Assay Detail
Binding
CHEMBL674046
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Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.70 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267014 | L-745870 | — | 1 | 9.40 |
| CHEMBL310843 | — | — | 1 | 8.57 |
| CHEMBL309372 | — | — | 1 | 8.37 |
| CHEMBL77563 | — | — | 2 | 8.07 |
| CHEMBL77151 | — | — | 2 | 8.02 |
| CHEMBL76982 | — | — | 2 | 7.83 |
| CHEMBL77969 | — | — | 1 | 7.69 |
| CHEMBL306711 | — | — | 1 | 7.58 |
| CHEMBL77708 | — | — | 1 | 7.28 |
| CHEMBL77850 | — | — | 1 | 7.10 |
| CHEMBL440687 | ABT-724 | — | 1 | 6.78 |
| CHEMBL76653 | — | — | 1 | 6.42 |
| CHEMBL80469 | — | — | 1 | 6.14 |
| CHEMBL78473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267014 | L-745870 | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL310843 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL309372 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL77563 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL77563 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL77151 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL77151 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL76982 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL76982 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL77969 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL306711 | — | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL77708 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL77850 | — | Ki | = | 79.6 | nM | 7.10 |
| CHEMBL440687 | ABT-724 | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL76653 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL80469 | — | Ki | = | 719.0 | nM | 6.14 |
| CHEMBL78473 | — | Ki | > | 10000.0 | nM | - |