Assay Detail
Binding
CHEMBL5049599
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Inhibition of AKK1 in HEK293F cells assessed as reduction in phospho mu2 formation incubated for 3 hrs by Western blot analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293F |
| Confidence | 9 — Direct single protein target |
| 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 |
|---|---|---|---|
| IC50 | 21 | 7.86 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5092306 | — | — | 1 | 9.10 |
| CHEMBL5088205 | — | — | 1 | 9.05 |
| CHEMBL5089410 | PILAVAPADIN | 2.0 | 1 | 8.70 |
| CHEMBL5084823 | — | — | 1 | 8.19 |
| CHEMBL5088767 | — | — | 1 | 8.12 |
| CHEMBL5082933 | — | — | 1 | 8.11 |
| CHEMBL5093649 | — | — | 1 | 8.07 |
| CHEMBL5080544 | — | — | 1 | 8.04 |
| CHEMBL5074638 | — | — | 1 | 8.04 |
| CHEMBL5084977 | — | — | 1 | 7.96 |
| CHEMBL5085373 | — | — | 1 | 7.72 |
| CHEMBL5085230 | — | — | 1 | 7.62 |
| CHEMBL5069779 | — | — | 1 | 7.60 |
| CHEMBL5074777 | — | — | 1 | 7.54 |
| CHEMBL5088856 | — | — | 1 | 7.44 |
| CHEMBL5079068 | — | — | 1 | 7.32 |
| CHEMBL5077192 | — | — | 1 | 7.10 |
| CHEMBL5085177 | — | — | 1 | 7.05 |
| CHEMBL5086617 | — | — | 1 | 6.54 |
| CHEMBL5079451 | — | — | 1 | - |
| CHEMBL5089204 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5092306 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5088205 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5089410 | PILAVAPADIN | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5084823 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5088767 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5082933 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5093649 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL5080544 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL5074638 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5084977 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5085373 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5085230 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5069779 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5074777 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5088856 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5079068 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5077192 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5085177 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5086617 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5079451 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5089204 | — | IC50 | > | 100.0 | nM | - |