Assay Detail
Binding
CHEMBL5377217
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CaMKK2 (161 to 449 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) star cells incubated for 20 mins in presence of kinase tracer 236 by TR-FRET
9
Total Activities
9
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 |
Target
Calcium/calmodulin-dependent protein kinase kinase 2 (CHEMBL5284) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.12 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5421767 | — | — | 1 | 8.85 |
| CHEMBL558642 | GSK-650394 | — | 1 | 8.64 |
| CHEMBL5439578 | — | — | 1 | 8.60 |
| CHEMBL5431962 | — | — | 1 | 8.40 |
| CHEMBL5426746 | — | — | 1 | 8.15 |
| CHEMBL5396413 | — | — | 1 | 8.15 |
| CHEMBL5422255 | — | — | 1 | 8.05 |
| CHEMBL5397685 | — | — | 1 | 7.30 |
| CHEMBL1182777 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5421767 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL558642 | GSK-650394 | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5439578 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5431962 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5426746 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5396413 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5422255 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5397685 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1182777 | — | IC50 | = | 120.0 | nM | 6.92 |