Assay Detail
Binding
CHEMBL4810446
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to FLAG-tagged GRK6 in human KMS11 cells incubated for 2.5 hrs by ITDR assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KMS-11 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.15 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4877302 | — | — | 1 | 7.52 |
| CHEMBL4860332 | — | — | 1 | 6.77 |
| CHEMBL4875929 | — | — | 1 | 6.21 |
| CHEMBL4854871 | — | — | 1 | 5.70 |
| CHEMBL4874424 | — | — | 1 | 5.70 |
| CHEMBL4847703 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4877302 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4860332 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4875929 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4854871 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4874424 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4847703 | — | IC50 | = | 10000.0 | nM | 5.00 |