Assay Detail
Binding
CHEMBL4192178
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant catalytic human GST-tagged LLRK2 (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate after 1 hr by alexaFluor-ADP-based FRET assay
29
Total Activities
29
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
Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.00 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204350 | — | — | 1 | 8.00 |
| CHEMBL4204860 | — | — | 1 | 7.70 |
| CHEMBL2012582 | — | — | 1 | 7.70 |
| CHEMBL4218001 | — | — | 1 | 7.70 |
| CHEMBL4218856 | — | — | 1 | 6.96 |
| CHEMBL4211027 | — | — | 1 | 6.89 |
| CHEMBL4206138 | — | — | 1 | 6.55 |
| CHEMBL4203258 | — | — | 1 | 6.31 |
| CHEMBL4216488 | — | — | 1 | 6.26 |
| CHEMBL4214911 | — | — | 1 | 6.12 |
| CHEMBL4215437 | — | — | 1 | 5.92 |
| CHEMBL4207078 | — | — | 1 | 5.88 |
| CHEMBL4217734 | — | — | 1 | 5.87 |
| CHEMBL4206654 | — | — | 1 | 5.82 |
| CHEMBL1311313 | — | — | 1 | 5.77 |
| CHEMBL378695 | — | — | 1 | 5.66 |
| CHEMBL4203202 | — | — | 1 | 5.63 |
| CHEMBL1434292 | — | — | 1 | 5.50 |
| CHEMBL4210498 | — | — | 1 | 5.44 |
| CHEMBL227491 | — | — | 1 | 5.44 |
| CHEMBL4205499 | — | — | 1 | 5.42 |
| CHEMBL4207019 | — | — | 1 | 5.42 |
| CHEMBL4213079 | — | — | 1 | 5.27 |
| CHEMBL4204060 | — | — | 1 | 5.24 |
| CHEMBL4202514 | — | — | 1 | 5.22 |
| CHEMBL4208935 | — | — | 1 | 5.16 |
| CHEMBL570013 | — | — | 1 | 5.14 |
| CHEMBL4214200 | — | — | 1 | 5.06 |
| CHEMBL4202671 | — | — | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204350 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4204860 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2012582 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4218001 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4218856 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4211027 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4206138 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4203258 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4216488 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4214911 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4215437 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4207078 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL4217734 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL4206654 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1311313 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL378695 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL4203202 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL1434292 | — | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL4210498 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL227491 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL4205499 | — | IC50 | = | 3830.0 | nM | 5.42 |
| CHEMBL4207019 | — | IC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL4213079 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL4204060 | — | IC50 | = | 5760.0 | nM | 5.24 |
| CHEMBL4202514 | — | IC50 | = | 6020.0 | nM | 5.22 |
| CHEMBL4208935 | — | IC50 | = | 6980.0 | nM | 5.16 |
| CHEMBL570013 | — | IC50 | = | 7270.0 | nM | 5.14 |
| CHEMBL4214200 | — | IC50 | = | 8740.0 | nM | 5.06 |
| CHEMBL4202671 | — | IC50 | = | 15400.0 | nM | 4.81 |