Assay Detail
Binding
CHEMBL5316663
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CD73 in human plasma incubated for 15 mins in presence of 15N5-AMP by LC/MS analysis
22
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Series of Potent, Selective, and Orally Bioavailable Nucleoside Inhibitors of CD73 That Demonstrates <i>In Vivo</i> Antitumor Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.99 | 9.59 |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439071 | — | — | 1 | 9.59 |
| CHEMBL5423436 | — | — | 2 | 9.42 |
| CHEMBL5404625 | — | — | 1 | 9.42 |
| CHEMBL5403339 | — | — | 1 | 8.82 |
| CHEMBL5398515 | — | — | 1 | 8.80 |
| CHEMBL5398484 | — | — | 1 | 8.55 |
| CHEMBL5415675 | — | — | 1 | 8.27 |
| CHEMBL5393743 | — | — | 1 | 8.25 |
| CHEMBL5435185 | — | — | 1 | 8.19 |
| CHEMBL5404674 | — | — | 1 | 8.14 |
| CHEMBL5417110 | — | — | 1 | 7.94 |
| CHEMBL5415259 | — | — | 1 | 7.81 |
| CHEMBL5421027 | — | — | 1 | 7.81 |
| CHEMBL5404795 | — | — | 1 | 7.80 |
| CHEMBL5416552 | — | — | 1 | 7.39 |
| CHEMBL5423764 | — | — | 1 | 7.30 |
| CHEMBL5398262 | — | — | 1 | 6.87 |
| CHEMBL5428426 | — | — | 1 | 6.80 |
| CHEMBL5409033 | — | — | 1 | 6.68 |
| CHEMBL5410317 | — | — | 1 | 6.04 |
| CHEMBL5419527 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439071 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5423436 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL5404625 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL5403339 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5398515 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5398484 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5415675 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5393743 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5435185 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5404674 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5417110 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL5415259 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL5421027 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5404795 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5416552 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5423764 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5398262 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL5428426 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5409033 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL5410317 | — | IC50 | = | 917.0 | nM | 6.04 |
| CHEMBL5419527 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5423436 | — | IC90 | = | 3.0 | nM | - |