Assay Detail
Binding
CHEMBL5353277
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Inhibition of wildtype full length LRRK2 (unknown origin)
27
Total Activities
27
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 azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.91 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | — | 1 | 9.00 |
| CHEMBL5404275 | — | — | 1 | 7.96 |
| CHEMBL5394684 | — | — | 1 | 7.92 |
| CHEMBL5405161 | — | — | 1 | 7.80 |
| CHEMBL5174380 | — | — | 1 | 7.59 |
| CHEMBL5399757 | — | — | 1 | 7.39 |
| CHEMBL5414563 | — | — | 1 | 7.38 |
| CHEMBL5424518 | — | — | 1 | 7.36 |
| CHEMBL5438802 | — | — | 1 | 7.34 |
| CHEMBL5396660 | — | — | 1 | 7.31 |
| CHEMBL5423852 | — | — | 1 | 7.20 |
| CHEMBL5407973 | — | — | 1 | 7.01 |
| CHEMBL5437823 | — | — | 1 | 6.92 |
| CHEMBL5415941 | — | — | 1 | 6.89 |
| CHEMBL5434798 | — | — | 1 | 6.89 |
| CHEMBL5419250 | — | — | 1 | 6.88 |
| CHEMBL5426110 | — | — | 1 | 6.71 |
| CHEMBL5411845 | — | — | 1 | 6.57 |
| CHEMBL5437039 | — | — | 1 | 6.46 |
| CHEMBL5415043 | — | — | 1 | 6.20 |
| CHEMBL5411778 | — | — | 1 | 6.19 |
| CHEMBL5429455 | — | — | 1 | 6.16 |
| CHEMBL5433554 | — | — | 1 | 6.08 |
| CHEMBL5402964 | — | — | 1 | 6.06 |
| CHEMBL5404341 | — | — | 1 | 6.03 |
| CHEMBL5416722 | — | — | 1 | 5.87 |
| CHEMBL5396817 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5404275 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5394684 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5405161 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5174380 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL5399757 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL5414563 | — | IC50 | = | 41.7 | nM | 7.38 |
| CHEMBL5424518 | — | IC50 | = | 43.3 | nM | 7.36 |
| CHEMBL5438802 | — | IC50 | = | 45.2 | nM | 7.34 |
| CHEMBL5396660 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5423852 | — | IC50 | = | 63.4 | nM | 7.20 |
| CHEMBL5407973 | — | IC50 | = | 97.1 | nM | 7.01 |
| CHEMBL5437823 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL5415941 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL5434798 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5419250 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL5426110 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL5411845 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5437039 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL5415043 | — | IC50 | = | 632.0 | nM | 6.20 |
| CHEMBL5411778 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL5429455 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5433554 | — | IC50 | = | 834.0 | nM | 6.08 |
| CHEMBL5402964 | — | IC50 | = | 868.0 | nM | 6.06 |
| CHEMBL5404341 | — | IC50 | = | 942.0 | nM | 6.03 |
| CHEMBL5416722 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL5396817 | — | IC50 | = | 3230.0 | nM | 5.49 |