Assay Detail
Binding
CHEMBL4011212
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Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D3 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis
21
Total Activities
21
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
Novel Bivalent Ligands Based on the Sumanirole Pharmacophore Reveal Dopamine D2 Receptor (D2R) Biased Agonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.10 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4093477 | — | — | 1 | 9.16 |
| CHEMBL4078379 | — | — | 1 | 8.61 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.53 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.45 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 8.17 |
| CHEMBL4097572 | — | — | 1 | 7.11 |
| CHEMBL4093223 | — | — | 1 | 7.09 |
| CHEMBL4068455 | — | — | 1 | 7.08 |
| CHEMBL4059581 | — | — | 1 | 7.03 |
| CHEMBL4076129 | — | — | 1 | 6.95 |
| CHEMBL4065353 | — | — | 1 | 6.94 |
| CHEMBL4071243 | — | — | 1 | 6.86 |
| CHEMBL4086953 | — | — | 1 | 6.85 |
| CHEMBL4100322 | — | — | 1 | 6.64 |
| CHEMBL4060603 | — | — | 1 | 6.42 |
| CHEMBL4096422 | — | — | 1 | 6.42 |
| CHEMBL4085282 | — | — | 1 | 6.25 |
| CHEMBL419792 | SUMANIROLE | 3.0 | 1 | 6.24 |
| CHEMBL4100734 | — | — | 1 | 6.22 |
| CHEMBL4095452 | — | — | 1 | 6.19 |
| CHEMBL4077430 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4093477 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL4078379 | — | Ki | = | 2.45 | nM | 8.61 |
| CHEMBL59 | DOPAMINE | Ki | = | 2.97 | nM | 8.53 |
| CHEMBL1112 | ARIPIPRAZOLE | Ki | = | 3.57 | nM | 8.45 |
| CHEMBL240773 | QUINPIROLE | Ki | = | 6.76 | nM | 8.17 |
| CHEMBL4097572 | — | Ki | = | 77.7 | nM | 7.11 |
| CHEMBL4093223 | — | Ki | = | 80.6 | nM | 7.09 |
| CHEMBL4068455 | — | Ki | = | 83.9 | nM | 7.08 |
| CHEMBL4059581 | — | Ki | = | 94.2 | nM | 7.03 |
| CHEMBL4076129 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL4065353 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL4071243 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL4086953 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL4100322 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL4060603 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL4096422 | — | Ki | = | 382.0 | nM | 6.42 |
| CHEMBL4085282 | — | Ki | = | 558.0 | nM | 6.25 |
| CHEMBL419792 | SUMANIROLE | Ki | = | 573.0 | nM | 6.24 |
| CHEMBL4100734 | — | Ki | = | 598.0 | nM | 6.22 |
| CHEMBL4095452 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL4077430 | — | Ki | = | 1350.0 | nM | 5.87 |