Assay Detail
Binding
CHEMBL5104730
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Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
5
Total Activities
5
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
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.90 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464150 | — | — | 1 | 8.19 |
| CHEMBL4559891 | — | — | 1 | 7.99 |
| CHEMBL4468760 | — | — | 1 | 7.93 |
| CHEMBL4573538 | — | — | 1 | 7.80 |
| CHEMBL5187909 | — | — | 1 | 7.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464150 | — | EC50 | = | 6.41 | nM | 8.19 |
| CHEMBL4559891 | — | EC50 | = | 10.3 | nM | 7.99 |
| CHEMBL4468760 | — | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4573538 | — | EC50 | = | 15.9 | nM | 7.80 |
| CHEMBL5187909 | — | EC50 | = | 25.6 | nM | 7.59 |