Assay Detail
Binding
CHEMBL4729978
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Inhibition of human C-terminal His6-tagged CD73 expressed in CHO cells preincubated for 15 mins followed by AMP addition and measured after 10 mins by malachite green reagent based assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| IC50 | 38 | 7.70 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4764985 | — | — | 1 | 9.60 |
| CHEMBL4752114 | — | — | 1 | 9.29 |
| CHEMBL4757563 | — | — | 1 | 9.28 |
| CHEMBL4743237 | — | — | 1 | 9.28 |
| CHEMBL4786598 | — | — | 1 | 9.24 |
| CHEMBL4471306 | QUEMLICLUSTAT | 2.0 | 1 | 9.07 |
| CHEMBL4751244 | — | — | 1 | 9.02 |
| CHEMBL4788790 | — | — | 1 | 9.00 |
| CHEMBL4784951 | — | — | 1 | 8.89 |
| CHEMBL4782655 | — | — | 1 | 8.89 |
| CHEMBL4753449 | — | — | 1 | 8.62 |
| CHEMBL4452072 | — | — | 1 | 8.52 |
| CHEMBL4798368 | — | — | 1 | 8.41 |
| CHEMBL4788607 | — | — | 1 | 8.00 |
| CHEMBL4745473 | — | — | 1 | 7.96 |
| CHEMBL4796959 | — | — | 1 | 7.93 |
| CHEMBL4760944 | — | — | 1 | 7.89 |
| CHEMBL4741942 | — | — | 1 | 7.75 |
| CHEMBL4754460 | — | — | 1 | 7.64 |
| CHEMBL4790529 | — | — | 1 | 7.61 |
| CHEMBL4749770 | — | — | 1 | 7.55 |
| CHEMBL4785716 | — | — | 1 | 7.54 |
| CHEMBL4791561 | — | — | 1 | 7.51 |
| CHEMBL4743063 | — | — | 1 | 7.06 |
| CHEMBL4756805 | — | — | 1 | 7.01 |
| CHEMBL4781819 | — | — | 1 | 6.97 |
| CHEMBL4785684 | — | — | 1 | 6.88 |
| CHEMBL4782125 | — | — | 1 | 6.79 |
| CHEMBL4789486 | — | — | 1 | 6.71 |
| CHEMBL4749007 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4764985 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4752114 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL4743237 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL4757563 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL4786598 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4471306 | QUEMLICLUSTAT | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL4751244 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL4788790 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4784951 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4782655 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4753449 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4452072 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4798368 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4788607 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4745473 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4796959 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4760944 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4741942 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4754460 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4790529 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL4749770 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4785716 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4791561 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4743063 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4756805 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4781819 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4785684 | — | IC50 | = | 130.7 | nM | 6.88 |
| CHEMBL4782125 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4789486 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4749007 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4784125 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4744820 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL4797508 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4759919 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL4790457 | — | IC50 | = | 1201.0 | nM | 5.92 |
| CHEMBL583969 | PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | IC50 | = | 2653.0 | nM | 5.58 |
| CHEMBL4785168 | — | IC50 | = | 2874.0 | nM | 5.54 |
| CHEMBL4781912 | — | IC50 | > | 5000.0 | nM | - |