Assay Detail
Binding
CHEMBL5135962
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged truncated human LRRK2 G2019S mutant using fluorescein labeled LRRKtide peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 90 mins in presence of ATP at Km concentration by TR-FRET Lanthascreen assay
6
Total Activities
6
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
2-Aminoquinazolines as LRRK2 Inhibitors for Treating Parkinson's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.82 | 10.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189225 | — | — | 1 | 10.19 |
| CHEMBL5195441 | — | — | 1 | 10.12 |
| CHEMBL5206036 | — | — | 1 | 9.77 |
| CHEMBL5199715 | — | — | 1 | 9.76 |
| CHEMBL5201483 | — | — | 1 | 9.73 |
| CHEMBL5204653 | — | — | 1 | 9.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189225 | — | IC50 | = | 0.06457 | nM | 10.19 |
| CHEMBL5195441 | — | IC50 | = | 0.07586 | nM | 10.12 |
| CHEMBL5206036 | — | IC50 | = | 0.169 | nM | 9.77 |
| CHEMBL5199715 | — | IC50 | = | 0.1742 | nM | 9.76 |
| CHEMBL5201483 | — | IC50 | = | 0.1875 | nM | 9.73 |
| CHEMBL5204653 | — | IC50 | = | 0.4508 | nM | 9.35 |