Assay Detail
Binding
CHEMBL4729979
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CD73 in human NCI-H1568 cells assessed as reduction in AMP-induced ADO expression preincubated for 15 mins followed by AMP addition and measured after 1 hr by LC-MS/MS analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H1568 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.79 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4764985 | — | — | 1 | 9.10 |
| CHEMBL4471306 | QUEMLICLUSTAT | 2.0 | 1 | 8.48 |
| CHEMBL4786598 | — | — | 1 | 8.43 |
| CHEMBL4752114 | — | — | 1 | 8.16 |
| CHEMBL583969 | PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | — | 1 | 4.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4764985 | — | EC50 | = | 0.79 | nM | 9.10 |
| CHEMBL4471306 | QUEMLICLUSTAT | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4786598 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4752114 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL583969 | PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | EC50 | = | 16268.0 | nM | 4.79 |