Assay Detail
Binding
CHEMBL671074
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Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand
34
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.29 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202213 | — | — | 1 | 8.70 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.40 |
| CHEMBL1202205 | — | — | 1 | 8.30 |
| CHEMBL1202215 | — | — | 1 | 8.30 |
| CHEMBL1202216 | — | — | 1 | 8.30 |
| CHEMBL1202206 | — | — | 1 | 8.15 |
| CHEMBL1202214 | — | — | 1 | 8.00 |
| CHEMBL1202202 | — | — | 1 | 7.92 |
| CHEMBL1202219 | — | — | 1 | 7.89 |
| CHEMBL1202211 | — | — | 1 | 7.77 |
| CHEMBL1202225 | — | — | 1 | 7.50 |
| CHEMBL341497 | — | — | 1 | 7.43 |
| CHEMBL1204119 | — | — | 1 | 7.35 |
| CHEMBL1202223 | — | — | 1 | 7.25 |
| CHEMBL2092961 | — | — | 1 | 7.22 |
| CHEMBL125455 | — | — | 1 | 7.19 |
| CHEMBL1204116 | — | — | 2 | 7.19 |
| CHEMBL1202209 | — | — | 1 | 7.17 |
| CHEMBL1202208 | — | — | 1 | 7.14 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.95 |
| CHEMBL1202210 | — | — | 1 | 6.89 |
| CHEMBL1202221 | — | — | 1 | 6.84 |
| CHEMBL1202217 | — | — | 1 | 6.77 |
| CHEMBL1202222 | — | — | 1 | 6.70 |
| CHEMBL1202212 | — | — | 1 | 6.68 |
| CHEMBL1202204 | — | — | 1 | 6.64 |
| CHEMBL1202220 | — | — | 1 | 6.61 |
| CHEMBL1203260 | — | — | 1 | 6.58 |
| CHEMBL1203257 | — | — | 1 | 6.12 |
| CHEMBL1202224 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202213 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1202215 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1202205 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1202216 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1202206 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1202214 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1202202 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1202219 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1202211 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1202225 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL341497 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1204119 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1202223 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2092961 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL125455 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1204116 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1202209 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1202208 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1204116 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL1202210 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL1202221 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL1202217 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL1202222 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL1202212 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL1202204 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL1202220 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL1203260 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL1203257 | — | IC50 | = | 766.0 | nM | 6.12 |
| CHEMBL1202224 | — | IC50 | = | 752.0 | nM | 6.12 |
| CHEMBL22242 | REMOXIPRIDE | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL1202207 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1202203 | — | IC50 | > | 10000.0 | nM | - |