Assay Detail
Functional
CHEMBL5029238
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Positive allosteric modulation of human D2 receptor expressed in CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring dopamine EC50 at 0.01 nM pretreated for 10 mins followed by forskolin stimulation for 5 mins and measured after 1 hr by HTRF assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of New Potent Positive Allosteric Modulators of Dopamine D<sub>2</sub> Receptors: Insights into the Bioisosteric Replacement of Proline to 3-Furoic Acid in the Melanostatin Neuropeptide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 6.74 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5078893 | — | — | 1 | 6.89 |
| CHEMBL317488 | — | — | 1 | 6.77 |
| CHEMBL5078216 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5078893 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL317488 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5078216 | — | EC50 | = | 280.0 | nM | 6.55 |