Assay Detail
Binding
CHEMBL4425335
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His6-tagged PDE10A2 catalytic domain expressed in Escherichia coli BL21(DE3) RIL cells using 3',5'-cGMP as substrate by colorimetric assay
18
Total Activities
18
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
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 5.01 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4583461 | — | — | 1 | 5.96 |
| CHEMBL4453729 | — | — | 1 | 5.26 |
| CHEMBL3092391 | — | — | 1 | 4.80 |
| CHEMBL167727 | — | — | 1 | 4.03 |
| CHEMBL164921 | — | — | 1 | - |
| CHEMBL4436742 | — | — | 1 | - |
| CHEMBL4466464 | — | — | 1 | - |
| CHEMBL164449 | — | — | 1 | - |
| CHEMBL266540 | QUINAZOLINONE | — | 1 | - |
| CHEMBL395092 | — | — | 1 | - |
| CHEMBL1409793 | — | — | 1 | - |
| CHEMBL165372 | — | — | 1 | - |
| CHEMBL4582404 | — | — | 1 | - |
| CHEMBL3981727 | — | — | 1 | - |
| CHEMBL4546836 | — | — | 1 | - |
| CHEMBL4517551 | — | — | 1 | - |
| CHEMBL1413383 | — | — | 1 | - |
| CHEMBL4557075 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4583461 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4453729 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL3092391 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL167727 | — | Ki | = | 94000.0 | nM | 4.03 |
| CHEMBL164921 | — | Ki | = | 500000.0 | nM | - |
| CHEMBL4436742 | — | Ki | = | 450000.0 | nM | - |
| CHEMBL4466464 | — | Ki | = | 380000.0 | nM | - |
| CHEMBL164449 | — | Ki | = | 590000.0 | nM | - |
| CHEMBL266540 | QUINAZOLINONE | Ki | = | 910000.0 | nM | - |
| CHEMBL395092 | — | Ki | = | 990000.0 | nM | - |
| CHEMBL1409793 | — | Ki | = | 500000.0 | nM | - |
| CHEMBL165372 | — | Ki | = | 560000.0 | nM | - |
| CHEMBL4582404 | — | Ki | = | 940000.0 | nM | - |
| CHEMBL3981727 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL4546836 | — | Ki | = | 1300000.0 | nM | - |
| CHEMBL4517551 | — | Ki | = | 410000.0 | nM | - |
| CHEMBL1413383 | — | Ki | = | 210000.0 | nM | - |
| CHEMBL4557075 | — | Ki | = | 1200000.0 | nM | - |