Assay Detail
Binding
CHEMBL1960211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrs
31
Total Activities
31
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
Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.41 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957366 | — | — | 1 | 9.00 |
| CHEMBL1957460 | — | — | 1 | 9.00 |
| CHEMBL1957367 | — | — | 1 | 8.70 |
| CHEMBL1957375 | — | — | 1 | 8.52 |
| CHEMBL1955881 | — | — | 1 | 8.52 |
| CHEMBL248380 | — | — | 1 | 8.10 |
| CHEMBL1957369 | — | — | 1 | 8.10 |
| CHEMBL1957374 | — | — | 1 | 8.05 |
| CHEMBL1957361 | — | — | 1 | 7.92 |
| CHEMBL1957462 | — | — | 1 | 7.89 |
| CHEMBL1957364 | — | — | 1 | 7.89 |
| CHEMBL1957373 | — | — | 1 | 7.68 |
| CHEMBL1957368 | — | — | 1 | 7.66 |
| CHEMBL1957381 | — | — | 1 | 7.57 |
| CHEMBL1957370 | — | — | 1 | 7.51 |
| CHEMBL1235237 | — | — | 1 | 7.46 |
| CHEMBL19224 | PAPAVERINE | 3.0 | 1 | 7.44 |
| CHEMBL1957379 | — | — | 1 | 7.28 |
| CHEMBL1957363 | — | — | 1 | 7.19 |
| CHEMBL1957377 | — | — | 1 | 7.17 |
| CHEMBL1957380 | — | — | 1 | 7.01 |
| CHEMBL1957365 | — | — | 1 | 6.97 |
| CHEMBL1957376 | — | — | 1 | 6.84 |
| CHEMBL1957362 | — | — | 1 | 6.50 |
| CHEMBL1957378 | — | — | 1 | 6.34 |
| CHEMBL1957360 | — | — | 1 | 6.25 |
| CHEMBL1957461 | — | — | 1 | 6.22 |
| CHEMBL1957372 | — | — | 1 | 6.13 |
| CHEMBL1957359 | — | — | 1 | 5.76 |
| CHEMBL1957371 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957366 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1957460 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1957367 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1957375 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1955881 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL248380 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1957369 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1957374 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1957361 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1957462 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1957364 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1957373 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1957368 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1957381 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1957370 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1235237 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL19224 | PAPAVERINE | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1957379 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1957363 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1957377 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1957380 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1957365 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL1957376 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL1957362 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL1957378 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL1957360 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL1957461 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL1957372 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL1957359 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL1957371 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL562513 | — | IC50 | < | 1.0 | nM | - |