Assay Detail
Binding
CHEMBL4183750
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Inhibition of full length Trypanosoma brucei PDEB1 expressed in Sf21 insect cells using cAMP as substrate by scintillation proximity assay
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Class 1 phosphodiesterase PDEB1 (CHEMBL2010636) ↗| Type | SINGLE PROTEIN |
| Organism | Trypanosoma brucei |
Publication
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.33 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2326941 | — | — | 1 | 8.40 |
| CHEMBL4210475 | — | — | 2 | 7.40 |
| CHEMBL4204999 | — | — | 1 | 7.00 |
| CHEMBL4202975 | — | — | 1 | 6.80 |
| CHEMBL4208363 | — | — | 1 | 6.70 |
| CHEMBL4218658 | — | — | 1 | 6.60 |
| CHEMBL4214364 | — | — | 1 | 6.50 |
| CHEMBL4204966 | — | — | 1 | 6.40 |
| CHEMBL4206114 | — | — | 1 | 6.40 |
| CHEMBL4217833 | — | — | 1 | 6.40 |
| CHEMBL4209841 | — | — | 1 | 6.30 |
| CHEMBL4209331 | — | — | 1 | 6.30 |
| CHEMBL4202704 | — | — | 1 | 6.30 |
| CHEMBL4213296 | — | — | 1 | 6.30 |
| CHEMBL4216582 | — | — | 1 | 6.20 |
| CHEMBL4218119 | — | — | 1 | 6.20 |
| CHEMBL4218358 | — | — | 1 | 6.10 |
| CHEMBL4214240 | — | — | 1 | 6.10 |
| CHEMBL4213729 | — | — | 1 | 6.00 |
| CHEMBL4206395 | — | — | 1 | 5.80 |
| CHEMBL4205916 | — | — | 1 | 5.80 |
| CHEMBL4213432 | — | — | 1 | 5.70 |
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 5.50 |
| CHEMBL4209972 | — | — | 1 | 5.40 |
| CHEMBL4203531 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2326941 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL4210475 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4210475 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4204999 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4202975 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL4208363 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL4218658 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL4214364 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL4204966 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL4217833 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL4206114 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL4209841 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4209331 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4202704 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4213296 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4216582 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4218119 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4218358 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4214240 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4213729 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4206395 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL4205916 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL4213432 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL193240 | ROFLUMILAST | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL4209972 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL4203531 | — | Ki | = | 7943.28 | nM | 5.10 |