Assay Detail
Binding
CHEMBL5040128
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human LRRK2 (H970/E2527) G2019S mutant expressed in mammalian system assessed as dissociation constant measured at 1 uM by DiscoveRx KINOMEscan assay
2
Total Activities
2
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
Design and Synthesis of Pyrrolo[2,3-<i>d</i>]pyrimidine-Derived Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Checkpoint Kinase 1 (CHK1)-Derived Crystallographic Surrogate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 2 | 8.34 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5087055 | — | — | 1 | 8.41 |
| CHEMBL5092087 | — | — | 1 | 8.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5087055 | — | Kd | = | 3.9 | nM | 8.41 |
| CHEMBL5092087 | — | Kd | = | 5.5 | nM | 8.26 |