Assay Detail
Functional
CHEMBL858653
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Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
32
Total Activities
16
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 16 | - | - |
| Kd | 9 | 7.86 | 8.95 |
| EC50 | 7 | 6.79 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305362 | — | — | 2 | 8.95 |
| CHEMBL300780 | — | — | 2 | 8.70 |
| CHEMBL154508 | — | — | 2 | 8.52 |
| CHEMBL426414 | — | — | 2 | 8.10 |
| CHEMBL25236 | BP-897 | — | 2 | 7.80 |
| CHEMBL361228 | — | — | 2 | 7.60 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 2 | 7.60 |
| CHEMBL112065 | — | — | 2 | 7.40 |
| CHEMBL110365 | — | — | 2 | 7.31 |
| CHEMBL168357 | — | — | 2 | 7.22 |
| CHEMBL169766 | — | — | 2 | 7.14 |
| CHEMBL26188 | — | — | 2 | 6.81 |
| CHEMBL114541 | — | — | 2 | 6.68 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 6.50 |
| CHEMBL168948 | — | — | 2 | 6.20 |
| CHEMBL277301 | — | — | 2 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305362 | — | Kd | = | 1.122 | nM | 8.95 |
| CHEMBL300780 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL154508 | — | Kd | = | 3.02 | nM | 8.52 |
| CHEMBL426414 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL25236 | BP-897 | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL361228 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL112065 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL110365 | — | EC50 | = | 48.98 | nM | 7.31 |
| CHEMBL168357 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL169766 | — | Kd | = | 72.44 | nM | 7.14 |
| CHEMBL26188 | — | EC50 | = | 154.88 | nM | 6.81 |
| CHEMBL114541 | — | EC50 | = | 208.93 | nM | 6.68 |
| CHEMBL54 | HALOPERIDOL | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL168948 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL277301 | — | EC50 | = | 1819.7 | nM | 5.74 |
| CHEMBL114541 | — | Activity | = | 100.0 | % | - |
| CHEMBL168357 | — | Activity | = | 40.0 | % | - |
| CHEMBL112065 | — | Activity | = | - | % | - |
| CHEMBL169766 | — | Activity | = | - | % | - |
| CHEMBL305362 | — | Activity | = | - | % | - |
| CHEMBL168948 | — | Activity | = | 30.0 | % | - |
| CHEMBL277301 | — | Activity | = | 41.0 | % | - |
| CHEMBL361228 | — | Activity | = | - | % | - |
| CHEMBL25236 | BP-897 | Activity | = | - | % | - |
| CHEMBL426414 | — | Activity | = | - | % | - |
| CHEMBL154508 | — | Activity | = | - | % | - |
| CHEMBL240773 | QUINPIROLE | Activity | = | 100.0 | % | - |
| CHEMBL110365 | — | Activity | = | 100.0 | % | - |
| CHEMBL54 | HALOPERIDOL | Activity | = | - | % | - |
| CHEMBL26188 | — | Activity | = | 54.0 | % | - |
| CHEMBL300780 | — | Activity | = | - | % | - |