Assay Detail
Binding
CHEMBL4350262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Trypanosoma brucei PDEB1 catalytic domain (565 to 918 residues) expressed in Escherichia coli BL21 incubated for 20 mins using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit based luminometry
28
Total Activities
28
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
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.94 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204999 | — | — | 1 | 7.00 |
| CHEMBL4210475 | — | — | 1 | 7.00 |
| CHEMBL4519708 | — | — | 1 | 6.40 |
| CHEMBL4464777 | — | — | 1 | 6.30 |
| CHEMBL4465919 | — | — | 1 | 6.20 |
| CHEMBL4473824 | — | — | 1 | 6.20 |
| CHEMBL4556148 | — | — | 1 | 6.10 |
| CHEMBL4520514 | — | — | 1 | 6.10 |
| CHEMBL4467085 | — | — | 1 | 6.00 |
| CHEMBL4551476 | — | — | 1 | 5.90 |
| CHEMBL4441002 | — | — | 1 | 5.90 |
| CHEMBL4543722 | — | — | 1 | 5.80 |
| CHEMBL4573706 | — | — | 1 | 5.70 |
| CHEMBL4587960 | — | — | 1 | 5.70 |
| CHEMBL4449673 | — | — | 1 | 5.40 |
| CHEMBL4544409 | — | — | 1 | 5.20 |
| CHEMBL4573906 | — | — | 1 | 5.10 |
| CHEMBL4476056 | — | — | 1 | 5.00 |
| CHEMBL4544133 | — | — | 1 | - |
| CHEMBL4445851 | — | — | 1 | - |
| CHEMBL4544549 | — | — | 1 | - |
| CHEMBL4575728 | — | — | 1 | - |
| CHEMBL4532826 | — | — | 1 | - |
| CHEMBL4541444 | — | — | 1 | - |
| CHEMBL4455736 | — | — | 1 | - |
| CHEMBL4527191 | — | — | 1 | - |
| CHEMBL4454672 | — | — | 1 | - |
| CHEMBL4470700 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204999 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4210475 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4519708 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL4464777 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4465919 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4473824 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4556148 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4520514 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4467085 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4551476 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL4441002 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL4543722 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL4573706 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL4587960 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL4449673 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL4544409 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL4573906 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL4476056 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4544133 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4445851 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4544549 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4575728 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4532826 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4541444 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4455736 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4527191 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4454672 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4470700 | — | Ki | > | 10000.0 | nM | - |