Assay Detail
Binding
CHEMBL5159130
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-Xa-tagged-AAK1 (30 to 330 residues) using (5-FAM)-Aha-KEEQSQITSQVTGQIGWR-NH2 as substrate incubated for 3 hrs in presence of ATP by electrophoretic analysis
31
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 |
Publication
Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.11 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5194899 | — | — | 1 | 8.38 |
| CHEMBL5202351 | — | — | 1 | 8.24 |
| CHEMBL4543869 | — | — | 1 | 8.21 |
| CHEMBL5195909 | — | — | 1 | 8.14 |
| CHEMBL5182431 | — | — | 1 | 7.96 |
| CHEMBL4872886 | — | — | 1 | 7.92 |
| CHEMBL5201888 | — | — | 1 | 7.92 |
| CHEMBL5205801 | — | — | 1 | 7.80 |
| CHEMBL5175828 | — | — | 1 | 7.77 |
| CHEMBL5207636 | — | — | 1 | 7.68 |
| CHEMBL5204563 | — | — | 1 | 7.66 |
| CHEMBL5170931 | — | — | 1 | 7.62 |
| CHEMBL5208293 | — | — | 1 | 7.52 |
| CHEMBL5200458 | — | — | 1 | 7.36 |
| CHEMBL5182634 | — | — | 1 | 7.17 |
| CHEMBL5204415 | — | — | 1 | 7.02 |
| CHEMBL5174061 | — | — | 1 | 6.96 |
| CHEMBL4862414 | — | — | 1 | 6.77 |
| CHEMBL5184309 | — | — | 1 | 6.77 |
| CHEMBL5209199 | — | — | 1 | 6.68 |
| CHEMBL5177481 | — | — | 1 | 6.66 |
| CHEMBL5193040 | — | — | 1 | 6.64 |
| CHEMBL5176849 | — | — | 1 | 6.47 |
| CHEMBL5171538 | — | — | 1 | 6.44 |
| CHEMBL5208680 | — | — | 1 | 6.44 |
| CHEMBL5187603 | — | — | 1 | 6.40 |
| CHEMBL5191369 | — | — | 1 | 6.38 |
| CHEMBL5172186 | — | — | 1 | 6.38 |
| CHEMBL5197898 | — | — | 1 | 5.96 |
| CHEMBL5179127 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5194899 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5202351 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4543869 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5195909 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL5182431 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4872886 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5201888 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5205801 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5175828 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5207636 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5204563 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5170931 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5208293 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5200458 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5182634 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5204415 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5174061 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4862414 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5184309 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5209199 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5177481 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5193040 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5176849 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5171538 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5208680 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5187603 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5191369 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5172186 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5197898 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5179127 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5193199 | — | IC50 | = | 5300.0 | nM | 5.28 |