Assay Detail
Binding
CHEMBL1924908
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Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei brucei |
| Cell Type | Sf21 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.89 | 5.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 5.33 |
| CHEMBL297555 | — | — | 1 | 5.11 |
| CHEMBL372575 | — | — | 1 | 5.06 |
| CHEMBL285913 | TREQUINSIN | 2.0 | 1 | 4.92 |
| CHEMBL1922286 | — | — | 1 | 4.90 |
| CHEMBL1922284 | — | — | 1 | 4.87 |
| CHEMBL1922283 | — | — | 1 | 4.78 |
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 4.14 |
| CHEMBL1922291 | — | — | 1 | - |
| CHEMBL1922290 | — | — | 1 | - |
| CHEMBL1922289 | — | — | 1 | - |
| CHEMBL1922288 | — | — | 1 | - |
| CHEMBL1922287 | — | — | 1 | - |
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | - |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | - |
| CHEMBL1922285 | — | — | 1 | - |
| CHEMBL1922282 | LIRIMILAST | 2.0 | 1 | - |
| CHEMBL48017 | — | — | 1 | - |
| CHEMBL18701 | RO-201724 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL297555 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL372575 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL285913 | TREQUINSIN | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1922286 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL1922284 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL1922283 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL1922291 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1922290 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1922289 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1922288 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1922287 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL193240 | ROFLUMILAST | IC50 | > | 100000.0 | nM | - |
| CHEMBL63 | ROLIPRAM | IC50 | > | 100000.0 | nM | - |
| CHEMBL1922285 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1922282 | LIRIMILAST | IC50 | > | 10000.0 | nM | - |
| CHEMBL48017 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL18701 | RO-201724 | IC50 | > | 100000.0 | nM | - |