Assay Detail
Binding
CHEMBL5136372
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse full-length wild type LRRK2 transfected in HEK293 cells using LRRKtide as substrate incubated for 1 hr in presence of ATP by TR-FRET based ADAPTA assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Leucine-rich repeat serine/threonine-protein kinase 2 (CHEMBL2010622) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of 1<i>H-</i>Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 4.70 | 5.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5181966 | — | — | 1 | 5.27 |
| CHEMBL5202841 | — | — | 1 | 4.12 |
| CHEMBL5196289 | — | — | 1 | - |
| CHEMBL5177578 | — | — | 1 | - |
| CHEMBL5170238 | — | — | 1 | - |
| CHEMBL5174380 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5181966 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL5202841 | — | EC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL5196289 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5177578 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5170238 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5174380 | — | EC50 | > | 100000.0 | nM | - |