Assay Detail
Binding
CHEMBL4053561
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.37 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077536 | — | — | 1 | 9.35 |
| CHEMBL4089939 | — | — | 1 | 9.05 |
| CHEMBL4083903 | — | — | 1 | 8.82 |
| CHEMBL4068843 | — | — | 1 | 8.61 |
| CHEMBL2219578 | — | — | 1 | 8.41 |
| CHEMBL4097669 | — | — | 1 | 8.01 |
| CHEMBL85606 | — | — | 1 | 7.96 |
| CHEMBL4079637 | — | — | 1 | 7.63 |
| CHEMBL4095216 | — | — | 1 | 7.50 |
| CHEMBL4086613 | — | — | 1 | 7.46 |
| CHEMBL4105375 | — | — | 1 | 7.29 |
| CHEMBL4083890 | — | — | 1 | 6.83 |
| CHEMBL4067792 | — | — | 1 | 6.59 |
| CHEMBL4099491 | — | — | 1 | 6.24 |
| CHEMBL4087513 | — | — | 1 | 5.98 |
| CHEMBL4062165 | — | — | 1 | 5.96 |
| CHEMBL27162 | — | — | 1 | 5.82 |
| CHEMBL4076796 | — | — | 1 | 5.23 |
| CHEMBL4092619 | — | — | 1 | - |
| CHEMBL4064919 | — | — | 1 | - |
| CHEMBL4073520 | — | — | 1 | - |
| CHEMBL4100358 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077536 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL4089939 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL4083903 | — | Ki | = | 1.51 | nM | 8.82 |
| CHEMBL4068843 | — | Ki | = | 2.47 | nM | 8.61 |
| CHEMBL2219578 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4097669 | — | Ki | = | 9.81 | nM | 8.01 |
| CHEMBL85606 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4079637 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL4095216 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4086613 | — | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL4105375 | — | Ki | = | 51.7 | nM | 7.29 |
| CHEMBL4083890 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL4067792 | — | Ki | = | 256.0 | nM | 6.59 |
| CHEMBL4099491 | — | Ki | = | 581.0 | nM | 6.24 |
| CHEMBL4087513 | — | Ki | = | 1040.0 | nM | 5.98 |
| CHEMBL4062165 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL27162 | — | Ki | = | 1520.0 | nM | 5.82 |
| CHEMBL4076796 | — | Ki | = | 5890.0 | nM | 5.23 |
| CHEMBL4092619 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4064919 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4073520 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4100358 | — | Ki | > | 50000.0 | nM | - |