Assay Detail
Binding
CHEMBL645776
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Binding affinity at human Adenosine A3 receptor expressed in HEK 293 cells by [125I]-AB MECA displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.94 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL610150 | — | — | 1 | 8.14 |
| CHEMBL464859 | NECA | — | 1 | 7.96 |
| CHEMBL2113595 | — | — | 1 | 7.84 |
| CHEMBL319387 | — | — | 1 | 7.77 |
| CHEMBL2113605 | — | — | 1 | 7.49 |
| CHEMBL2113592 | — | — | 1 | 7.42 |
| CHEMBL2113601 | — | — | 1 | 7.12 |
| CHEMBL2113604 | — | — | 1 | 7.05 |
| CHEMBL2113588 | — | — | 1 | 6.60 |
| CHEMBL2113602 | — | — | 1 | 6.59 |
| CHEMBL2113519 | — | — | 1 | 6.53 |
| CHEMBL2113600 | — | — | 1 | 6.40 |
| CHEMBL2113606 | — | — | 1 | 6.39 |
| CHEMBL2113582 | — | — | 1 | 6.26 |
| CHEMBL2113593 | — | — | 1 | 6.25 |
| CHEMBL2113581 | — | — | 1 | 6.16 |
| CHEMBL2113580 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL610150 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL464859 | NECA | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2113595 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL319387 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL2113605 | — | Ki | = | 32.3 | nM | 7.49 |
| CHEMBL2113592 | — | Ki | = | 38.3 | nM | 7.42 |
| CHEMBL2113601 | — | Ki | = | 75.4 | nM | 7.12 |
| CHEMBL2113604 | — | Ki | = | 88.3 | nM | 7.05 |
| CHEMBL2113588 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL2113602 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL2113519 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL2113600 | — | Ki | = | 395.0 | nM | 6.40 |
| CHEMBL2113606 | — | Ki | = | 409.0 | nM | 6.39 |
| CHEMBL2113582 | — | Ki | = | 546.0 | nM | 6.26 |
| CHEMBL2113593 | — | Ki | = | 558.0 | nM | 6.25 |
| CHEMBL2113581 | — | Ki | = | 697.0 | nM | 6.16 |
| CHEMBL2113580 | — | Ki | = | 814.0 | nM | 6.09 |