Assay Detail
Binding
CHEMBL1259386
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed in rat C6 cells after 120 mins by liquid scintillation counting
23
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | C6 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rigid analogues of the α2-adrenergic blocker atipamezole: small changes, big consequences.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.71 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1256414 | — | — | 3 | 9.96 |
| CHEMBL1255723 | — | — | 1 | 9.74 |
| CHEMBL1256378 | — | — | 1 | 9.69 |
| CHEMBL1255724 | — | — | 1 | 9.46 |
| CHEMBL1256609 | — | — | 1 | 9.16 |
| CHEMBL1255771 | — | — | 1 | 9.04 |
| CHEMBL1255770 | — | — | 1 | 8.94 |
| CHEMBL1256610 | — | — | 1 | 8.79 |
| CHEMBL1255617 | — | — | 3 | 8.72 |
| CHEMBL353972 | ATIPAMEZOLE | 2.0 | 1 | 8.65 |
| CHEMBL1255616 | — | — | 1 | 8.64 |
| CHEMBL1256503 | — | — | 3 | 8.55 |
| CHEMBL1256566 | — | — | 1 | 8.19 |
| CHEMBL1255582 | FIPAMEZOLE | 2.0 | 1 | 8.17 |
| CHEMBL1256565 | — | — | 1 | 8.01 |
| CHEMBL1256608 | — | — | 1 | 7.93 |
| CHEMBL1256502 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1256414 | — | Ki | = | 0.1096 | nM | 9.96 |
| CHEMBL1256414 | — | Ki | = | 0.1148 | nM | 9.94 |
| CHEMBL1255723 | — | Ki | = | 0.182 | nM | 9.74 |
| CHEMBL1256378 | — | Ki | = | 0.2042 | nM | 9.69 |
| CHEMBL1256414 | — | Ki | = | 0.2754 | nM | 9.56 |
| CHEMBL1255724 | — | Ki | = | 0.3467 | nM | 9.46 |
| CHEMBL1256609 | — | Ki | = | 0.6918 | nM | 9.16 |
| CHEMBL1255771 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL1255770 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL1256610 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL1255617 | — | Ki | = | 1.905 | nM | 8.72 |
| CHEMBL353972 | ATIPAMEZOLE | Ki | = | 2.239 | nM | 8.65 |
| CHEMBL1255616 | — | Ki | = | 2.291 | nM | 8.64 |
| CHEMBL1256503 | — | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL1255617 | — | Ki | = | 3.715 | nM | 8.43 |
| CHEMBL1256566 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL1255582 | FIPAMEZOLE | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL1255617 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL1256503 | — | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL1256565 | — | Ki | = | 9.772 | nM | 8.01 |
| CHEMBL1256608 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL1256502 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL1256503 | — | Ki | = | 144.54 | nM | 6.84 |