Assay Detail
Binding
CHEMBL4815484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cells co-expressing CRE-Luc incubated for 60 mins by microbeta scintillation counting method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H<sub>2</sub>R and D<sub>3</sub>R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.39 | 9.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.58 |
| CHEMBL4856059 | — | — | 1 | 6.81 |
| CHEMBL4846638 | — | — | 1 | 6.58 |
| CHEMBL4875600 | — | — | 1 | 6.50 |
| CHEMBL4865765 | — | — | 1 | 6.45 |
| CHEMBL4860528 | — | — | 1 | 6.35 |
| CHEMBL4857560 | — | — | 1 | 6.32 |
| CHEMBL4853107 | — | — | 1 | 6.30 |
| CHEMBL4848815 | — | — | 1 | 6.28 |
| CHEMBL4878215 | — | — | 1 | 6.26 |
| CHEMBL4853668 | — | — | 1 | 6.25 |
| CHEMBL4846201 | — | — | 1 | 6.23 |
| CHEMBL4856005 | — | — | 1 | 6.22 |
| CHEMBL4867962 | — | — | 1 | 6.10 |
| CHEMBL249420 | DEXPRAMIPEXOLE | 3.0 | 1 | 6.00 |
| CHEMBL4853772 | — | — | 1 | 5.93 |
| CHEMBL4876799 | — | — | 1 | 5.90 |
| CHEMBL4846380 | — | — | 1 | 5.77 |
| CHEMBL4872375 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 0.263 | nM | 9.58 |
| CHEMBL4856059 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL4846638 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL4875600 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL4865765 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL4860528 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL4857560 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL4853107 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4848815 | — | Ki | = | 524.81 | nM | 6.28 |
| CHEMBL4878215 | — | Ki | = | 549.54 | nM | 6.26 |
| CHEMBL4853668 | — | Ki | = | 562.34 | nM | 6.25 |
| CHEMBL4846201 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL4856005 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL4867962 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL249420 | DEXPRAMIPEXOLE | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4853772 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL4876799 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL4846380 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL4872375 | — | Ki | = | 2511.89 | nM | 5.60 |