Assay Detail
Binding
CHEMBL1918958
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His-tagged human PDE10A expressed in Escherichia coli using [3H]cAMP after 1 hr by scintillation proximity assay
79
Total Activities
79
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
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (CHEMBL4409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 79 | 8.14 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1916128 | — | — | 1 | 10.30 |
| CHEMBL1916129 | — | — | 1 | 10.22 |
| CHEMBL1916130 | — | — | 1 | 10.05 |
| CHEMBL1916127 | — | — | 1 | 10.00 |
| CHEMBL1916125 | — | — | 1 | 9.85 |
| CHEMBL1916124 | — | — | 1 | 9.70 |
| CHEMBL1916117 | — | — | 1 | 9.46 |
| CHEMBL1916123 | — | — | 1 | 9.30 |
| CHEMBL1916114 | — | — | 1 | 9.26 |
| CHEMBL1916132 | — | — | 1 | 9.15 |
| CHEMBL1916113 | — | — | 1 | 9.15 |
| CHEMBL1916131 | — | — | 1 | 9.10 |
| CHEMBL1916116 | — | — | 1 | 9.07 |
| CHEMBL1916135 | — | — | 1 | 8.82 |
| CHEMBL1916115 | — | — | 1 | 8.82 |
| CHEMBL1916126 | — | — | 1 | 8.77 |
| CHEMBL1915896 | — | — | 1 | 8.74 |
| CHEMBL1916118 | — | — | 1 | 8.72 |
| CHEMBL1915890 | — | — | 1 | 8.72 |
| CHEMBL1916112 | — | — | 1 | 8.70 |
| CHEMBL1915906 | — | — | 1 | 8.55 |
| CHEMBL1916139 | — | — | 1 | 8.54 |
| CHEMBL1916136 | — | — | 1 | 8.46 |
| CHEMBL1916095 | — | — | 1 | 8.44 |
| CHEMBL1915912 | — | — | 1 | 8.43 |
| CHEMBL1916134 | — | — | 1 | 8.41 |
| CHEMBL1916090 | — | — | 1 | 8.38 |
| CHEMBL1915892 | — | — | 1 | 8.37 |
| CHEMBL1916094 | — | — | 1 | 8.28 |
| CHEMBL1916137 | — | — | 1 | 8.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1916128 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL1916129 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL1916130 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL1916127 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1916125 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL1916124 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1916117 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL1916123 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1916114 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL1916132 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1916113 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1916131 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1916116 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL1916115 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1916135 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1916126 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1915896 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1916118 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1915890 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1916112 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1915906 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL1916139 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1916136 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1916095 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1915912 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1916134 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1916090 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL1915892 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1916094 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL1916137 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL1916138 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL1915905 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1915910 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL1916109 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL1915904 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL1086110 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL1916108 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1915891 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1915888 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1916119 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL1916093 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL1916106 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL1916103 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1916091 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1916120 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL1916133 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL1915909 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL1916089 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL1916096 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL1915908 | — | IC50 | = | 14.2 | nM | 7.85 |