Assay Detail
Binding
CHEMBL5737614
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ca2+-Calmodulin Dependent PDE Enzyme Assays: PDE1B, PDE1A, and PDE1C are cloned and purified following standard protein generation procedures. The assay buffer is prepared to give a final concentration in the assay of 50 mM Tris-HCl, 50 mM MgCl2, 4 mM CaCl2, 0.1% Bovine serum albumin and 6 U/ml Calmodulin in water, at pH 7.5. The final enzyme concentration is 0.25, 0.074 and 0.0012 nM, for PDE1A, PDE1B and PDE1C respectively. The reactions are started by addition of the substrate, [3H]cAMP, to give a final concentration of 47 nM.
45
Total Activities
13
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A (CHEMBL3421) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
[1,2,4]Triazolo[4,3-A]pyrazin-6(5H)-one derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.56 | 9.67 |
| kon | 15 | - | - |
| k_off | 15 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6042932 | — | — | 3 | 9.67 |
| CHEMBL5977186 | — | — | 3 | 9.59 |
| CHEMBL6057973 | — | — | 3 | 9.46 |
| CHEMBL6005179 | — | — | 3 | 9.44 |
| CHEMBL5908735 | — | — | 3 | 9.09 |
| CHEMBL5773878 | — | — | 3 | 9.00 |
| CHEMBL5844485 | — | — | 3 | 8.59 |
| CHEMBL6062186 | — | — | 3 | 8.56 |
| CHEMBL5762359 | — | — | 3 | 8.10 |
| CHEMBL5812282 | — | — | 3 | 8.06 |
| CHEMBL5945056 | — | — | 3 | 7.94 |
| CHEMBL5760003 | — | — | 9 | 7.86 |
| CHEMBL5866418 | — | — | 3 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6042932 | — | IC50 | = | 0.214 | nM | 9.67 |
| CHEMBL5977186 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL6057973 | — | IC50 | = | 0.343 | nM | 9.46 |
| CHEMBL6005179 | — | IC50 | = | 0.366 | nM | 9.44 |
| CHEMBL5908735 | — | IC50 | = | 0.816 | nM | 9.09 |
| CHEMBL5773878 | — | IC50 | = | 0.996 | nM | 9.00 |
| CHEMBL5844485 | — | IC50 | = | 2.59 | nM | 8.59 |
| CHEMBL6062186 | — | IC50 | = | 2.75 | nM | 8.56 |
| CHEMBL5762359 | — | IC50 | = | 8.01 | nM | 8.10 |
| CHEMBL5812282 | — | IC50 | = | 8.62 | nM | 8.06 |
| CHEMBL5945056 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5760003 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL5760003 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL5866418 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5760003 | — | IC50 | = | 26.8 | nM | 7.57 |
| CHEMBL6005179 | — | k_off | = | - | s-1 | - |
| CHEMBL5812282 | — | kon | = | - | — | - |
| CHEMBL5812282 | — | k_off | = | - | s-1 | - |
| CHEMBL5844485 | — | kon | = | - | — | - |
| CHEMBL5844485 | — | k_off | = | - | s-1 | - |
| CHEMBL5760003 | — | kon | = | - | — | - |
| CHEMBL5760003 | — | k_off | = | - | s-1 | - |
| CHEMBL6057973 | — | k_off | = | - | s-1 | - |
| CHEMBL5760003 | — | k_off | = | - | s-1 | - |
| CHEMBL5760003 | — | kon | = | - | — | - |
| CHEMBL5760003 | — | k_off | = | - | s-1 | - |
| CHEMBL6062186 | — | kon | = | - | — | - |
| CHEMBL6062186 | — | k_off | = | - | s-1 | - |
| CHEMBL5945056 | — | k_off | = | - | s-1 | - |
| CHEMBL6057973 | — | kon | = | - | — | - |
| CHEMBL6005179 | — | kon | = | - | — | - |
| CHEMBL5760003 | — | kon | = | - | — | - |
| CHEMBL5908735 | — | k_off | = | - | s-1 | - |
| CHEMBL5908735 | — | kon | = | - | — | - |
| CHEMBL5866418 | — | k_off | = | - | s-1 | - |
| CHEMBL5866418 | — | kon | = | - | — | - |
| CHEMBL5773878 | — | k_off | = | - | s-1 | - |
| CHEMBL5773878 | — | kon | = | - | — | - |
| CHEMBL5945056 | — | kon | = | - | — | - |
| CHEMBL5977186 | — | kon | = | - | — | - |
| CHEMBL6042932 | — | k_off | = | - | s-1 | - |
| CHEMBL5977186 | — | k_off | = | - | s-1 | - |
| CHEMBL5762359 | — | kon | = | - | — | - |
| CHEMBL6042932 | — | kon | = | - | — | - |
| CHEMBL5762359 | — | k_off | = | - | s-1 | - |