Assay Detail
Binding
CHEMBL5353385
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Inhibition of GRK2 (unknown origin)
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Targeting GRK2 and GRK5 for treating chronic degenerative diseases: Advances and future perspectives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.37 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3809020 | — | — | 1 | 7.70 |
| CHEMBL1738878 | — | — | 2 | 7.70 |
| CHEMBL1738877 | — | — | 1 | 7.52 |
| CHEMBL60254 | BALANOL | — | 1 | 7.38 |
| CHEMBL4228779 | — | — | 1 | 6.80 |
| CHEMBL5412633 | — | — | 1 | 6.60 |
| CHEMBL384073 | GSK-180736A | — | 1 | 6.11 |
| CHEMBL487046 | — | — | 1 | 5.30 |
| CHEMBL517171 | GSK-1713088A | — | 1 | 5.20 |
| CHEMBL476259 | GSK-1326255A | — | 1 | 5.10 |
| CHEMBL463931 | GSK-2163632A | — | 1 | 4.70 |
| CHEMBL4464632 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3809020 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1738878 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1738877 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL60254 | BALANOL | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4228779 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5412633 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL384073 | GSK-180736A | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL487046 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL517171 | GSK-1713088A | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL476259 | GSK-1326255A | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL463931 | GSK-2163632A | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL1738878 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4464632 | — | IC50 | > | 100000.0 | nM | - |