Assay Detail
ADMET
CHEMBL4666938
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Inhibition of recombinant human GST-tagged LRRK2 (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate incubated for 60 mins by Adapta assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.02 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744172 | — | — | 1 | 7.75 |
| CHEMBL4760562 | — | — | 1 | 7.10 |
| CHEMBL4777342 | — | — | 1 | 7.09 |
| CHEMBL4745474 | — | — | 1 | 6.75 |
| CHEMBL2178799 | — | — | 1 | 6.40 |
| CHEMBL4740778 | — | — | 1 | - |
| CHEMBL4742159 | — | — | 1 | - |
| CHEMBL4764019 | — | — | 1 | - |
| CHEMBL4746726 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744172 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4760562 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4777342 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4745474 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2178799 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4740778 | — | IC50 | - | — | - | |
| CHEMBL4742159 | — | IC50 | - | — | - | |
| CHEMBL4764019 | — | IC50 | - | — | - | |
| CHEMBL4746726 | — | IC50 | - | — | - |