Assay Detail
Binding
CHEMBL5040108
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human GST tagged truncated LRRK2 G2019S mutant incubated for 2 hrs by TR-FRET based Lanthascreen kinase activity assay
26
Total Activities
26
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
Design and Synthesis of Pyrrolo[2,3-<i>d</i>]pyrimidine-Derived Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Checkpoint Kinase 1 (CHK1)-Derived Crystallographic Surrogate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.30 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5075978 | — | — | 1 | 9.52 |
| CHEMBL5091909 | — | — | 1 | 9.40 |
| CHEMBL5086513 | — | — | 1 | 9.15 |
| CHEMBL5073900 | — | — | 1 | 8.70 |
| CHEMBL5083563 | — | — | 1 | 8.70 |
| CHEMBL5090953 | — | — | 1 | 8.70 |
| CHEMBL5089194 | — | — | 1 | 8.52 |
| CHEMBL5093192 | — | — | 1 | 7.96 |
| CHEMBL5073457 | — | — | 1 | 7.89 |
| CHEMBL5089834 | — | — | 1 | 7.89 |
| CHEMBL5078779 | — | — | 1 | 7.85 |
| CHEMBL5092519 | — | — | 1 | 7.48 |
| CHEMBL5070699 | — | — | 1 | 7.12 |
| CHEMBL5093047 | — | — | 1 | 6.92 |
| CHEMBL5083940 | — | — | 1 | 6.90 |
| CHEMBL5080604 | — | — | 1 | 6.81 |
| CHEMBL5083394 | — | — | 1 | 6.67 |
| CHEMBL5092458 | — | — | 1 | 6.61 |
| CHEMBL5091544 | — | — | 1 | 6.59 |
| CHEMBL5091290 | — | — | 1 | 6.36 |
| CHEMBL5089345 | — | — | 1 | 6.23 |
| CHEMBL5081980 | — | — | 1 | 6.10 |
| CHEMBL407391 | DIMETHYLADENINE | — | 1 | 5.85 |
| CHEMBL5086355 | — | — | 1 | 5.70 |
| CHEMBL226345 | ADENINE | 3.0 | 1 | 5.17 |
| CHEMBL388593 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5075978 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL5091909 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL5086513 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL5073900 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL5083563 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL5090953 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL5089194 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5093192 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5073457 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5089834 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5078779 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5092519 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5070699 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL5093047 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL5083940 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL5080604 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL5083394 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL5092458 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL5091544 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL5091290 | — | Ki | = | 439.0 | nM | 6.36 |
| CHEMBL5089345 | — | Ki | = | 589.0 | nM | 6.23 |
| CHEMBL5081980 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL407391 | DIMETHYLADENINE | Ki | = | 1425.0 | nM | 5.85 |
| CHEMBL5086355 | — | Ki | = | 1982.0 | nM | 5.70 |
| CHEMBL226345 | ADENINE | Ki | = | 6715.0 | nM | 5.17 |
| CHEMBL388593 | — | Ki | = | 11312.0 | nM | 4.95 |