Assay Detail
Binding
CHEMBL3769086
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Trypanosoma brucei PDEB1 using [3H]-cAMP as substrate after 15 mins by scintillation proximity assay
24
Total Activities
23
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
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.80 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3765188 | — | — | 1 | 8.50 |
| CHEMBL2326941 | — | — | 2 | 8.40 |
| CHEMBL3763233 | — | — | 1 | 8.00 |
| CHEMBL3765037 | — | — | 1 | 7.90 |
| CHEMBL3764370 | — | — | 1 | 7.80 |
| CHEMBL3765786 | — | — | 1 | 7.20 |
| CHEMBL3765606 | — | — | 1 | 7.20 |
| CHEMBL3765010 | — | — | 1 | 7.20 |
| CHEMBL3763352 | — | — | 1 | 7.10 |
| CHEMBL3765222 | — | — | 1 | 7.10 |
| CHEMBL3764909 | — | — | 1 | 7.00 |
| CHEMBL3765581 | — | — | 1 | 7.00 |
| CHEMBL3765225 | — | — | 1 | 6.90 |
| CHEMBL3765733 | — | — | 1 | 6.80 |
| CHEMBL3763271 | — | — | 1 | 6.50 |
| CHEMBL3763456 | — | — | 1 | 6.50 |
| CHEMBL3763547 | — | — | 1 | 5.80 |
| CHEMBL3764415 | — | — | 1 | 5.70 |
| CHEMBL3764366 | — | — | 1 | 5.40 |
| CHEMBL3763265 | — | — | 1 | 5.00 |
| CHEMBL440878 | — | — | 1 | 4.90 |
| CHEMBL3764675 | — | — | 1 | 4.00 |
| CHEMBL3764466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3765188 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL2326941 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2326941 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL3763233 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3765037 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3764370 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3765786 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3765606 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3765010 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3763352 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3765222 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3764909 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3765581 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3765225 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3765733 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3763271 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3763456 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3763547 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3764415 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3764366 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3763265 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL440878 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3764675 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL3764466 | — | IC50 | > | 10000.0 | nM | - |