Assay Detail
Binding
CHEMBL4406063
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Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 51 | 6.21 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4590966 | — | — | 1 | 7.52 |
| CHEMBL4442936 | — | — | 1 | 7.07 |
| CHEMBL4514800 | — | — | 1 | 7.07 |
| CHEMBL4450429 | — | — | 1 | 7.00 |
| CHEMBL4584372 | — | — | 1 | 6.89 |
| CHEMBL4514586 | — | — | 1 | 6.88 |
| CHEMBL4475699 | — | — | 1 | 6.79 |
| CHEMBL4448853 | — | — | 1 | 6.75 |
| CHEMBL4444691 | — | — | 1 | 6.67 |
| CHEMBL4561808 | — | — | 1 | 6.66 |
| CHEMBL4578364 | — | — | 1 | 6.62 |
| CHEMBL4440698 | — | — | 1 | 6.54 |
| CHEMBL4453405 | — | — | 1 | 6.49 |
| CHEMBL4531363 | — | — | 1 | 6.42 |
| CHEMBL4452683 | — | — | 1 | 6.42 |
| CHEMBL4590356 | — | — | 1 | 6.30 |
| CHEMBL4472900 | — | — | 1 | 6.29 |
| CHEMBL4541924 | — | — | 1 | 6.26 |
| CHEMBL4577162 | — | — | 1 | 6.24 |
| CHEMBL4475406 | — | — | 1 | 6.24 |
| CHEMBL540612 | — | — | 1 | 6.20 |
| CHEMBL4443039 | — | — | 1 | 6.17 |
| CHEMBL4586582 | — | — | 1 | 6.17 |
| CHEMBL4590839 | — | — | 1 | 6.17 |
| CHEMBL4580817 | — | — | 1 | 6.11 |
| CHEMBL4454380 | — | — | 1 | 6.09 |
| CHEMBL4454872 | — | — | 1 | 6.07 |
| CHEMBL4593394 | — | — | 1 | 6.07 |
| CHEMBL4453478 | — | — | 1 | 6.06 |
| CHEMBL4522558 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4590966 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4442936 | — | Ki | = | 85.8 | nM | 7.07 |
| CHEMBL4514800 | — | Ki | = | 85.1 | nM | 7.07 |
| CHEMBL4450429 | — | Ki | = | 100.8 | nM | 7.00 |
| CHEMBL4584372 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4514586 | — | Ki | = | 132.8 | nM | 6.88 |
| CHEMBL4475699 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL4448853 | — | Ki | = | 179.2 | nM | 6.75 |
| CHEMBL4444691 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL4561808 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL4578364 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL4440698 | — | Ki | = | 291.7 | nM | 6.54 |
| CHEMBL4453405 | — | Ki | = | 326.1 | nM | 6.49 |
| CHEMBL4452683 | — | Ki | = | 384.6 | nM | 6.42 |
| CHEMBL4531363 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL4590356 | — | Ki | = | 501.2 | nM | 6.30 |
| CHEMBL4472900 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL4541924 | — | Ki | = | 553.0 | nM | 6.26 |
| CHEMBL4577162 | — | Ki | = | 575.0 | nM | 6.24 |
| CHEMBL4475406 | — | Ki | = | 575.0 | nM | 6.24 |
| CHEMBL540612 | — | Ki | = | 634.0 | nM | 6.20 |
| CHEMBL4443039 | — | Ki | = | 676.0 | nM | 6.17 |
| CHEMBL4586582 | — | Ki | = | 676.0 | nM | 6.17 |
| CHEMBL4590839 | — | Ki | = | 671.0 | nM | 6.17 |
| CHEMBL4580817 | — | Ki | = | 776.0 | nM | 6.11 |
| CHEMBL4454380 | — | Ki | = | 813.0 | nM | 6.09 |
| CHEMBL4593394 | — | Ki | = | 851.0 | nM | 6.07 |
| CHEMBL4454872 | — | Ki | = | 844.0 | nM | 6.07 |
| CHEMBL4453478 | — | Ki | = | 878.0 | nM | 6.06 |
| CHEMBL4522558 | — | Ki | = | 912.0 | nM | 6.04 |
| CHEMBL4456964 | — | Ki | = | 945.0 | nM | 6.03 |
| CHEMBL4546749 | — | Ki | = | 962.3 | nM | 6.02 |
| CHEMBL4585289 | — | Ki | = | 977.2 | nM | 6.01 |
| CHEMBL4467528 | — | Ki | = | 988.6 | nM | 6.00 |
| CHEMBL4439544 | — | Ki | = | 1047.0 | nM | 5.98 |
| CHEMBL4456007 | — | Ki | = | 1131.0 | nM | 5.95 |
| CHEMBL4442408 | — | Ki | = | 1142.0 | nM | 5.94 |
| CHEMBL4439535 | — | Ki | = | 1298.0 | nM | 5.89 |
| CHEMBL4525624 | — | Ki | = | 1318.0 | nM | 5.88 |
| CHEMBL4590211 | — | Ki | = | 1339.0 | nM | 5.87 |
| CHEMBL4543870 | — | Ki | = | 1413.0 | nM | 5.85 |
| CHEMBL4469584 | — | Ki | = | 1585.0 | nM | 5.80 |
| CHEMBL4569006 | — | Ki | = | 1609.0 | nM | 5.79 |
| CHEMBL4455719 | — | Ki | = | 1833.0 | nM | 5.74 |
| CHEMBL4527244 | — | Ki | = | 2011.0 | nM | 5.70 |
| CHEMBL4584481 | — | Ki | = | 2073.0 | nM | 5.68 |
| CHEMBL4470439 | — | Ki | = | 2171.0 | nM | 5.66 |
| CHEMBL4550187 | — | Ki | = | 2171.0 | nM | 5.66 |
| CHEMBL4452329 | — | Ki | = | 2222.0 | nM | 5.65 |
| CHEMBL4568916 | — | Ki | = | 2326.0 | nM | 5.63 |