Assay Detail
Binding
CHEMBL4831022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NEK2 (unknown origin) using 5' FAM-KKLNRTLSVA-COOH peptide as a substrate in the presence of ATP incubated for 60 mins by microfluidics assay
30
Total Activities
30
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 |
Target
Serine/threonine-protein kinase Nek2 (CHEMBL3835) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.88 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4860697 | — | — | 1 | 8.49 |
| CHEMBL4863351 | — | — | 1 | 5.89 |
| CHEMBL4868026 | — | — | 1 | 5.63 |
| CHEMBL4847680 | — | — | 1 | 4.70 |
| CHEMBL4870662 | — | — | 1 | 4.70 |
| CHEMBL4878572 | — | — | 1 | - |
| CHEMBL4868818 | — | — | 1 | - |
| CHEMBL4855716 | — | — | 1 | - |
| CHEMBL4874305 | — | — | 1 | - |
| CHEMBL4872048 | — | — | 1 | - |
| CHEMBL4849272 | — | — | 1 | - |
| CHEMBL4860913 | — | — | 1 | - |
| CHEMBL4849959 | — | — | 1 | - |
| CHEMBL4852822 | — | — | 1 | - |
| CHEMBL4863689 | — | — | 1 | - |
| CHEMBL4876014 | — | — | 1 | - |
| CHEMBL4859133 | — | — | 1 | - |
| CHEMBL4867699 | — | — | 1 | - |
| CHEMBL4872616 | — | — | 1 | - |
| CHEMBL4846528 | — | — | 1 | - |
| CHEMBL4852877 | — | — | 1 | - |
| CHEMBL4859180 | — | — | 1 | - |
| CHEMBL4869856 | — | — | 1 | - |
| CHEMBL4879086 | — | — | 1 | - |
| CHEMBL4857928 | — | — | 1 | - |
| CHEMBL4873041 | — | — | 1 | - |
| CHEMBL4863364 | — | — | 1 | - |
| CHEMBL4878277 | — | — | 1 | - |
| CHEMBL4857926 | — | — | 1 | - |
| CHEMBL4877108 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4860697 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4863351 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4868026 | — | IC50 | = | 2350.0 | nM | 5.63 |
| CHEMBL4847680 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4870662 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4878572 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4868818 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4855716 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4874305 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4872048 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4849272 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4860913 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4849959 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4852822 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4863689 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4876014 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4859133 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4867699 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4872616 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4846528 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4852877 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4859180 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4869856 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4879086 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4857928 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4873041 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4863364 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4878277 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4857926 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4877108 | — | IC50 | > | 20000.0 | nM | - |