Assay Detail
Binding
CHEMBL5129723
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Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Expi293F |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 26 | 5.15 | 9.54 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | — | 1 | 9.54 |
| CHEMBL1256672 | — | — | 1 | 8.04 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 7.76 |
| CHEMBL160333 | — | — | 1 | 6.96 |
| CHEMBL408564 | — | — | 1 | 6.25 |
| CHEMBL3954022 | — | — | 1 | 5.96 |
| CHEMBL337319 | BENZOGUANAMINE | — | 1 | 5.82 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.44 |
| CHEMBL113 | CAFFEINE | 4.0 | 1 | 5.26 |
| CHEMBL485745 | GW434756X | — | 1 | 5.05 |
| CHEMBL336555 | — | — | 1 | 5.02 |
| CHEMBL5208068 | — | — | 1 | 4.87 |
| CHEMBL5184937 | — | — | 1 | 4.66 |
| CHEMBL5204663 | — | — | 1 | 4.54 |
| CHEMBL5197657 | — | — | 1 | 4.50 |
| CHEMBL4550896 | — | — | 1 | 4.40 |
| CHEMBL5193059 | — | — | 1 | 4.31 |
| CHEMBL5201800 | — | — | 1 | 4.30 |
| CHEMBL143703 | — | — | 1 | 4.29 |
| CHEMBL1467 | ALLOPURINOL | 4.0 | 1 | 4.11 |
| CHEMBL5195119 | — | — | 1 | 4.00 |
| CHEMBL47633 | — | — | 1 | 3.89 |
| CHEMBL1573515 | — | — | 1 | 3.88 |
| CHEMBL5193006 | — | — | 1 | 3.86 |
| CHEMBL5197070 | — | — | 1 | 3.68 |
| CHEMBL1417210 | — | — | 1 | 3.39 |
| CHEMBL63803 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113142 | ZM-241385 | Kd | = | 0.286 | nM | 9.54 |
| CHEMBL1256672 | — | Kd | = | 9.1 | nM | 8.04 |
| CHEMBL477 | ADENOSINE | Kd | = | 17.3 | nM | 7.76 |
| CHEMBL160333 | — | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL408564 | — | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL3954022 | — | Kd | = | 1110.0 | nM | 5.96 |
| CHEMBL337319 | BENZOGUANAMINE | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL1355736 | THEOPHYLLINE | Kd | = | 3630.0 | nM | 5.44 |
| CHEMBL113 | CAFFEINE | Kd | = | 5510.0 | nM | 5.26 |
| CHEMBL485745 | GW434756X | Kd | = | 8900.0 | nM | 5.05 |
| CHEMBL336555 | — | Kd | = | 9600.0 | nM | 5.02 |
| CHEMBL5208068 | — | Kd | = | 13500.0 | nM | 4.87 |
| CHEMBL5184937 | — | Kd | = | 21800.0 | nM | 4.66 |
| CHEMBL5204663 | — | Kd | = | 28800.0 | nM | 4.54 |
| CHEMBL5197657 | — | Kd | = | 31800.0 | nM | 4.50 |
| CHEMBL4550896 | — | Kd | = | 40000.0 | nM | 4.40 |
| CHEMBL5193059 | — | Kd | = | 49000.0 | nM | 4.31 |
| CHEMBL5201800 | — | Kd | = | 50000.0 | nM | 4.30 |
| CHEMBL143703 | — | Kd | = | 50900.0 | nM | 4.29 |
| CHEMBL1467 | ALLOPURINOL | Kd | = | 77000.0 | nM | 4.11 |
| CHEMBL5195119 | — | Kd | = | 100000.0 | nM | 4.00 |
| CHEMBL47633 | — | Kd | = | 130000.0 | nM | 3.89 |
| CHEMBL1573515 | — | Kd | = | 131000.0 | nM | 3.88 |
| CHEMBL5193006 | — | Kd | = | 139000.0 | nM | 3.86 |
| CHEMBL5197070 | — | Kd | = | 210000.0 | nM | 3.68 |
| CHEMBL1417210 | — | Kd | = | 410000.0 | nM | 3.39 |
| CHEMBL63803 | — | Activity | - | — | - |