Assay Detail
Binding
CHEMBL2071880
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Inhibition of human recombinant PDE10A-catalyzed cAMP hydrolysis
42
Total Activities
42
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
Novel triazines as potent and selective phosphodiesterase 10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 8.00 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2069321 | — | — | 1 | 9.55 |
| CHEMBL2070655 | — | — | 1 | 9.07 |
| CHEMBL2070651 | — | — | 1 | 8.83 |
| CHEMBL2070666 | — | — | 1 | 8.83 |
| CHEMBL2070654 | — | — | 1 | 8.81 |
| CHEMBL2070664 | — | — | 1 | 8.78 |
| CHEMBL2070668 | — | — | 1 | 8.73 |
| CHEMBL2070653 | — | — | 1 | 8.69 |
| CHEMBL2070648 | — | — | 1 | 8.62 |
| CHEMBL2070647 | — | — | 1 | 8.48 |
| CHEMBL2070650 | — | — | 1 | 8.47 |
| CHEMBL2070659 | — | — | 1 | 8.45 |
| CHEMBL2070656 | — | — | 1 | 8.40 |
| CHEMBL2070652 | — | — | 1 | 8.38 |
| CHEMBL2070667 | — | — | 1 | 8.29 |
| CHEMBL2070649 | — | — | 1 | 8.29 |
| CHEMBL2070657 | — | — | 1 | 8.19 |
| CHEMBL2070669 | — | — | 1 | 8.15 |
| CHEMBL2070661 | — | — | 1 | 8.14 |
| CHEMBL2070662 | — | — | 1 | 8.11 |
| CHEMBL2070670 | — | — | 1 | 8.08 |
| CHEMBL2070658 | — | — | 1 | 8.04 |
| CHEMBL2070671 | — | — | 1 | 8.03 |
| CHEMBL2070641 | — | — | 1 | 8.01 |
| CHEMBL2070645 | — | — | 1 | 8.00 |
| CHEMBL2070665 | — | — | 1 | 7.93 |
| CHEMBL2070646 | — | — | 1 | 7.91 |
| CHEMBL2070639 | — | — | 1 | 7.88 |
| CHEMBL2070663 | — | — | 1 | 7.88 |
| CHEMBL2070631 | — | — | 1 | 7.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2069321 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL2070655 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL2070666 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL2070651 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL2070654 | — | IC50 | = | 1.53 | nM | 8.81 |
| CHEMBL2070664 | — | IC50 | = | 1.65 | nM | 8.78 |
| CHEMBL2070668 | — | IC50 | = | 1.85 | nM | 8.73 |
| CHEMBL2070653 | — | IC50 | = | 2.06 | nM | 8.69 |
| CHEMBL2070648 | — | IC50 | = | 2.41 | nM | 8.62 |
| CHEMBL2070647 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2070650 | — | IC50 | = | 3.35 | nM | 8.47 |
| CHEMBL2070659 | — | IC50 | = | 3.55 | nM | 8.45 |
| CHEMBL2070656 | — | IC50 | = | 3.99 | nM | 8.40 |
| CHEMBL2070652 | — | IC50 | = | 4.16 | nM | 8.38 |
| CHEMBL2070649 | — | IC50 | = | 5.13 | nM | 8.29 |
| CHEMBL2070667 | — | IC50 | = | 5.11 | nM | 8.29 |
| CHEMBL2070657 | — | IC50 | = | 6.53 | nM | 8.19 |
| CHEMBL2070669 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2070661 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2070662 | — | IC50 | = | 7.84 | nM | 8.11 |
| CHEMBL2070670 | — | IC50 | = | 8.33 | nM | 8.08 |
| CHEMBL2070658 | — | IC50 | = | 9.11 | nM | 8.04 |
| CHEMBL2070671 | — | IC50 | = | 9.43 | nM | 8.03 |
| CHEMBL2070641 | — | IC50 | = | 9.83 | nM | 8.01 |
| CHEMBL2070645 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL2070665 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL2070646 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL2070639 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL2070663 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL2070631 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL2070640 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2070660 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL2070644 | — | IC50 | = | 42.4 | nM | 7.37 |
| CHEMBL2070633 | — | IC50 | = | 45.9 | nM | 7.34 |
| CHEMBL2070634 | — | IC50 | = | 47.6 | nM | 7.32 |
| CHEMBL2070637 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL2070632 | — | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL2070635 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL2070636 | — | IC50 | = | 91.3 | nM | 7.04 |
| CHEMBL2070642 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL2070638 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL2070643 | — | IC50 | = | 2430.0 | nM | 5.61 |