Assay Detail
ADMET
CHEMBL4183751
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human PDE4B1 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 | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 5.91 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.40 |
| CHEMBL2326941 | — | — | 1 | 9.20 |
| CHEMBL4202704 | — | — | 1 | 7.50 |
| CHEMBL4202975 | — | — | 1 | 6.80 |
| CHEMBL4210475 | — | — | 2 | 6.20 |
| CHEMBL4218119 | — | — | 1 | 6.20 |
| CHEMBL4209331 | — | — | 1 | 6.00 |
| CHEMBL4214364 | — | — | 1 | 5.70 |
| CHEMBL4204999 | — | — | 1 | 5.70 |
| CHEMBL4218658 | — | — | 1 | 5.70 |
| CHEMBL4206114 | — | — | 1 | 5.60 |
| CHEMBL4217833 | — | — | 1 | 5.60 |
| CHEMBL4206395 | — | — | 1 | 5.60 |
| CHEMBL4204966 | — | — | 1 | 5.50 |
| CHEMBL4218358 | — | — | 1 | 5.50 |
| CHEMBL4213729 | — | — | 1 | 5.50 |
| CHEMBL4208363 | — | — | 1 | 5.50 |
| CHEMBL4214240 | — | — | 1 | 5.40 |
| CHEMBL4209841 | — | — | 1 | 5.40 |
| CHEMBL4213432 | — | — | 1 | 5.20 |
| CHEMBL4213296 | — | — | 1 | 5.20 |
| CHEMBL4205916 | — | — | 1 | 5.10 |
| CHEMBL4216582 | — | — | 1 | 5.00 |
| CHEMBL4203531 | — | — | 1 | 4.90 |
| CHEMBL4209972 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL2326941 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL4202704 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL4202975 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL4218119 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4210475 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4210475 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4209331 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4218658 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL4214364 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL4204999 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL4217833 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL4206114 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL4206395 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL4218358 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL4204966 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL4213729 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL4208363 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL4214240 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL4209841 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL4213432 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL4213296 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL4205916 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL4216582 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4203531 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL4209972 | — | Ki | = | 50118.72 | nM | 4.30 |