Assay Detail
Binding
CHEMBL1274011
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Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.41 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1270323 | — | — | 1 | 9.47 |
| CHEMBL1270423 | — | — | 1 | 9.03 |
| CHEMBL1270121 | — | — | 1 | 8.82 |
| CHEMBL1270227 | — | — | 1 | 8.75 |
| CHEMBL1270013 | — | — | 1 | 8.71 |
| CHEMBL1270322 | — | — | 1 | 8.58 |
| CHEMBL1270516 | — | — | 1 | 8.54 |
| CHEMBL93403 | — | — | 1 | 8.30 |
| CHEMBL156845 | — | — | 1 | 8.04 |
| CHEMBL345111 | — | — | 1 | 7.95 |
| CHEMBL1270422 | — | — | 1 | 7.49 |
| CHEMBL1270120 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1270323 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL1270423 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL1270121 | — | Ki | = | 1.52 | nM | 8.82 |
| CHEMBL1270227 | — | Ki | = | 1.76 | nM | 8.75 |
| CHEMBL1270013 | — | Ki | = | 1.93 | nM | 8.71 |
| CHEMBL1270322 | — | Ki | = | 2.64 | nM | 8.58 |
| CHEMBL1270516 | — | Ki | = | 2.92 | nM | 8.54 |
| CHEMBL93403 | — | Ki | = | 4.97 | nM | 8.30 |
| CHEMBL156845 | — | Ki | = | 9.21 | nM | 8.04 |
| CHEMBL345111 | — | Ki | = | 11.29 | nM | 7.95 |
| CHEMBL1270422 | — | Ki | = | 32.71 | nM | 7.49 |
| CHEMBL1270120 | — | Ki | = | 63.95 | nM | 7.19 |