Assay Detail
Binding
CHEMBL5628130
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-CGS21680 from human A3AR expressed in HEK cells assessed as inhibition constant
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure activity relationships of 5-HT<sub>2B</sub> and 5-HT<sub>2C</sub> serotonin receptor antagonists: N<sup>6</sup>, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 5.44 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5633183 | — | — | 1 | 7.14 |
| CHEMBL5633824 | — | — | 1 | 7.03 |
| CHEMBL5632085 | — | — | 1 | 6.41 |
| CHEMBL5632406 | — | — | 1 | 6.03 |
| CHEMBL5631554 | — | — | 1 | 5.43 |
| CHEMBL2170801 | — | — | 1 | 5.36 |
| CHEMBL5633642 | — | — | 1 | 5.30 |
| CHEMBL5633293 | — | — | 1 | 5.28 |
| CHEMBL5632374 | — | — | 1 | 5.20 |
| CHEMBL5632033 | — | — | 1 | 5.18 |
| CHEMBL5633551 | — | — | 1 | 5.14 |
| CHEMBL5633886 | — | — | 1 | 5.11 |
| CHEMBL5632857 | — | — | 1 | 5.08 |
| CHEMBL5633744 | — | — | 1 | 5.03 |
| CHEMBL5633589 | — | — | 1 | 5.01 |
| CHEMBL4743059 | — | — | 1 | 4.93 |
| CHEMBL5632946 | — | — | 1 | 4.78 |
| CHEMBL5631700 | — | — | 1 | 4.46 |
| CHEMBL5631697 | — | — | 1 | - |
| CHEMBL5633118 | — | — | 1 | - |
| CHEMBL5633044 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5633183 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL5633824 | — | Ki | = | 92.5 | nM | 7.03 |
| CHEMBL5632085 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL5632406 | — | Ki | = | 932.0 | nM | 6.03 |
| CHEMBL5631554 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL2170801 | — | Ki | = | 4380.0 | nM | 5.36 |
| CHEMBL5633642 | — | Ki | = | 5040.0 | nM | 5.30 |
| CHEMBL5633293 | — | Ki | = | 5270.0 | nM | 5.28 |
| CHEMBL5632374 | — | Ki | = | 6280.0 | nM | 5.20 |
| CHEMBL5632033 | — | Ki | = | 6620.0 | nM | 5.18 |
| CHEMBL5633551 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL5633886 | — | Ki | = | 7810.0 | nM | 5.11 |
| CHEMBL5632857 | — | Ki | = | 8260.0 | nM | 5.08 |
| CHEMBL5633744 | — | Ki | = | 9320.0 | nM | 5.03 |
| CHEMBL5633589 | — | Ki | = | 9720.0 | nM | 5.01 |
| CHEMBL4743059 | — | Ki | = | 11700.0 | nM | 4.93 |
| CHEMBL5632946 | — | Ki | = | 16600.0 | nM | 4.78 |
| CHEMBL5631700 | — | Ki | = | 34300.0 | nM | 4.46 |
| CHEMBL5631697 | — | Ki | - | — | - | |
| CHEMBL5633118 | — | Ki | - | — | - | |
| CHEMBL5633044 | — | Ki | - | — | - |