Assay Detail
Binding
CHEMBL5136370
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse full-length LRRK2 G2019S mutant transfected in HEK293 cells using LRRKtide as substrate in presence of ATP by incubated for 1 hr TR-FRET based ADAPTA assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Leucine-rich repeat serine/threonine-protein kinase 2 (CHEMBL2010622) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of 1<i>H-</i>Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 40 | 5.66 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | — | 1 | 7.52 |
| CHEMBL5170238 | — | — | 1 | 6.58 |
| CHEMBL5181966 | — | — | 1 | 6.55 |
| CHEMBL5177578 | — | — | 1 | 6.54 |
| CHEMBL5173029 | — | — | 1 | 6.47 |
| CHEMBL5174380 | — | — | 1 | 6.41 |
| CHEMBL5172291 | — | — | 1 | 6.41 |
| CHEMBL5187306 | — | — | 1 | 6.22 |
| CHEMBL5198878 | — | — | 1 | 6.22 |
| CHEMBL5170225 | — | — | 1 | 6.16 |
| CHEMBL5179102 | — | — | 1 | 6.12 |
| CHEMBL5200500 | — | — | 1 | 6.12 |
| CHEMBL5197009 | — | — | 1 | 6.10 |
| CHEMBL5190962 | — | — | 1 | 6.04 |
| CHEMBL5204372 | — | — | 1 | 5.97 |
| CHEMBL5199239 | — | — | 1 | 5.89 |
| CHEMBL5185437 | — | — | 1 | 5.86 |
| CHEMBL5194234 | — | — | 1 | 5.84 |
| CHEMBL5202841 | — | — | 1 | 5.82 |
| CHEMBL5198203 | — | — | 1 | 5.77 |
| CHEMBL5196289 | — | — | 1 | 5.68 |
| CHEMBL5190480 | — | — | 1 | 5.64 |
| CHEMBL5207639 | — | — | 1 | 5.51 |
| CHEMBL5185136 | — | — | 1 | 5.50 |
| CHEMBL5202898 | — | — | 1 | 5.32 |
| CHEMBL5198788 | — | — | 1 | 5.31 |
| CHEMBL5205363 | — | — | 1 | 5.29 |
| CHEMBL5199105 | — | — | 1 | 5.19 |
| CHEMBL5188336 | — | — | 1 | 4.91 |
| CHEMBL5183984 | — | — | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098877 | MLi-2 | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5170238 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5181966 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5177578 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5173029 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5174380 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5172291 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5187306 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5198878 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5170225 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5200500 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5179102 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5197009 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5190962 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5204372 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL5199239 | — | EC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL5185437 | — | EC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL5194234 | — | EC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL5202841 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5198203 | — | EC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL5196289 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5190480 | — | EC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL5207639 | — | EC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL5185136 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5202898 | — | EC50 | = | 4780.0 | nM | 5.32 |
| CHEMBL5198788 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5205363 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5199105 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5188336 | — | EC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL5183984 | — | EC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL5207466 | — | EC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL5195211 | — | EC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL5191932 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5208171 | — | EC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL5170423 | — | EC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL5185379 | — | EC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL5207757 | — | EC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL5198175 | — | EC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL5184765 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5173076 | — | EC50 | > | 100000.0 | nM | - |