Assay Detail
Binding
CHEMBL3707515
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Scintillation Proximity Assay: The ability of a compound to inhibit PDE10 enzymatic activity can be demonstrated by any number of assays that are known in the art. The products of Examples 1-175 were tested in the assay described below.PDE10 activity was measured using a scintillation assay (SPA-based method) similar to that previously described by Seeger, T. F. et al., Brain Research 985 (2003) 113-126. The compounds' relative activity as PDE10 inhibitors was investigated by assaying a fixed amount of enzyme in the presence of the test compound and low substrate concentration (cAMP) such that an IC50 could be determined. More specifically, this assay uses a Scintillation Proximity Assay (SPA) to measure the inhibition of rat1 and human recombinant2 PDE10 enzyme activity by compounds in vitro (preparation of enzymes described below). The assay is performed in a 384-well format with 50 uL assay buffer (50 mM TRIS pH 7.5; 1.3 mM MgCl2; 0.01% Brij) containing enough PDE10.
73
Total Activities
71
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
Triazine derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 73 | 8.96 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3695556 | — | — | 1 | 10.41 |
| CHEMBL3691455 | — | — | 1 | 10.35 |
| CHEMBL3695520 | — | — | 1 | 10.11 |
| CHEMBL3691413 | — | — | 1 | 9.96 |
| CHEMBL3695528 | — | — | 1 | 9.78 |
| CHEMBL3691454 | — | — | 1 | 9.74 |
| CHEMBL3691443 | — | — | 1 | 9.68 |
| CHEMBL3695526 | — | — | 1 | 9.66 |
| CHEMBL3695564 | — | — | 1 | 9.59 |
| CHEMBL3695563 | — | — | 1 | 9.58 |
| CHEMBL3691404 | — | — | 1 | 9.56 |
| CHEMBL3691406 | — | — | 2 | 9.56 |
| CHEMBL3695522 | — | — | 1 | 9.55 |
| CHEMBL3695537 | — | — | 1 | 9.53 |
| CHEMBL3695532 | — | — | 1 | 9.48 |
| CHEMBL3695552 | — | — | 1 | 9.46 |
| CHEMBL3691398 | — | — | 1 | 9.42 |
| CHEMBL3695558 | — | — | 1 | 9.39 |
| CHEMBL3695557 | — | — | 1 | 9.37 |
| CHEMBL3695541 | — | — | 1 | 9.33 |
| CHEMBL3639902 | — | — | 1 | 9.31 |
| CHEMBL3691441 | — | — | 1 | 9.27 |
| CHEMBL3695515 | — | — | 1 | 9.24 |
| CHEMBL3691397 | — | — | 1 | 9.23 |
| CHEMBL3691460 | — | — | 1 | 9.21 |
| CHEMBL3695516 | — | — | 1 | 9.20 |
| CHEMBL3691461 | — | — | 1 | 9.18 |
| CHEMBL3695548 | — | — | 1 | 9.12 |
| CHEMBL3695555 | — | — | 1 | 9.11 |
| CHEMBL3639944 | — | — | 1 | 9.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3695556 | — | IC50 | = | 0.0386 | nM | 10.41 |
| CHEMBL3691455 | — | IC50 | = | 0.0444 | nM | 10.35 |
| CHEMBL3695520 | — | IC50 | = | 0.0777 | nM | 10.11 |
| CHEMBL3691413 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3695528 | — | IC50 | = | 0.166 | nM | 9.78 |
| CHEMBL3691454 | — | IC50 | = | 0.182 | nM | 9.74 |
| CHEMBL3691443 | — | IC50 | = | 0.211 | nM | 9.68 |
| CHEMBL3695526 | — | IC50 | = | 0.219 | nM | 9.66 |
| CHEMBL3695564 | — | IC50 | = | 0.257 | nM | 9.59 |
| CHEMBL3695563 | — | IC50 | = | 0.265 | nM | 9.58 |
| CHEMBL3691406 | — | IC50 | = | 0.277 | nM | 9.56 |
| CHEMBL3691404 | — | IC50 | = | 0.275 | nM | 9.56 |
| CHEMBL3695522 | — | IC50 | = | 0.279 | nM | 9.55 |
| CHEMBL3695537 | — | IC50 | = | 0.295 | nM | 9.53 |
| CHEMBL3695532 | — | IC50 | = | 0.333 | nM | 9.48 |
| CHEMBL3695552 | — | IC50 | = | 0.345 | nM | 9.46 |
| CHEMBL3691406 | — | IC50 | = | 0.346 | nM | 9.46 |
| CHEMBL3691398 | — | IC50 | = | 0.384 | nM | 9.42 |
| CHEMBL3695558 | — | IC50 | = | 0.406 | nM | 9.39 |
| CHEMBL3695557 | — | IC50 | = | 0.427 | nM | 9.37 |
| CHEMBL3695541 | — | IC50 | = | 0.468 | nM | 9.33 |
| CHEMBL3639902 | — | IC50 | = | 0.486 | nM | 9.31 |
| CHEMBL3691441 | — | IC50 | = | 0.539 | nM | 9.27 |
| CHEMBL3695515 | — | IC50 | = | 0.573 | nM | 9.24 |
| CHEMBL3691397 | — | IC50 | = | 0.582 | nM | 9.23 |
| CHEMBL3691460 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL3695516 | — | IC50 | = | 0.625 | nM | 9.20 |
| CHEMBL3691461 | — | IC50 | = | 0.664 | nM | 9.18 |
| CHEMBL3695548 | — | IC50 | = | 0.755 | nM | 9.12 |
| CHEMBL3695555 | — | IC50 | = | 0.785 | nM | 9.11 |
| CHEMBL3639944 | — | IC50 | = | 0.801 | nM | 9.10 |
| CHEMBL3691390 | — | IC50 | = | 0.876 | nM | 9.06 |
| CHEMBL3691396 | — | IC50 | = | 0.891 | nM | 9.05 |
| CHEMBL3691409 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL3695536 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3695518 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3695545 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL3691427 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL3695561 | — | IC50 | = | 1.14 | nM | 8.94 |
| CHEMBL3695503 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL3695525 | — | IC50 | = | 1.31 | nM | 8.88 |
| CHEMBL3691394 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL3691416 | — | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL3695512 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL3695543 | — | IC50 | = | 1.78 | nM | 8.75 |
| CHEMBL3695553 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL3691439 | — | IC50 | = | 1.95 | nM | 8.71 |
| CHEMBL3695514 | — | IC50 | = | 2.34 | nM | 8.63 |
| CHEMBL3691389 | — | IC50 | = | 2.51 | nM | 8.60 |
| CHEMBL3691392 | — | IC50 | = | 2.53 | nM | 8.60 |