Assay Detail
Binding
CHEMBL4031825
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human wild type LRRK2 phosphorylation at ser935 expressed in BacMam transduced HEK293 cells after 48 hrs by in-cell Western assay
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.88 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3969077 | — | — | 1 | 7.77 |
| CHEMBL3961632 | — | — | 2 | 7.17 |
| CHEMBL3933899 | — | — | 1 | 7.16 |
| CHEMBL4084769 | — | — | 1 | 7.12 |
| CHEMBL3939513 | — | — | 1 | 7.07 |
| CHEMBL4100265 | — | — | 1 | 7.03 |
| CHEMBL4092521 | — | — | 1 | 6.96 |
| CHEMBL3961481 | — | — | 1 | 6.89 |
| CHEMBL4101218 | — | — | 1 | 6.80 |
| CHEMBL3919862 | — | — | 1 | 6.24 |
| CHEMBL4063115 | — | — | 1 | 6.16 |
| CHEMBL4077034 | — | — | 1 | 5.89 |
| CHEMBL4065198 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3969077 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3961632 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3961632 | — | IC50 | = | 67.61 | nM | 7.17 |
| CHEMBL3933899 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4084769 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3939513 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4100265 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4092521 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3961481 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4101218 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3919862 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4063115 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4077034 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4065198 | — | IC50 | - | — | - |