Assay Detail
Binding
CHEMBL5040109
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti-phospho-LRRKtide antibody addition and measured after 30 mins by TR-FRET based Lanthascreen kinase activity assay
32
Total Activities
31
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 |
|---|---|---|---|
| IC50 | 32 | 6.79 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5075978 | — | — | 1 | 8.22 |
| CHEMBL5091909 | — | — | 1 | 8.22 |
| CHEMBL5086513 | — | — | 1 | 7.82 |
| CHEMBL5086506 | — | — | 1 | 7.80 |
| CHEMBL5089152 | — | — | 2 | 7.72 |
| CHEMBL5087055 | — | — | 1 | 7.70 |
| CHEMBL5092087 | — | — | 1 | 7.64 |
| CHEMBL5080937 | — | — | 1 | 7.47 |
| CHEMBL5090953 | — | — | 1 | 7.47 |
| CHEMBL5075824 | — | — | 1 | 7.42 |
| CHEMBL5083563 | — | — | 1 | 7.42 |
| CHEMBL5073900 | — | — | 1 | 7.38 |
| CHEMBL5088551 | — | — | 1 | 7.37 |
| CHEMBL5078540 | — | — | 1 | 7.33 |
| CHEMBL5091819 | — | — | 1 | 7.31 |
| CHEMBL5094228 | — | — | 1 | 7.24 |
| CHEMBL5089194 | — | — | 1 | 7.12 |
| CHEMBL5078779 | — | — | 1 | 6.78 |
| CHEMBL5073457 | — | — | 1 | 6.63 |
| CHEMBL5089834 | — | — | 1 | 6.61 |
| CHEMBL5074790 | — | — | 1 | 6.29 |
| CHEMBL5093192 | — | — | 1 | 6.24 |
| CHEMBL5092519 | — | — | 1 | 5.90 |
| CHEMBL5083940 | — | — | 1 | 5.83 |
| CHEMBL5070699 | — | — | 1 | 5.68 |
| CHEMBL5080604 | — | — | 1 | 5.50 |
| CHEMBL5091544 | — | — | 1 | 5.33 |
| CHEMBL5083394 | — | — | 1 | 5.25 |
| CHEMBL5093047 | — | — | 1 | 5.22 |
| CHEMBL5091290 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5075978 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5091909 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5086513 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5086506 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5089152 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5087055 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5092087 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5090953 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5080937 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5075824 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5083563 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5073900 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5088551 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5089152 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5078540 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5091819 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5094228 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5089194 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5078779 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5073457 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL5089834 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL5074790 | — | IC50 | = | 508.0 | nM | 6.29 |
| CHEMBL5093192 | — | IC50 | = | 572.0 | nM | 6.24 |
| CHEMBL5092519 | — | IC50 | = | 1258.0 | nM | 5.90 |
| CHEMBL5083940 | — | IC50 | = | 1484.0 | nM | 5.83 |
| CHEMBL5070699 | — | IC50 | = | 2109.0 | nM | 5.68 |
| CHEMBL5080604 | — | IC50 | = | 3192.0 | nM | 5.50 |
| CHEMBL5091544 | — | IC50 | = | 4619.0 | nM | 5.33 |
| CHEMBL5083394 | — | IC50 | = | 5663.0 | nM | 5.25 |
| CHEMBL5093047 | — | IC50 | = | 6055.0 | nM | 5.22 |
| CHEMBL5091290 | — | IC50 | = | 6832.0 | nM | 5.17 |
| CHEMBL5089345 | — | IC50 | = | 14381.0 | nM | 4.84 |