Assay Detail
Binding
CHEMBL989823
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human PDE4D2 expressed in Escherichia coli BL21 by liquid scintillation counting
91
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and structure-activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 91 | 5.68 | 7.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL458298 | — | — | 2 | 7.74 |
| CHEMBL511686 | — | — | 2 | 7.66 |
| CHEMBL45834 | — | — | 1 | 7.55 |
| CHEMBL508134 | — | — | 2 | 7.21 |
| CHEMBL47113 | — | — | 1 | 7.15 |
| CHEMBL456591 | — | — | 2 | 6.75 |
| CHEMBL457663 | — | — | 2 | 6.75 |
| CHEMBL517124 | — | — | 1 | 6.70 |
| CHEMBL456573 | — | — | 2 | 6.70 |
| CHEMBL458297 | — | — | 2 | 6.46 |
| CHEMBL457215 | — | — | 2 | 6.42 |
| CHEMBL45055 | — | — | 1 | 6.40 |
| CHEMBL456574 | — | — | 2 | 6.40 |
| CHEMBL456590 | — | — | 2 | 6.39 |
| CHEMBL456617 | — | — | 2 | 6.30 |
| CHEMBL63 | ROLIPRAM | 2.0 | 2 | 6.26 |
| CHEMBL458933 | — | — | 2 | 6.20 |
| CHEMBL45854 | — | — | 1 | 6.19 |
| CHEMBL458932 | — | — | 2 | 6.18 |
| CHEMBL443679 | — | — | 2 | 6.14 |
| CHEMBL457662 | — | — | 2 | 5.96 |
| CHEMBL298000 | — | — | 1 | 5.80 |
| CHEMBL456327 | — | — | 2 | 5.72 |
| CHEMBL458931 | — | — | 2 | 5.66 |
| CHEMBL516301 | — | — | 2 | 5.64 |
| CHEMBL513099 | — | — | 2 | 5.59 |
| CHEMBL460188 | — | — | 2 | 5.59 |
| CHEMBL44109 | — | — | 1 | 5.51 |
| CHEMBL456368 | — | — | 2 | 5.46 |
| CHEMBL456618 | — | — | 2 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL458298 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL511686 | — | IC50 | = | 21.88 | nM | 7.66 |
| CHEMBL458298 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL45834 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL511686 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL508134 | — | IC50 | = | 61.66 | nM | 7.21 |
| CHEMBL508134 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL47113 | — | IC50 | = | 70.79 | nM | 7.15 |
| CHEMBL457663 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL456591 | — | IC50 | = | 177.83 | nM | 6.75 |
| CHEMBL457663 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL456591 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL517124 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL456573 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL456573 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL458297 | — | IC50 | = | 346.74 | nM | 6.46 |
| CHEMBL458297 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL457215 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL457215 | — | IC50 | = | 380.19 | nM | 6.42 |
| CHEMBL45055 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL456574 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL456590 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL456590 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL456574 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL456617 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 549.54 | nM | 6.26 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL458933 | — | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL458933 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL45854 | — | IC50 | = | 645.65 | nM | 6.19 |
| CHEMBL458932 | — | IC50 | = | 667.0 | nM | 6.18 |
| CHEMBL458932 | — | IC50 | = | 660.69 | nM | 6.18 |
| CHEMBL443679 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL443679 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL456617 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL457662 | — | IC50 | = | 1096.48 | nM | 5.96 |
| CHEMBL457662 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL298000 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL456327 | — | IC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL456327 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL458931 | — | IC50 | = | 2187.76 | nM | 5.66 |
| CHEMBL458931 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL516301 | — | IC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL460188 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL513099 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL513099 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL460188 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL44109 | — | IC50 | = | 3090.3 | nM | 5.51 |
| CHEMBL456368 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL456368 | — | IC50 | = | 3467.37 | nM | 5.46 |