Assay Detail
Binding
CHEMBL5049598
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3H-LP-927443 from AAK1 in mouse brain membrane homogenate assessed as inhibition constant at 1 uM incubated for 1 hr by liquid scintillation counter analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of (<i>S</i>)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 9.22 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5088205 | — | — | 1 | 10.40 |
| CHEMBL5082933 | — | — | 1 | 10.15 |
| CHEMBL5092306 | — | — | 1 | 10.10 |
| CHEMBL5093649 | — | — | 1 | 9.85 |
| CHEMBL5074777 | — | — | 1 | 9.77 |
| CHEMBL5069779 | — | — | 1 | 9.66 |
| CHEMBL5084823 | — | — | 1 | 9.60 |
| CHEMBL5089410 | PILAVAPADIN | 2.0 | 1 | 9.51 |
| CHEMBL5088856 | — | — | 1 | 9.39 |
| CHEMBL5086617 | — | — | 1 | 9.29 |
| CHEMBL5085230 | — | — | 1 | 9.19 |
| CHEMBL5085177 | — | — | 1 | 9.15 |
| CHEMBL5088767 | — | — | 1 | 8.96 |
| CHEMBL5084977 | — | — | 1 | 8.96 |
| CHEMBL5074638 | — | — | 1 | 8.92 |
| CHEMBL5085373 | — | — | 1 | 8.74 |
| CHEMBL5089204 | — | — | 1 | 8.68 |
| CHEMBL5079068 | — | — | 1 | 8.49 |
| CHEMBL5079451 | — | — | 1 | 8.41 |
| CHEMBL5077192 | — | — | 1 | 8.35 |
| CHEMBL5088528 | — | — | 1 | 8.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5088205 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL5082933 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL5092306 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL5093649 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL5074777 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL5069779 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL5084823 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL5089410 | PILAVAPADIN | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL5088856 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL5086617 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL5085230 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL5085177 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL5088767 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL5084977 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL5074638 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL5085373 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL5089204 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL5079068 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL5079451 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL5077192 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL5088528 | — | Ki | = | 7.2 | nM | 8.14 |