Assay Detail
Binding
CHEMBL829121
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Inhibition of [125I]AB-MECA binding to rat Adenosine A3 receptor expressed in CHO cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.96 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 9.48 |
| CHEMBL2368455 | — | — | 1 | 9.12 |
| CHEMBL2112157 | — | — | 1 | 9.06 |
| CHEMBL175543 | — | — | 1 | 9.00 |
| CHEMBL27376 | — | — | 1 | 8.96 |
| CHEMBL119709 | IB-MECA | — | 1 | 8.96 |
| CHEMBL2112155 | — | — | 1 | 8.80 |
| CHEMBL2112162 | — | — | 1 | 8.80 |
| CHEMBL307199 | — | — | 1 | 8.57 |
| CHEMBL2368367 | — | — | 1 | 8.41 |
| CHEMBL66393 | — | — | 1 | 8.02 |
| CHEMBL2368366 | — | — | 1 | 8.00 |
| CHEMBL2368369 | — | — | 1 | 7.96 |
| CHEMBL193385 | — | — | 1 | 7.46 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 7.42 |
| CHEMBL283057 | — | — | 1 | 6.80 |
| CHEMBL364671 | — | — | 1 | 6.54 |
| CHEMBL193421 | — | — | 1 | 6.40 |
| CHEMBL193692 | — | — | 1 | 6.27 |
| CHEMBL383144 | — | — | 1 | 5.19 |
| CHEMBL194830 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL2368455 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL2112157 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL175543 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL27376 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL119709 | IB-MECA | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2112155 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2112162 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL307199 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL2368367 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL66393 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL2368366 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2368369 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL193385 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL283057 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL364671 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL193421 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL193692 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL383144 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL194830 | — | Ki | > | 10000.0 | nM | - |