Assay Detail
Binding
CHEMBL641340
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Inhibition of [3H]MSX-2 binding to rat adenosine A2A receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 6.10 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36963 | — | — | 1 | 7.85 |
| CHEMBL40055 | — | — | 1 | 7.41 |
| CHEMBL416963 | — | — | 1 | 6.89 |
| CHEMBL286527 | — | — | 1 | 6.70 |
| CHEMBL37875 | — | — | 1 | 6.54 |
| CHEMBL37726 | — | — | 1 | 6.50 |
| CHEMBL35701 | — | — | 1 | 6.47 |
| CHEMBL288459 | — | — | 1 | 6.44 |
| CHEMBL37050 | — | — | 1 | 6.35 |
| CHEMBL274855 | — | — | 1 | 6.34 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.33 |
| CHEMBL38193 | — | — | 1 | 6.32 |
| CHEMBL38304 | — | — | 1 | 6.26 |
| CHEMBL37243 | — | — | 1 | 6.24 |
| CHEMBL8789 | — | — | 1 | 6.19 |
| CHEMBL284288 | — | — | 1 | 6.15 |
| CHEMBL16997 | — | — | 1 | 6.10 |
| CHEMBL37933 | — | — | 1 | 6.05 |
| CHEMBL35415 | — | — | 1 | 5.92 |
| CHEMBL435575 | — | — | 1 | 5.85 |
| CHEMBL287129 | — | — | 1 | 5.75 |
| CHEMBL37082 | — | — | 1 | 5.73 |
| CHEMBL284991 | — | — | 1 | 5.70 |
| CHEMBL416417 | — | — | 1 | 5.67 |
| CHEMBL35094 | — | — | 1 | 5.42 |
| CHEMBL2113345 | — | — | 1 | 5.23 |
| CHEMBL36952 | — | — | 1 | 5.09 |
| CHEMBL285191 | — | — | 1 | 4.68 |
| CHEMBL34862 | — | — | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36963 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL40055 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL416963 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL286527 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL37875 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL37726 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL35701 | — | Ki | = | 336.0 | nM | 6.47 |
| CHEMBL288459 | — | Ki | = | 365.0 | nM | 6.44 |
| CHEMBL37050 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL274855 | — | Ki | = | 458.0 | nM | 6.34 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL38193 | — | Ki | = | 479.0 | nM | 6.32 |
| CHEMBL38304 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL37243 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL8789 | — | Ki | = | 642.0 | nM | 6.19 |
| CHEMBL284288 | — | Ki | = | 709.0 | nM | 6.15 |
| CHEMBL16997 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL37933 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL35415 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL435575 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL287129 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL37082 | — | Ki | = | 1877.0 | nM | 5.73 |
| CHEMBL284991 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL416417 | — | Ki | = | 2139.0 | nM | 5.67 |
| CHEMBL35094 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL2113345 | — | Ki | = | 5905.0 | nM | 5.23 |
| CHEMBL36952 | — | Ki | = | 8070.0 | nM | 5.09 |
| CHEMBL285191 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL34862 | — | Ki | = | 24000.0 | nM | 4.62 |