Assay Detail
Binding
CHEMBL4397356
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]IABN from recombinant human D3 receptor stably expressed in HEK293 cell membranes measured after 60 mins by scintillation counting analysis
44
Total Activities
44
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
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D<sub>3</sub> Receptor (D<sub>3</sub>R) Ligand Promiscuity across Highly Conserved Aminergic G-Protein-Coupled Receptors (GPCRs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 6.94 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | 2.0 | 1 | 9.48 |
| CHEMBL4525842 | — | — | 1 | 8.49 |
| CHEMBL4083252 | — | — | 1 | 8.19 |
| CHEMBL4084262 | — | — | 1 | 7.92 |
| CHEMBL4438361 | — | — | 1 | 7.83 |
| CHEMBL4062553 | — | — | 1 | 7.71 |
| CHEMBL4459784 | — | — | 1 | 7.68 |
| CHEMBL26789 | — | — | 1 | 7.62 |
| CHEMBL4549664 | — | — | 1 | 7.59 |
| CHEMBL4534961 | — | — | 1 | 7.59 |
| CHEMBL4073927 | — | — | 1 | 7.59 |
| CHEMBL4476163 | — | — | 1 | 7.56 |
| CHEMBL4438524 | — | — | 1 | 7.49 |
| CHEMBL4471201 | — | — | 1 | 7.48 |
| CHEMBL4535104 | — | — | 1 | 7.40 |
| CHEMBL4475482 | — | — | 1 | 7.35 |
| CHEMBL4554630 | — | — | 1 | 7.31 |
| CHEMBL4451865 | — | — | 1 | 7.24 |
| CHEMBL4466055 | — | — | 1 | 7.23 |
| CHEMBL4528652 | — | — | 1 | 7.21 |
| CHEMBL4590969 | — | — | 1 | 7.20 |
| CHEMBL4552459 | — | — | 1 | 7.12 |
| CHEMBL4514100 | — | — | 1 | 7.05 |
| CHEMBL4516504 | — | — | 1 | 7.03 |
| CHEMBL4100699 | — | — | 1 | 7.01 |
| CHEMBL4541692 | — | — | 1 | 7.00 |
| CHEMBL4483044 | — | — | 1 | 6.95 |
| CHEMBL4541869 | — | — | 1 | 6.86 |
| CHEMBL4555876 | — | — | 1 | 6.68 |
| CHEMBL4516927 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267930 | SPIPERONE | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL4525842 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL4083252 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4084262 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4438361 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL4062553 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL4459784 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL26789 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL4549664 | — | Ki | = | 25.4 | nM | 7.59 |
| CHEMBL4534961 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL4073927 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL4476163 | — | Ki | = | 27.8 | nM | 7.56 |
| CHEMBL4438524 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL4471201 | — | Ki | = | 33.3 | nM | 7.48 |
| CHEMBL4535104 | — | Ki | = | 39.8 | nM | 7.40 |
| CHEMBL4475482 | — | Ki | = | 45.1 | nM | 7.35 |
| CHEMBL4554630 | — | Ki | = | 48.7 | nM | 7.31 |
| CHEMBL4451865 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4466055 | — | Ki | = | 59.2 | nM | 7.23 |
| CHEMBL4528652 | — | Ki | = | 61.5 | nM | 7.21 |
| CHEMBL4590969 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4552459 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL4514100 | — | Ki | = | 89.7 | nM | 7.05 |
| CHEMBL4516504 | — | Ki | = | 92.9 | nM | 7.03 |
| CHEMBL4100699 | — | Ki | = | 97.7 | nM | 7.01 |
| CHEMBL4541692 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL4483044 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL4541869 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL4555876 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL4516927 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL4435765 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL4461920 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL4591835 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL4515093 | — | Ki | = | 418.0 | nM | 6.38 |
| CHEMBL4555952 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL4473583 | — | Ki | = | 1098.0 | nM | 5.96 |
| CHEMBL4472434 | — | Ki | = | 1145.0 | nM | 5.94 |
| CHEMBL4435834 | — | Ki | = | 2773.0 | nM | 5.56 |
| CHEMBL4453955 | — | Ki | = | 6647.0 | nM | 5.18 |
| CHEMBL4558652 | — | Ki | = | 14587.0 | nM | 4.84 |
| CHEMBL4483472 | — | Ki | = | 23256.0 | nM | 4.63 |
| CHEMBL4591203 | — | Ki | = | 72753.0 | nM | 4.14 |
| CHEMBL4470847 | — | Ki | > | 39319.0 | nM | - |
| CHEMBL4588709 | — | Ki | > | 50316.0 | nM | - |