Assay Detail
Binding
CHEMBL5732087
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Inhibition activities of all the N-substituted pyrazolo [3,4-d] pyrimidine ketone compounds according to the present invention to the phosphodiesterase IX are tested.
291
Total Activities
96
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A (CHEMBL3535) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-substituted pyrazolo [3,4-D] pyrimidine ketone compound, and preparation process and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 97 | 7.30 | 9.22 |
| kon | 97 | - | - |
| k_off | 97 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5913347 | — | — | 3 | 9.22 |
| CHEMBL6030210 | — | — | 6 | 9.00 |
| CHEMBL5845348 | — | — | 3 | 8.52 |
| CHEMBL5772616 | — | — | 3 | 8.40 |
| CHEMBL3360414 | — | — | 3 | 8.22 |
| CHEMBL2178115 | — | — | 3 | 8.22 |
| CHEMBL4642517 | — | — | 3 | 8.22 |
| CHEMBL5905560 | — | — | 3 | 8.22 |
| CHEMBL5935604 | — | — | 3 | 8.10 |
| CHEMBL5743746 | — | — | 3 | 7.92 |
| CHEMBL6010702 | — | — | 3 | 7.85 |
| CHEMBL5752355 | — | — | 3 | 7.85 |
| CHEMBL5807865 | — | — | 3 | 7.82 |
| CHEMBL5773329 | — | — | 3 | 7.82 |
| CHEMBL5782166 | — | — | 3 | 7.77 |
| CHEMBL5835850 | — | — | 3 | 7.77 |
| CHEMBL5892732 | — | — | 3 | 7.75 |
| CHEMBL5951992 | — | — | 3 | 7.75 |
| CHEMBL5739598 | — | — | 3 | 7.72 |
| CHEMBL6050087 | — | — | 3 | 7.72 |
| CHEMBL5795614 | — | — | 3 | 7.72 |
| CHEMBL6037063 | — | — | 3 | 7.70 |
| CHEMBL6011618 | — | — | 3 | 7.70 |
| CHEMBL5907734 | — | — | 3 | 7.70 |
| CHEMBL5900239 | — | — | 3 | 7.68 |
| CHEMBL5905409 | — | — | 3 | 7.64 |
| CHEMBL5917179 | — | — | 3 | 7.64 |
| CHEMBL6041092 | — | — | 3 | 7.60 |
| CHEMBL5858733 | — | — | 3 | 7.60 |
| CHEMBL5828438 | — | — | 3 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5913347 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL6030210 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5845348 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5772616 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4642517 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2178115 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5905560 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3360414 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5935604 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5743746 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5752355 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL6010702 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5807865 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5773329 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5835850 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5782166 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5951992 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5892732 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5739598 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL6050087 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5795614 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL6037063 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5907734 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL6011618 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5900239 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5917179 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5905409 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL6041092 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5828438 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5858733 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5991832 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3360418 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5942047 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL6005532 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5937721 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5990600 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL6028498 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5887999 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5744663 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5759834 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5760244 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5805751 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5970889 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5938188 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5867132 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5852017 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5870653 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL6005436 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5848017 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL6057068 | — | IC50 | = | 44.0 | nM | 7.36 |