Assay Detail
Binding
CHEMBL829680
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Inhibition of [125I]-AB-MECA binding to human Adenosine A3 receptor expressed in CHO cells
39
Total Activities
39
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 | 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 | 39 | 8.57 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL175543 | — | — | 1 | 9.54 |
| CHEMBL2368455 | — | — | 1 | 9.42 |
| CHEMBL2112156 | — | — | 1 | 9.25 |
| CHEMBL2368364 | — | — | 1 | 9.24 |
| CHEMBL2112160 | — | — | 1 | 9.20 |
| CHEMBL2368366 | — | — | 1 | 9.16 |
| CHEMBL2112163 | — | — | 1 | 9.11 |
| CHEMBL2368363 | — | — | 1 | 9.08 |
| CHEMBL193421 | — | — | 1 | 9.07 |
| CHEMBL191809 | — | — | 1 | 8.89 |
| CHEMBL2112157 | — | — | 1 | 8.85 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 8.85 |
| CHEMBL27376 | — | — | 1 | 8.82 |
| CHEMBL353319 | — | — | 1 | 8.82 |
| CHEMBL2112161 | — | — | 1 | 8.82 |
| CHEMBL2112175 | — | — | 1 | 8.80 |
| CHEMBL119709 | IB-MECA | — | 1 | 8.74 |
| CHEMBL307199 | — | — | 1 | 8.74 |
| CHEMBL27809 | — | — | 1 | 8.72 |
| CHEMBL283057 | — | — | 1 | 8.66 |
| CHEMBL280580 | — | — | 1 | 8.62 |
| CHEMBL2112155 | — | — | 1 | 8.62 |
| CHEMBL2112162 | — | — | 1 | 8.54 |
| CHEMBL2368365 | — | — | 1 | 8.51 |
| CHEMBL2368367 | — | — | 1 | 8.44 |
| CHEMBL2112158 | — | — | 1 | 8.43 |
| CHEMBL193692 | — | — | 1 | 8.41 |
| CHEMBL193385 | — | — | 1 | 8.36 |
| CHEMBL364671 | — | — | 1 | 8.35 |
| CHEMBL2368368 | — | — | 1 | 8.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL175543 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL2368455 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL2112156 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL2368364 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL2112160 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL2368366 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL2112163 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL2368363 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL193421 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL191809 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2112157 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL27376 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL353319 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2112161 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2112175 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL119709 | IB-MECA | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL307199 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL27809 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL283057 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2112155 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL280580 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL2112162 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2368365 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL2368367 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL2112158 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL193692 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL193385 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL364671 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2368368 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2368369 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL66393 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL417292 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL383144 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL2112159 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2112164 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL194830 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2368370 | — | Ki | = | 217.0 | nM | 6.66 |