Assay Detail
Binding
CHEMBL829615
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Inhibition of [3H]R-PIA binding to human Adenosine A1 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 | 6.57 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66393 | — | — | 1 | 8.13 |
| CHEMBL191809 | — | — | 1 | 8.04 |
| CHEMBL307199 | — | — | 1 | 7.77 |
| CHEMBL193385 | — | — | 1 | 7.70 |
| CHEMBL417292 | — | — | 1 | 7.46 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 7.41 |
| CHEMBL364671 | — | — | 1 | 7.38 |
| CHEMBL2368365 | — | — | 1 | 7.32 |
| CHEMBL193692 | — | — | 1 | 7.30 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.29 |
| CHEMBL27809 | — | — | 1 | 7.19 |
| CHEMBL2368368 | — | — | 1 | 7.09 |
| CHEMBL193421 | — | — | 1 | 6.92 |
| CHEMBL27376 | — | — | 1 | 6.87 |
| CHEMBL2368364 | — | — | 1 | 6.70 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.66 |
| CHEMBL353319 | — | — | 1 | 6.62 |
| CHEMBL175543 | — | — | 1 | 6.58 |
| CHEMBL2368455 | — | — | 1 | 6.57 |
| CHEMBL2368363 | — | — | 1 | 6.47 |
| CHEMBL2112160 | — | — | 1 | 6.35 |
| CHEMBL194830 | — | — | 1 | 6.32 |
| CHEMBL2112156 | — | — | 1 | 6.27 |
| CHEMBL2112161 | — | — | 1 | 6.21 |
| CHEMBL2112155 | — | — | 1 | 6.19 |
| CHEMBL280580 | — | — | 1 | 6.16 |
| CHEMBL2112158 | — | — | 1 | 6.15 |
| CHEMBL2112163 | — | — | 1 | 6.11 |
| CHEMBL2368369 | — | — | 1 | 5.92 |
| CHEMBL2368366 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66393 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL191809 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL307199 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL193385 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL417292 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL364671 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2368365 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL193692 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL119709 | IB-MECA | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL27809 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL2368368 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL193421 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL27376 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL2368364 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL353319 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL175543 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL2368455 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL2368363 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL2112160 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL194830 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL2112156 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL2112161 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL2112155 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL280580 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL2112158 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL2112163 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL2368369 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2368366 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL2112175 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL2112157 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL283057 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL2368367 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL2112162 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL2112159 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL2112164 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL383144 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL2368370 | — | Ki | = | 14.0 | % | - |