Assay Detail
Binding
CHEMBL4010109
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 by TR-FRET assay
26
Total Activities
26
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 | 26 | 7.81 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100904 | — | — | 1 | 9.15 |
| CHEMBL4098877 | MLi-2 | — | 1 | 9.12 |
| CHEMBL4093185 | — | — | 1 | 9.10 |
| CHEMBL4066983 | — | — | 1 | 8.72 |
| CHEMBL4065697 | — | — | 1 | 8.70 |
| CHEMBL4093321 | — | — | 1 | 8.66 |
| CHEMBL4075961 | — | — | 1 | 8.59 |
| CHEMBL4065525 | — | — | 1 | 8.57 |
| CHEMBL4075195 | — | — | 1 | 8.36 |
| CHEMBL4082856 | — | — | 1 | 8.24 |
| CHEMBL4071415 | — | — | 1 | 8.19 |
| CHEMBL4103352 | — | — | 1 | 8.18 |
| CHEMBL3928102 | — | — | 1 | 8.14 |
| CHEMBL4068699 | — | — | 1 | 7.92 |
| CHEMBL4062772 | — | — | 1 | 7.89 |
| CHEMBL4102839 | — | — | 1 | 7.82 |
| CHEMBL4078558 | — | — | 1 | 7.75 |
| CHEMBL4074145 | — | — | 1 | 7.39 |
| CHEMBL4090725 | — | — | 1 | 7.19 |
| CHEMBL4089811 | — | — | 1 | 7.01 |
| CHEMBL4060044 | — | — | 1 | 6.87 |
| CHEMBL4081949 | — | — | 1 | 6.59 |
| CHEMBL1234032 | — | — | 1 | 6.04 |
| CHEMBL4103247 | — | — | 1 | 5.91 |
| CHEMBL4078985 | — | — | 1 | 5.21 |
| CHEMBL4098447 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100904 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4098877 | MLi-2 | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL4093185 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4066983 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4065697 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4093321 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4075961 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4065525 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4075195 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4082856 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4071415 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4103352 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3928102 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4068699 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4062772 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4102839 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4078558 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4074145 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4090725 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4089811 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4060044 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4081949 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL1234032 | — | IC50 | = | 904.0 | nM | 6.04 |
| CHEMBL4103247 | — | IC50 | = | 1231.0 | nM | 5.91 |
| CHEMBL4078985 | — | IC50 | = | 6186.0 | nM | 5.21 |
| CHEMBL4098447 | — | IC50 | < | 0.6 | nM | - |