Assay Detail
Functional
CHEMBL2175361
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei brucei Squib-427 after 72 hrs by fluorescence assay
32
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei brucei |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.05 | 6.28 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171452 | — | — | 2 | 6.28 |
| CHEMBL2171456 | — | — | 1 | 5.70 |
| CHEMBL2171451 | — | — | 1 | 5.64 |
| CHEMBL2171461 | — | — | 1 | 5.60 |
| CHEMBL2171663 | — | — | 1 | 5.35 |
| CHEMBL2171664 | — | — | 1 | 5.20 |
| CHEMBL2171459 | — | — | 1 | 5.09 |
| CHEMBL2171462 | — | — | 1 | 5.08 |
| CHEMBL2171464 | — | — | 1 | 5.07 |
| CHEMBL2171661 | — | — | 1 | 5.07 |
| CHEMBL2171455 | — | — | 1 | 5.04 |
| CHEMBL2171457 | — | — | 1 | 5.02 |
| CHEMBL2171460 | — | — | 1 | 5.02 |
| CHEMBL2171658 | — | — | 1 | 5.02 |
| CHEMBL2171458 | — | — | 1 | 5.00 |
| CHEMBL2171651 | — | — | 1 | 5.00 |
| CHEMBL2171657 | — | — | 1 | 4.50 |
| CHEMBL2171656 | — | — | 1 | 4.50 |
| CHEMBL2171662 | — | — | 1 | 4.50 |
| CHEMBL2171454 | — | — | 1 | 4.48 |
| CHEMBL2171654 | — | — | 1 | 4.47 |
| CHEMBL2171453 | — | — | 1 | 4.46 |
| CHEMBL2171659 | — | — | 1 | - |
| CHEMBL2171660 | — | — | 1 | - |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | - |
| CHEMBL2171463 | — | — | 1 | - |
| CHEMBL2171465 | — | — | 1 | - |
| CHEMBL2171650 | — | — | 1 | - |
| CHEMBL2171652 | — | — | 1 | - |
| CHEMBL2171653 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171452 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL2171456 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2171451 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2171461 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2171663 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2171664 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2171459 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL2171462 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL2171464 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL2171661 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL2171455 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL2171457 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL2171460 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL2171658 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL2171458 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2171651 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2171662 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2171657 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2171656 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2171454 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2171654 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL2171453 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL63 | ROLIPRAM | IC50 | - | — | - | |
| CHEMBL2171660 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL2171659 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL2171452 | — | Inhibition | - | % | - | |
| CHEMBL2171463 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL2171465 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL2171650 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL2171652 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL2171653 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL2171655 | — | IC50 | > | 64000.0 | nM | - |