Assay Detail
Functional
CHEMBL4337844
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Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins 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 | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1<i>S</i>,3<i>R</i>)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 7.83 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3421729 | MEVIDALEN | 2.0 | 1 | 8.52 |
| CHEMBL3421730 | — | — | 1 | 7.86 |
| CHEMBL3421836 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3421729 | MEVIDALEN | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3421730 | — | EC50 | = | 13.9 | nM | 7.86 |
| CHEMBL3421836 | — | EC50 | = | 76.0 | nM | 7.12 |