Assay Detail
Binding
CHEMBL2187068
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Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter
44
Total Activities
43
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 8.41 | 11.00 |
| IC50 | 1 | 8.09 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL332091 | — | — | 1 | 11.00 |
| CHEMBL2181965 | — | — | 1 | 9.70 |
| CHEMBL175543 | — | — | 1 | 9.54 |
| CHEMBL2181976 | — | — | 1 | 9.44 |
| CHEMBL589080 | — | — | 1 | 9.39 |
| CHEMBL88147 | — | — | 1 | 9.23 |
| CHEMBL434534 | — | — | 1 | 9.10 |
| CHEMBL2181975 | — | — | 1 | 9.10 |
| CHEMBL211862 | — | — | 1 | 9.10 |
| CHEMBL193421 | — | — | 1 | 9.07 |
| CHEMBL2181971 | — | — | 1 | 9.04 |
| CHEMBL123705 | — | — | 1 | 9.02 |
| CHEMBL2181970 | — | — | 1 | 8.72 |
| CHEMBL398587 | — | — | 1 | 8.70 |
| CHEMBL99178 | — | — | 1 | 8.68 |
| CHEMBL2181964 | — | — | 1 | 8.66 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 8.66 |
| CHEMBL1625681 | — | — | 1 | 8.64 |
| CHEMBL265096 | — | — | 1 | 8.57 |
| CHEMBL2181972 | — | — | 1 | 8.47 |
| CHEMBL371404 | — | — | 1 | 8.46 |
| CHEMBL193692 | — | — | 1 | 8.41 |
| CHEMBL322250 | — | — | 1 | 8.40 |
| CHEMBL305975 | — | — | 1 | 8.40 |
| CHEMBL119709 | IB-MECA | — | 1 | 8.39 |
| CHEMBL2177153 | — | — | 1 | 8.37 |
| CHEMBL333799 | — | — | 1 | 8.33 |
| CHEMBL2181977 | — | — | 1 | 8.22 |
| CHEMBL108705 | — | — | 1 | 8.10 |
| CHEMBL2181973 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL332091 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL2181965 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL175543 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL2181976 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL589080 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL88147 | — | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL2181975 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL211862 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL434534 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL193421 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL2181971 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL123705 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL2181970 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL398587 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL99178 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2181964 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1625681 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL265096 | — | Ki | = | 2.69 | nM | 8.57 |
| CHEMBL2181972 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL371404 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL193692 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL322250 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL305975 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL119709 | IB-MECA | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL2177153 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL333799 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL2181977 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL108705 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL2181973 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL339066 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL188035 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL186113 | GW-328267 | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL128929 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL122396 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL198779 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2181969 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2181968 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL113420 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL363419 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2181967 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL89093 | — | Ki | = | 561.0 | nM | 6.25 |
| CHEMBL2181966 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL186113 | GW-328267 | Ki | >= | 1000.0 | nM | - |