Assay Detail
Binding
CHEMBL5588046
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged PKMYT1 (75 to 362 residues) expressed in insect cells using GTDEGIYDVPLLG as substrate preincubated for 15 mins followed by substrate and ATP addition and measured after 1 hr by ADP-Glo kinase assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Insect cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (CHEMBL3984) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Drug Design of 2-Amino-[1,1'-biphenyl]-3-carboxamide Derivatives as Selective PKMYT1 Inhibitors for the Treatment of <i>CCNE1</i>-Amplified Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.62 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5199076 | LUNRESERTIB | 2.0 | 1 | 8.08 |
| CHEMBL5598020 | — | — | 1 | 7.78 |
| CHEMBL5597456 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5199076 | LUNRESERTIB | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5598020 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL5597456 | — | IC50 | = | 100.8 | nM | 7.00 |