Assay Detail
Binding
CHEMBL4192179
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant catalytic human GST-tagged LLRK2 G2019S mutant (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate after 1 hr by alexaFluor-ADP-based FRET assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 25 | 5.96 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012582 | — | — | 1 | 7.70 |
| CHEMBL4218001 | — | — | 1 | 7.52 |
| CHEMBL4204350 | — | — | 1 | 7.30 |
| CHEMBL4204860 | — | — | 1 | 6.92 |
| CHEMBL4218856 | — | — | 1 | 6.54 |
| CHEMBL4211027 | — | — | 1 | 6.51 |
| CHEMBL4216488 | — | — | 1 | 6.29 |
| CHEMBL4203258 | — | — | 1 | 6.27 |
| CHEMBL4206138 | — | — | 1 | 6.24 |
| CHEMBL4207078 | — | — | 1 | 5.99 |
| CHEMBL4214911 | — | — | 1 | 5.96 |
| CHEMBL4215437 | — | — | 1 | 5.84 |
| CHEMBL4206654 | — | — | 1 | 5.70 |
| CHEMBL4217734 | — | — | 1 | 5.66 |
| CHEMBL378695 | — | — | 1 | 5.63 |
| CHEMBL227491 | — | — | 1 | 5.53 |
| CHEMBL4207019 | — | — | 1 | 5.51 |
| CHEMBL4203202 | — | — | 1 | 5.48 |
| CHEMBL4205499 | — | — | 1 | 5.43 |
| CHEMBL1434292 | — | — | 1 | 5.43 |
| CHEMBL4210498 | — | — | 1 | 5.27 |
| CHEMBL4202514 | — | — | 1 | 5.23 |
| CHEMBL1311313 | — | — | 1 | 5.17 |
| CHEMBL4214200 | — | — | 1 | 5.13 |
| CHEMBL4213079 | — | — | 1 | 4.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012582 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4218001 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4204350 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4204860 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4218856 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4211027 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4216488 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4203258 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4206138 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4207078 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4214911 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL4215437 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL4206654 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL4217734 | — | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL378695 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL227491 | — | IC50 | = | 2980.0 | nM | 5.53 |
| CHEMBL4207019 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL4203202 | — | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL4205499 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL1434292 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL4210498 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4202514 | — | IC50 | = | 5930.0 | nM | 5.23 |
| CHEMBL1311313 | — | IC50 | = | 6680.0 | nM | 5.17 |
| CHEMBL4214200 | — | IC50 | = | 7490.0 | nM | 5.13 |
| CHEMBL4213079 | — | IC50 | = | 21500.0 | nM | 4.67 |