Assay Detail
Binding
CHEMBL2175366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Trypanosoma brucei recombinant TbrPDEB1 expressed in Sf21 insect cells assessed as reduction of [3H]-cAMP hydrolysis by scintillation proximity assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Class 1 phosphodiesterase PDEB1 (CHEMBL2010636) ↗| Type | SINGLE PROTEIN |
| Organism | Trypanosoma brucei |
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 | 5.95 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171452 | — | — | 1 | 7.31 |
| CHEMBL2171451 | — | — | 1 | 6.80 |
| CHEMBL2171460 | — | — | 1 | 6.60 |
| CHEMBL2171456 | — | — | 1 | 6.40 |
| CHEMBL2171660 | — | — | 1 | 6.39 |
| CHEMBL2171461 | — | — | 1 | 6.30 |
| CHEMBL2171664 | — | — | 1 | 6.30 |
| CHEMBL2171462 | — | — | 1 | 6.20 |
| CHEMBL2171459 | — | — | 1 | 6.20 |
| CHEMBL2171458 | — | — | 1 | 6.10 |
| CHEMBL2171658 | — | — | 1 | 6.10 |
| CHEMBL2171657 | — | — | 1 | 6.08 |
| CHEMBL2171457 | — | — | 1 | 6.00 |
| CHEMBL2171663 | — | — | 1 | 6.00 |
| CHEMBL2171651 | — | — | 1 | 5.70 |
| CHEMBL2171656 | — | — | 1 | 5.70 |
| CHEMBL2171655 | — | — | 1 | 5.70 |
| CHEMBL2171654 | — | — | 1 | 5.60 |
| CHEMBL2171453 | — | — | 1 | 5.60 |
| CHEMBL2171454 | — | — | 1 | 5.30 |
| CHEMBL2171455 | — | — | 1 | 5.30 |
| CHEMBL2171661 | — | — | 1 | 5.20 |
| CHEMBL2171662 | — | — | 1 | 5.00 |
| CHEMBL2171659 | — | — | 1 | 4.92 |
| CHEMBL2171653 | — | — | 1 | - |
| CHEMBL2171652 | — | — | 1 | - |
| CHEMBL2171650 | — | — | 1 | - |
| CHEMBL2171465 | — | — | 1 | - |
| CHEMBL2171464 | — | — | 1 | - |
| CHEMBL2171463 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171452 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2171451 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2171460 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2171456 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2171660 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2171461 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2171664 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2171462 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2171459 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2171458 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL2171658 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL2171657 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL2171457 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2171663 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2171651 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2171656 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2171655 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2171654 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2171453 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2171454 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2171455 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2171661 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2171662 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2171659 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2171653 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2171652 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2171650 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2171465 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2171464 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2171463 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL63 | ROLIPRAM | IC50 | > | 100000.0 | nM | - |