Assay Detail
Binding
CHEMBL3706152
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Inhibition Assay: An IMAP TR-FRET assay was used to analyze the enzyme activity (Molecular Devices Corp., Sunnyvale Calif.). 5 μL of serial diluted PDE10A (BPS Bioscience, San Diego, Calif.) or tissue homogenate was incubated with equal volumes of diluted fluorescein labeled cAMP or cGMP for 60 min in 384-well polystyrene assay plates (Corning, Corning, N.Y.) at room temperature. After incubation, the reaction was stopped by adding 60 μL of diluted binding reagents and was incubated for 3 hours to overnight at room temperature. The plates were read on an Envision (Perkin Elmer, Waltham, Mass.) for time resolved fluorescence resonance energy transfer.
360
Total Activities
351
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (CHEMBL6140) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 360 | 7.12 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3660647 | — | — | 3 | 10.40 |
| CHEMBL2180802 | — | — | 1 | 10.35 |
| CHEMBL3660644 | — | — | 1 | 10.26 |
| CHEMBL3660645 | — | — | 1 | 10.25 |
| CHEMBL3906366 | — | — | 1 | 10.01 |
| CHEMBL3660642 | — | — | 1 | 9.88 |
| CHEMBL3660646 | — | — | 1 | 9.77 |
| CHEMBL3660640 | — | — | 1 | 9.72 |
| CHEMBL3660643 | — | — | 1 | 9.43 |
| CHEMBL3660641 | — | — | 1 | 9.30 |
| CHEMBL3656315 | — | — | 1 | 9.01 |
| CHEMBL3660579 | — | — | 1 | 9.00 |
| CHEMBL3660632 | — | — | 1 | 9.00 |
| CHEMBL3660637 | — | — | 1 | 8.95 |
| CHEMBL3660639 | — | — | 1 | 8.94 |
| CHEMBL3660586 | — | — | 1 | 8.85 |
| CHEMBL3660499 | — | — | 1 | 8.78 |
| CHEMBL3660585 | — | — | 1 | 8.70 |
| CHEMBL3660605 | — | — | 1 | 8.70 |
| CHEMBL3660623 | — | — | 1 | 8.70 |
| CHEMBL3660634 | — | — | 1 | 8.70 |
| CHEMBL3660638 | — | — | 1 | 8.69 |
| CHEMBL3660636 | — | — | 1 | 8.64 |
| CHEMBL3660635 | — | — | 1 | 8.63 |
| CHEMBL3660581 | — | — | 1 | 8.52 |
| CHEMBL3660584 | — | — | 1 | 8.52 |
| CHEMBL3660622 | — | — | 1 | 8.52 |
| CHEMBL3660593 | — | — | 1 | 8.47 |
| CHEMBL3660607 | — | — | 1 | 8.41 |
| CHEMBL3660553 | — | — | 1 | 8.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3660647 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL2180802 | — | IC50 | = | 0.045 | nM | 10.35 |
| CHEMBL3660644 | — | IC50 | = | 0.055 | nM | 10.26 |
| CHEMBL3660645 | — | IC50 | = | 0.056 | nM | 10.25 |
| CHEMBL3906366 | — | IC50 | = | 0.098 | nM | 10.01 |
| CHEMBL3660642 | — | IC50 | = | 0.132 | nM | 9.88 |
| CHEMBL3660646 | — | IC50 | = | 0.171 | nM | 9.77 |
| CHEMBL3660640 | — | IC50 | = | 0.189 | nM | 9.72 |
| CHEMBL3660643 | — | IC50 | = | 0.369 | nM | 9.43 |
| CHEMBL3660641 | — | IC50 | = | 0.502 | nM | 9.30 |
| CHEMBL3656315 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL3660632 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3660579 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3660637 | — | IC50 | = | 1.134 | nM | 8.95 |
| CHEMBL3660639 | — | IC50 | = | 1.148 | nM | 8.94 |
| CHEMBL3660586 | — | IC50 | = | 1.422 | nM | 8.85 |
| CHEMBL3660499 | — | IC50 | = | 1.661 | nM | 8.78 |
| CHEMBL3660647 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3660634 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3660623 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3660605 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3660585 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3660638 | — | IC50 | = | 2.064 | nM | 8.69 |
| CHEMBL3660636 | — | IC50 | = | 2.298 | nM | 8.64 |
| CHEMBL3660635 | — | IC50 | = | 2.319 | nM | 8.63 |
| CHEMBL3660647 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3660581 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3660622 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3660584 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3660593 | — | IC50 | = | 3.418 | nM | 8.47 |
| CHEMBL3660607 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3660553 | — | IC50 | = | 4.944 | nM | 8.31 |
| CHEMBL3660633 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3660602 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3660583 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3660564 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL3660504 | — | IC50 | = | 5.25 | nM | 8.28 |
| CHEMBL3660546 | — | IC50 | = | 5.39 | nM | 8.27 |
| CHEMBL3660560 | — | IC50 | = | 5.914 | nM | 8.23 |
| CHEMBL3660620 | — | IC50 | = | 6.435 | nM | 8.19 |
| CHEMBL3660609 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3660603 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3660538 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3660547 | — | IC50 | = | 7.393 | nM | 8.13 |
| CHEMBL3660551 | — | IC50 | = | 7.529 | nM | 8.12 |
| CHEMBL3660603 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3639594 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3660580 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3660554 | — | IC50 | = | 8.696 | nM | 8.06 |
| CHEMBL3660582 | — | IC50 | = | 9.0 | nM | 8.05 |