Assay Detail
Binding
CHEMBL641335
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Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | COS-7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.68 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL133591 | — | — | 1 | 9.27 |
| CHEMBL132629 | — | — | 1 | 9.06 |
| CHEMBL133566 | — | — | 1 | 8.92 |
| CHEMBL133387 | — | — | 1 | 8.80 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 8.37 |
| CHEMBL439976 | — | — | 1 | 8.34 |
| CHEMBL129903 | — | — | 1 | 7.71 |
| CHEMBL128929 | — | — | 1 | 7.21 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 6.96 |
| CHEMBL340998 | — | — | 1 | 6.89 |
| CHEMBL464859 | NECA | — | 1 | 6.77 |
| CHEMBL16687 | CGS-15943 | — | 1 | 6.60 |
| CHEMBL338352 | — | — | 1 | 6.36 |
| CHEMBL285819 | — | — | 1 | 6.19 |
| CHEMBL133809 | — | — | 1 | - |
| CHEMBL302376 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL133591 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL132629 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL133566 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL133387 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL439976 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL129903 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL128929 | — | Ki | = | 61.7 | nM | 7.21 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL340998 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL464859 | NECA | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL16687 | CGS-15943 | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL338352 | — | Ki | = | 442.0 | nM | 6.36 |
| CHEMBL285819 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL133809 | — | Ki | = | 1000000.0 | nM | - |
| CHEMBL302376 | — | Ki | = | 1000000.0 | nM | - |