Assay Detail
Binding
CHEMBL760830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit 50% activity of phosphodiesterase VA isoenzyme at 100 uM
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.13 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL144196 | — | — | 1 | 7.30 |
| CHEMBL144400 | — | — | 1 | 6.85 |
| CHEMBL423559 | — | — | 1 | 6.62 |
| CHEMBL142238 | — | — | 1 | 6.52 |
| CHEMBL436402 | — | — | 1 | 6.36 |
| CHEMBL142782 | — | — | 1 | 6.08 |
| CHEMBL28079 | ZAPRINAST | 2.0 | 1 | 6.05 |
| CHEMBL357921 | — | — | 1 | 6.05 |
| CHEMBL144341 | — | — | 1 | 5.92 |
| CHEMBL145159 | — | — | 1 | 5.66 |
| CHEMBL359185 | — | — | 1 | 5.52 |
| CHEMBL357851 | — | — | 1 | 5.44 |
| CHEMBL356928 | — | — | 1 | 5.19 |
| CHEMBL423933 | — | — | 1 | 5.08 |
| CHEMBL142969 | — | — | 1 | 5.01 |
| CHEMBL342998 | — | — | 1 | 4.96 |
| CHEMBL355919 | — | — | 1 | 4.89 |
| CHEMBL144374 | — | — | 1 | 4.85 |
| CHEMBL144940 | — | — | 1 | 4.70 |
| CHEMBL358296 | — | — | 1 | 4.70 |
| CHEMBL358574 | — | — | 1 | 4.66 |
| CHEMBL144545 | — | — | 1 | 4.62 |
| CHEMBL341866 | — | — | 1 | 4.50 |
| CHEMBL357428 | — | — | 1 | 4.47 |
| CHEMBL356138 | — | — | 1 | 4.43 |
| CHEMBL142922 | — | — | 1 | 4.43 |
| CHEMBL439809 | — | — | 1 | 4.42 |
| CHEMBL144656 | — | — | 1 | 4.42 |
| CHEMBL144047 | — | — | 1 | 4.40 |
| CHEMBL358721 | — | — | 1 | 4.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL144196 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL144400 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL423559 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL142238 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL436402 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL142782 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL28079 | ZAPRINAST | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL357921 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL144341 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL145159 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL359185 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL357851 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL356928 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL423933 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL142969 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL342998 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL355919 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL144374 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL358296 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL144940 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL358574 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL144545 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL341866 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL357428 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL356138 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL142922 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL439809 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL144656 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL144047 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL358721 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL344720 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL144978 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL145515 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL146165 | — | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL356323 | CIPAMFYLLINE | IC50 | = | 71000.0 | nM | 4.15 |