Assay Detail
Binding
CHEMBL4404524
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Inhibition of native CD73 in human MDA-MB-231 cell membrane preparations [3H]AMP as substrate incubated for 25 mins by scintillation counting method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2-Substituted α,β-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.40 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4585872 | — | — | 1 | 8.48 |
| CHEMBL4475460 | — | — | 1 | 8.34 |
| CHEMBL4591580 | — | — | 1 | 7.81 |
| CHEMBL4456465 | — | — | 1 | 7.49 |
| CHEMBL4462911 | — | — | 1 | 7.45 |
| CHEMBL4536899 | — | — | 1 | 7.31 |
| CHEMBL4472826 | — | — | 1 | 7.18 |
| CHEMBL583969 | PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | — | 1 | 6.68 |
| CHEMBL4569080 | — | — | 1 | 6.62 |
| CHEMBL1164951 | PHOSPHOMETHYLPHOSPHONIC ACID GUANOSYL ESTER | — | 1 | 6.59 |
| CHEMBL4445938 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4585872 | — | Ki | = | 3.33 | nM | 8.48 |
| CHEMBL4475460 | — | Ki | = | 4.57 | nM | 8.34 |
| CHEMBL4591580 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL4456465 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL4462911 | — | Ki | = | 35.7 | nM | 7.45 |
| CHEMBL4536899 | — | Ki | = | 49.1 | nM | 7.31 |
| CHEMBL4472826 | — | Ki | = | 65.4 | nM | 7.18 |
| CHEMBL583969 | PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL4569080 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL1164951 | PHOSPHOMETHYLPHOSPHONIC ACID GUANOSYL ESTER | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL4445938 | — | Ki | - | — | - |