Assay Detail
Binding
CHEMBL5507799
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged recombinant human AAK1 (1 to 510 residues) expressed in insect cells using Aha-KEEQSQITSQVTGQIGWR-NH2 as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay
26
Total Activities
26
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
Design, synthesis and biological evaluation of novel 1,2,4a,5-tetrahydro-4H-benzo[b][1,4]oxazino[4,3-d][1,4]oxazine-based AAK1 inhibitors with anti-viral property against SARS-CoV-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.22 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439128 | — | — | 1 | 8.12 |
| CHEMBL5557266 | — | — | 1 | 8.03 |
| CHEMBL5564665 | — | — | 1 | 7.95 |
| CHEMBL5560434 | — | — | 1 | 7.88 |
| CHEMBL5542596 | — | — | 1 | 7.81 |
| CHEMBL5555032 | — | — | 1 | 7.45 |
| CHEMBL5559910 | — | — | 1 | 7.35 |
| CHEMBL5560369 | — | — | 1 | 7.32 |
| CHEMBL5557141 | — | — | 1 | 7.30 |
| CHEMBL5561202 | — | — | 1 | 7.27 |
| CHEMBL516312 | — | — | 1 | 7.24 |
| CHEMBL5556790 | — | — | 1 | 7.22 |
| CHEMBL5561763 | — | — | 1 | 7.13 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.11 |
| CHEMBL5566377 | — | — | 1 | 7.09 |
| CHEMBL5564289 | — | — | 1 | 7.01 |
| CHEMBL5561927 | — | — | 1 | 6.98 |
| CHEMBL5566931 | — | — | 1 | 6.93 |
| CHEMBL5542834 | — | — | 1 | 6.81 |
| CHEMBL5556067 | — | — | 1 | 6.81 |
| CHEMBL5517717 | — | — | 1 | 6.80 |
| CHEMBL5560803 | — | — | 1 | 6.65 |
| CHEMBL4452939 | — | — | 1 | 6.53 |
| CHEMBL5518125 | — | — | 1 | 6.39 |
| CHEMBL5567875 | — | — | 1 | - |
| CHEMBL5517817 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439128 | — | IC50 | = | 7.57 | nM | 8.12 |
| CHEMBL5557266 | — | IC50 | = | 9.38 | nM | 8.03 |
| CHEMBL5564665 | — | IC50 | = | 11.19 | nM | 7.95 |
| CHEMBL5560434 | — | IC50 | = | 13.19 | nM | 7.88 |
| CHEMBL5542596 | — | IC50 | = | 15.33 | nM | 7.81 |
| CHEMBL5555032 | — | IC50 | = | 35.8 | nM | 7.45 |
| CHEMBL5559910 | — | IC50 | = | 44.4 | nM | 7.35 |
| CHEMBL5560369 | — | IC50 | = | 48.41 | nM | 7.32 |
| CHEMBL5557141 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5561202 | — | IC50 | = | 53.62 | nM | 7.27 |
| CHEMBL516312 | — | IC50 | = | 57.81 | nM | 7.24 |
| CHEMBL5556790 | — | IC50 | = | 59.67 | nM | 7.22 |
| CHEMBL5561763 | — | IC50 | = | 74.68 | nM | 7.13 |
| CHEMBL535 | SUNITINIB | IC50 | = | 76.86 | nM | 7.11 |
| CHEMBL5566377 | — | IC50 | = | 81.68 | nM | 7.09 |
| CHEMBL5564289 | — | IC50 | = | 97.2 | nM | 7.01 |
| CHEMBL5561927 | — | IC50 | = | 103.96 | nM | 6.98 |
| CHEMBL5566931 | — | IC50 | = | 118.68 | nM | 6.93 |
| CHEMBL5542834 | — | IC50 | = | 155.33 | nM | 6.81 |
| CHEMBL5556067 | — | IC50 | = | 154.77 | nM | 6.81 |
| CHEMBL5517717 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5560803 | — | IC50 | = | 225.14 | nM | 6.65 |
| CHEMBL4452939 | — | IC50 | = | 295.6 | nM | 6.53 |
| CHEMBL5518125 | — | IC50 | = | 406.03 | nM | 6.39 |
| CHEMBL5567875 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5517817 | — | IC50 | > | 500.0 | nM | - |