Assay Detail
Binding
CHEMBL4010117
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged LRRK2 (970 to 2527 residues) G2019S mutant expressed in baculovirus using fluorescein-ERM as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr in presence of 5 mM ATP by TR-FRET assay
12
Total Activities
12
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
Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.55 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | — | 1 | 8.19 |
| CHEMBL4066983 | — | — | 1 | 8.00 |
| CHEMBL4093321 | — | — | 1 | 7.96 |
| CHEMBL4065697 | — | — | 1 | 7.89 |
| CHEMBL4100904 | — | — | 1 | 7.85 |
| CHEMBL4065525 | — | — | 1 | 7.85 |
| CHEMBL4093185 | — | — | 1 | 7.66 |
| CHEMBL4075195 | — | — | 1 | 7.16 |
| CHEMBL4082856 | — | — | 1 | 7.12 |
| CHEMBL4075961 | — | — | 1 | 7.04 |
| CHEMBL3928102 | — | — | 1 | 7.02 |
| CHEMBL4103352 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4066983 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4093321 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4065697 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4100904 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4065525 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4093185 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4075195 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4082856 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4075961 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3928102 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4103352 | — | IC50 | = | 128.0 | nM | 6.89 |