Assay Detail
Functional
CHEMBL4392180
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Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.77 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216393 | — | — | 1 | 8.70 |
| CHEMBL375596 | — | — | 1 | 7.17 |
| CHEMBL4448320 | — | — | 1 | 7.08 |
| CHEMBL4587925 | — | — | 1 | 6.34 |
| CHEMBL4443054 | — | — | 1 | 6.33 |
| CHEMBL4442548 | — | — | 1 | 5.88 |
| CHEMBL4454068 | — | — | 1 | 5.79 |
| CHEMBL4437912 | — | — | 1 | 5.72 |
| CHEMBL4588808 | — | — | 1 | 5.67 |
| CHEMBL4473652 | — | — | 1 | 5.60 |
| CHEMBL4473792 | — | — | 1 | 5.51 |
| CHEMBL4572245 | — | — | 1 | 5.33 |
| CHEMBL4464861 | — | — | 1 | 5.20 |
| CHEMBL4443848 | — | — | 1 | 5.15 |
| CHEMBL4591118 | — | — | 1 | 4.40 |
| CHEMBL4436479 | — | — | 1 | 4.15 |
| CHEMBL4592753 | — | — | 1 | 4.06 |
| CHEMBL4453069 | — | — | 1 | - |
| CHEMBL4456754 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216393 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL375596 | — | IC50 | = | 68.4 | nM | 7.17 |
| CHEMBL4448320 | — | IC50 | = | 82.7 | nM | 7.08 |
| CHEMBL4587925 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL4443054 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL4442548 | — | IC50 | = | 1311.0 | nM | 5.88 |
| CHEMBL4454068 | — | IC50 | = | 1629.0 | nM | 5.79 |
| CHEMBL4437912 | — | IC50 | = | 1908.0 | nM | 5.72 |
| CHEMBL4588808 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL4473652 | — | IC50 | = | 2521.0 | nM | 5.60 |
| CHEMBL4473792 | — | IC50 | = | 3064.0 | nM | 5.51 |
| CHEMBL4572245 | — | IC50 | = | 4701.0 | nM | 5.33 |
| CHEMBL4464861 | — | IC50 | = | 6343.0 | nM | 5.20 |
| CHEMBL4443848 | — | IC50 | = | 7059.0 | nM | 5.15 |
| CHEMBL4591118 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4436479 | — | IC50 | = | 70157.0 | nM | 4.15 |
| CHEMBL4592753 | — | IC50 | = | 86493.0 | nM | 4.06 |
| CHEMBL4453069 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4456754 | — | IC50 | > | 100000.0 | nM | - |