Assay Detail
Binding
CHEMBL5707334
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged LRRK2 G2019S/A2016T mutant (1326 to 2527 residues) (unknown origin) in presence of ATP
3
Total Activities
3
Compounds Tested
1
Activity Types
2
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
Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.92 | 7.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0005180 |
| EFO_TERM | EFO_TERM | - | — | parkinson disease |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.40 |
| CHEMBL406821 | — | — | 1 | 5.48 |
| CHEMBL559147 | Y-27632 | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL406821 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL559147 | Y-27632 | IC50 | = | 13000.0 | nM | 4.89 |