Assay Detail
Binding
CHEMBL2213618
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE10A
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.11 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2204542 | — | — | 1 | 9.22 |
| CHEMBL2204538 | THPP-1 | — | 1 | 9.00 |
| CHEMBL2204539 | — | — | 1 | 9.00 |
| CHEMBL2204543 | — | — | 1 | 8.52 |
| CHEMBL2204537 | — | — | 1 | 8.35 |
| CHEMBL2204544 | — | — | 1 | 8.10 |
| CHEMBL2205202 | — | — | 1 | 8.10 |
| CHEMBL2205203 | — | — | 1 | 7.85 |
| CHEMBL2205204 | — | — | 1 | 7.77 |
| CHEMBL2204541 | — | — | 1 | 7.20 |
| CHEMBL2205221 | — | — | 1 | 7.03 |
| CHEMBL2205205 | — | — | 1 | 7.03 |
| CHEMBL2205206 | — | — | 1 | 7.01 |
| CHEMBL2205216 | — | — | 1 | 6.93 |
| CHEMBL2205220 | — | — | 1 | 6.92 |
| CHEMBL2205215 | — | — | 1 | 6.91 |
| CHEMBL2205207 | — | — | 1 | 6.87 |
| CHEMBL2205214 | — | — | 1 | 6.81 |
| CHEMBL2205213 | — | — | 1 | 6.73 |
| CHEMBL2205212 | — | — | 1 | 6.65 |
| CHEMBL2204540 | — | — | 1 | 6.61 |
| CHEMBL2205208 | — | — | 1 | 6.38 |
| CHEMBL2205218 | — | — | 1 | 6.30 |
| CHEMBL2205217 | — | — | 1 | 6.29 |
| CHEMBL2205211 | — | — | 1 | 6.28 |
| CHEMBL2205209 | — | — | 1 | 6.07 |
| CHEMBL2205210 | — | — | 1 | 6.06 |
| CHEMBL2205219 | — | — | 1 | 6.06 |
| CHEMBL2205223 | — | — | 1 | 6.00 |
| CHEMBL2205222 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2204542 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2204538 | THPP-1 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2204539 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2204543 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2204537 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2204544 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2205202 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL2205203 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2205204 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2204541 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL2205221 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL2205205 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL2205206 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL2205216 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL2205220 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL2205215 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL2205207 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL2205214 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL2205213 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL2205212 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL2204540 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL2205208 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL2205218 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL2205217 | — | Ki | = | 512.0 | nM | 6.29 |
| CHEMBL2205211 | — | Ki | = | 522.0 | nM | 6.28 |
| CHEMBL2205209 | — | Ki | = | 843.0 | nM | 6.07 |
| CHEMBL2205210 | — | Ki | = | 868.0 | nM | 6.06 |
| CHEMBL2205219 | — | Ki | = | 864.0 | nM | 6.06 |
| CHEMBL2205223 | — | Ki | = | 991.0 | nM | 6.00 |
| CHEMBL2205222 | — | Ki | = | 4340.0 | nM | 5.36 |