Assay Detail
Binding
CHEMBL3854625
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Inhibition of PKA (unknown origin) using LRRASLG as substrate incubated for 30 mins by ADP-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.47 | 4.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL427058 | GSK-466317A | — | 1 | 4.90 |
| CHEMBL441702 | GSK-270822A | — | 1 | 4.30 |
| CHEMBL374453 | GSK-299115A | — | 1 | 4.20 |
| CHEMBL6067650 | PAROXETINE HYDROCHLORIDE | 4.0 | 1 | - |
| CHEMBL3918278 | — | — | 1 | - |
| CHEMBL384073 | GSK-180736A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL427058 | GSK-466317A | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL441702 | GSK-270822A | IC50 | = | 50100.0 | nM | 4.30 |
| CHEMBL374453 | GSK-299115A | IC50 | = | 63100.0 | nM | 4.20 |
| CHEMBL6067650 | PAROXETINE HYDROCHLORIDE | IC50 | > | 45000.0 | nM | - |
| CHEMBL3918278 | — | IC50 | = | 199500.0 | nM | - |
| CHEMBL384073 | GSK-180736A | IC50 | > | 500000.0 | nM | - |