Assay Detail
Binding
CHEMBL4406029
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Displacement of [125I]I-AB-MECA from recombinant mouse A3AR expressed in HEK293 cell membranes measured after 60 mins by liquid scintillation counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A3 Adenosine Receptors: Affinity Enhancement by N6-(2-Phenylethyl) Substitution.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.78 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4571380 | — | — | 1 | 7.75 |
| CHEMBL4465891 | — | — | 1 | 7.67 |
| CHEMBL4483546 | — | — | 1 | 7.58 |
| CHEMBL4556534 | — | — | 1 | 7.40 |
| CHEMBL4442223 | — | — | 1 | 7.26 |
| CHEMBL4561796 | — | — | 1 | 7.22 |
| CHEMBL4456051 | — | — | 1 | 7.21 |
| CHEMBL4573502 | — | — | 1 | 7.14 |
| CHEMBL4476812 | — | — | 1 | 7.13 |
| CHEMBL4459700 | — | — | 1 | 7.12 |
| CHEMBL4459684 | — | — | 1 | 7.12 |
| CHEMBL4455589 | — | — | 1 | 7.03 |
| CHEMBL4591186 | — | — | 1 | 6.91 |
| CHEMBL4438591 | — | — | 1 | 6.81 |
| CHEMBL4562690 | — | — | 1 | 6.58 |
| CHEMBL4453175 | — | — | 1 | 6.48 |
| CHEMBL4437771 | — | — | 1 | 6.39 |
| CHEMBL2089346 | — | — | 1 | 6.32 |
| CHEMBL4519265 | — | — | 1 | 6.31 |
| CHEMBL4537118 | — | — | 1 | 6.28 |
| CHEMBL4550711 | — | — | 1 | 6.17 |
| CHEMBL2089347 | — | — | 1 | 6.01 |
| CHEMBL4475372 | — | — | 1 | 6.00 |
| CHEMBL4448826 | — | — | 1 | 5.94 |
| CHEMBL4521342 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4571380 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL4465891 | — | Ki | = | 21.5 | nM | 7.67 |
| CHEMBL4483546 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4556534 | — | Ki | = | 39.8 | nM | 7.40 |
| CHEMBL4442223 | — | Ki | = | 54.4 | nM | 7.26 |
| CHEMBL4561796 | — | Ki | = | 60.4 | nM | 7.22 |
| CHEMBL4456051 | — | Ki | = | 61.6 | nM | 7.21 |
| CHEMBL4573502 | — | Ki | = | 72.2 | nM | 7.14 |
| CHEMBL4476812 | — | Ki | = | 74.7 | nM | 7.13 |
| CHEMBL4459700 | — | Ki | = | 76.4 | nM | 7.12 |
| CHEMBL4459684 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL4455589 | — | Ki | = | 92.5 | nM | 7.03 |
| CHEMBL4591186 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL4438591 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL4562690 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL4453175 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL4437771 | — | Ki | = | 404.0 | nM | 6.39 |
| CHEMBL2089346 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL4519265 | — | Ki | = | 488.0 | nM | 6.31 |
| CHEMBL4537118 | — | Ki | = | 531.0 | nM | 6.28 |
| CHEMBL4550711 | — | Ki | = | 675.0 | nM | 6.17 |
| CHEMBL2089347 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL4475372 | — | Ki | = | 995.0 | nM | 6.00 |
| CHEMBL4448826 | — | Ki | = | 1140.0 | nM | 5.94 |
| CHEMBL4521342 | — | Ki | = | 2520.0 | nM | 5.60 |