AMPHOTERICIN B | 4.0 | 1 | 6.89 |
| CHEMBL5402532 | — | — | 1 | 6.70 |
| CHEMBL5406357 | — | — | 1 | 5.58 |
| CHEMBL5430423 | — | — | 1 | 5.35 |
| CHEMBL5418830 | — | — | 1 | 5.23 |
| CHEMBL5437482 | — | — | 1 | 5.12 |
| CHEMBL5430852 | — | — | 1 | 5.11 |
| CHEMBL5398251 | — | — | 1 | 5.05 |
| CHEMBL5426223 | — | — | 1 | 5.04 |
| CHEMBL5436490 | — | — | 1 | 5.03 |
| CHEMBL5416460 | — | — | 1 | 5.03 |
| CHEMBL5396330 | — | — | 1 | 5.00 |
| CHEMBL5407179 | — | — | 1 | 5.00 |
| CHEMBL3431258 | — | — | 1 | 4.93 |
| CHEMBL5396842 | — | — | 1 | 4.92 |
| CHEMBL5434127 | — | — | 1 | 4.88 |
| CHEMBL5429046 | — | — | 1 | 4.85 |
| CHEMBL5414096 | — | — | 1 | 4.76 |
| CHEMBL5400035 | — | — | 1 | 4.76 |
| CHEMBL5416563 | — | — | 1 | 4.72 |
| CHEMBL5394006 | — | — | 1 | 4.64 |
| CHEMBL5438033 | — | — | 1 | 4.61 |
| CHEMBL5428957 | — | — | 1 | 4.59 |
| CHEMBL5402709 | — | — | 1 | 4.57 |
| CHEMBL5419956 | — | — | 1 | 4.51 |
| CHEMBL5431973 | — | — | 1 | 4.49 |
| CHEMBL5428270 | — | — | 1 | 4.47 |
| CHEMBL5412591 | — | — | 1 | 4.46 |
| CHEMBL5429051 | — | — | 1 | 4.25 |
| CHEMBL5397842 | — | — | 1 | 4.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267345 | AMPHOTERICIN B | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5402532 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5406357 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5430423 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5418830 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL5437482 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL5430852 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL5398251 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL5426223 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL5436490 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL5416460 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL5407179 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL5396330 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL3431258 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL5396842 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL5434127 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL5429046 | — | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL5414096 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL5400035 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL5416563 | — | IC50 | = | 19100.0 | nM | 4.72 |
| CHEMBL5394006 | — | IC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL5438033 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL5428957 | — | IC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL5402709 | — | IC50 | = | 27100.0 | nM | 4.57 |
| CHEMBL5419956 | — | IC50 | = | 30600.0 | nM | 4.51 |
| CHEMBL5431973 | — | IC50 | = | 32100.0 | nM | 4.49 |
| CHEMBL5428270 | — | IC50 | = | 33600.0 | nM | 4.47 |
| CHEMBL5412591 | — | IC50 | = | 34900.0 | nM | 4.46 |
| CHEMBL5429051 | — | IC50 | = | 55700.0 | nM | 4.25 |
| CHEMBL5397842 | — | IC50 | = | 69200.0 | nM | 4.16 |
| CHEMBL5407537 | — | IC50 | = | 74600.0 | nM | 4.13 |
| CHEMBL5430403 | — | IC50 | = | 82100.0 | nM | 4.09 |
| CHEMBL5398366 | — | IC50 | = | 85200.0 | nM | 4.07 |
| CHEMBL5413093 | — | IC50 | = | 93400.0 | nM | 4.03 |
| CHEMBL5411027 | — | IC50 | = | 94000.0 | nM | 4.03 |
| CHEMBL1877859 | — | IC50 | = | 94100.0 | nM | 4.03 |
| CHEMBL5438796 | — | IC50 | = | 161000.0 | nM | - |
| CHEMBL5430658 | — | IC50 | = | 184400.0 | nM | - |
| CHEMBL5439730 | — | IC50 | = | 337400.0 | nM | - |
| CHEMBL5433944 | — | IC50 | = | 132300.0 | nM | - |
| CHEMBL5425292 | — | IC50 | = | 3541000.0 | nM | - |
| CHEMBL5416541 | — | IC50 | = | 113400.0 | nM | - |