Assay Detail
Binding
CHEMBL3390652
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Inhibition of recombinant LRRK2 (unknown origin) using gamma-32P-ATP assessed as LRRKtide substrate phosphorylation level by autoradiography
15
Total Activities
15
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
Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.55 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012582 | — | — | 1 | 8.46 |
| CHEMBL2206014 | — | — | 1 | 7.82 |
| CHEMBL3335345 | — | — | 1 | 7.51 |
| CHEMBL3335349 | — | — | 1 | 7.34 |
| CHEMBL3335330 | — | — | 1 | 6.79 |
| CHEMBL3335346 | — | — | 1 | 6.71 |
| CHEMBL3335333 | — | — | 1 | 6.69 |
| CHEMBL3335344 | — | — | 1 | 6.69 |
| CHEMBL3335328 | — | — | 1 | 6.58 |
| CHEMBL3335331 | — | — | 1 | 6.33 |
| CHEMBL3335348 | — | — | 1 | 5.82 |
| CHEMBL3335332 | — | — | 1 | 5.00 |
| CHEMBL3335335 | — | — | 1 | 5.00 |
| CHEMBL3335329 | — | — | 1 | 4.92 |
| CHEMBL3335347 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012582 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL2206014 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3335345 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3335349 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3335330 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL3335346 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL3335333 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL3335344 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL3335328 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL3335331 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL3335348 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3335332 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3335335 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3335329 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3335347 | — | IC50 | > | 10000.0 | nM | - |