Assay Detail
Binding
CHEMBL2398947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged LRRK2 after 1 hr by TR-FRET assay
4
Total Activities
4
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
Leucine-rich repeat serine/threonine-protein kinase 2 (CHEMBL1075104) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The development of CNS-active LRRK2 inhibitors using property-directed optimisation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.77 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 9.00 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.82 |
| CHEMBL2397013 | — | — | 1 | 7.66 |
| CHEMBL406821 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL535 | SUNITINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2397013 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL406821 | — | IC50 | = | 244.0 | nM | 6.61 |