Assay Detail
Binding
CHEMBL5371121
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CDK2 pretreated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins in presence of 10 uM ATP by radiometric Hot-SpotSM Kinase assay
5
Total Activities
5
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
Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.37 | 8.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077071 | — | — | 1 | 8.61 |
| CHEMBL5399420 | — | — | 1 | 7.64 |
| CHEMBL5401158 | — | — | 1 | 7.01 |
| CHEMBL5435746 | — | — | 1 | 6.87 |
| CHEMBL5415967 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077071 | — | IC50 | = | 2.47 | nM | 8.61 |
| CHEMBL5399420 | — | IC50 | = | 23.03 | nM | 7.64 |
| CHEMBL5401158 | — | IC50 | = | 98.31 | nM | 7.01 |
| CHEMBL5435746 | — | IC50 | = | 135.01 | nM | 6.87 |
| CHEMBL5415967 | — | IC50 | = | 193.21 | nM | 6.71 |