Assay Detail
Binding
CHEMBL5040107
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant 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
36
Total Activities
35
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 | 36 | 6.74 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5075978 | — | — | 1 | 8.30 |
| CHEMBL5091909 | — | — | 1 | 8.22 |
| CHEMBL5086506 | — | — | 1 | 8.00 |
| CHEMBL5086513 | — | — | 1 | 7.96 |
| CHEMBL5087055 | — | — | 1 | 7.92 |
| CHEMBL5089152 | — | — | 2 | 7.92 |
| CHEMBL5092087 | — | — | 1 | 7.85 |
| CHEMBL5080937 | — | — | 1 | 7.68 |
| CHEMBL5075824 | — | — | 1 | 7.60 |
| CHEMBL5073900 | — | — | 1 | 7.57 |
| CHEMBL5090953 | — | — | 1 | 7.55 |
| CHEMBL5083563 | — | — | 1 | 7.52 |
| CHEMBL5088551 | — | — | 1 | 7.46 |
| CHEMBL5078540 | — | — | 1 | 7.43 |
| CHEMBL5091819 | — | — | 1 | 7.38 |
| CHEMBL5089194 | — | — | 1 | 7.37 |
| CHEMBL5094228 | — | — | 1 | 7.29 |
| CHEMBL5093192 | — | — | 1 | 6.80 |
| CHEMBL5078779 | — | — | 1 | 6.70 |
| CHEMBL5073457 | — | — | 1 | 6.69 |
| CHEMBL5089834 | — | — | 1 | 6.66 |
| CHEMBL5074790 | — | — | 1 | 6.45 |
| CHEMBL5092519 | — | — | 1 | 6.32 |
| CHEMBL5070699 | — | — | 1 | 5.89 |
| CHEMBL5093047 | — | — | 1 | 5.76 |
| CHEMBL5083940 | — | — | 1 | 5.72 |
| CHEMBL5080604 | — | — | 1 | 5.65 |
| CHEMBL5083394 | — | — | 1 | 5.51 |
| CHEMBL407391 | DIMETHYLADENINE | — | 1 | 5.47 |
| CHEMBL5092458 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5075978 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5091909 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5086506 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5086513 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5087055 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5089152 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5092087 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5080937 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5075824 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5073900 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5089152 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5090953 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5083563 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5088551 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5078540 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5091819 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5089194 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5094228 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5093192 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL5078779 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL5073457 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL5089834 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL5074790 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL5092519 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL5070699 | — | IC50 | = | 1287.0 | nM | 5.89 |
| CHEMBL5093047 | — | IC50 | = | 1739.0 | nM | 5.76 |
| CHEMBL5083940 | — | IC50 | = | 1909.0 | nM | 5.72 |
| CHEMBL5080604 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL5083394 | — | IC50 | = | 3083.0 | nM | 5.51 |
| CHEMBL407391 | DIMETHYLADENINE | IC50 | = | 3355.0 | nM | 5.47 |
| CHEMBL5092458 | — | IC50 | = | 3532.0 | nM | 5.45 |
| CHEMBL5091544 | — | IC50 | = | 3764.0 | nM | 5.42 |
| CHEMBL5091290 | — | IC50 | = | 6387.0 | nM | 5.20 |
| CHEMBL5089345 | — | IC50 | = | 8564.0 | nM | 5.07 |
| CHEMBL226345 | ADENINE | IC50 | = | 15809.0 | nM | 4.80 |
| CHEMBL388593 | — | IC50 | = | 26630.0 | nM | 4.58 |