Assay Detail
Binding
CHEMBL4233136
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Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay
36
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Identification of PKMYT1 inhibitors by screening the GSK published protein kinase inhibitor set I and II.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.35 | 9.30 |
| IC50 | 18 | 6.32 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 2 | 9.30 |
| CHEMBL49120 | PD-0166285 | 1.0 | 2 | 9.10 |
| CHEMBL106772 | — | — | 2 | 8.64 |
| CHEMBL574058 | — | — | 2 | 7.98 |
| CHEMBL587965 | — | — | 2 | 7.96 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 2 | 7.90 |
| CHEMBL237347 | GW559768X | — | 2 | 7.77 |
| CHEMBL545839 | — | — | 2 | 7.59 |
| CHEMBL4241193 | — | — | 2 | 7.49 |
| CHEMBL217092 | SARACATINIB | 3.0 | 2 | 7.40 |
| CHEMBL251549 | GW782612X | — | 2 | 7.32 |
| CHEMBL4246519 | — | — | 2 | 7.29 |
| CHEMBL582038 | — | — | 2 | 7.17 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 2 | 6.33 |
| CHEMBL579952 | — | — | 2 | 6.14 |
| CHEMBL218088 | GW435821X | — | 2 | 5.86 |
| CHEMBL7917 | TYRPHOSTIN AG-1478 | — | 2 | 5.73 |
| CHEMBL230911 | GSK-625137A | — | 2 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL49120 | PD-0166285 | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL106772 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL5416410 | DASATINIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL49120 | PD-0166285 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL574058 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL587965 | — | Ki | = | 10.94 | nM | 7.96 |
| CHEMBL288441 | BOSUTINIB | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL237347 | GW559768X | Ki | = | 16.85 | nM | 7.77 |
| CHEMBL106772 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL545839 | — | Ki | = | 25.68 | nM | 7.59 |
| CHEMBL4241193 | — | Ki | = | 32.4 | nM | 7.49 |
| CHEMBL217092 | SARACATINIB | Ki | = | 39.8 | nM | 7.40 |
| CHEMBL251549 | GW782612X | Ki | = | 48.47 | nM | 7.32 |
| CHEMBL4246519 | — | Ki | = | 51.73 | nM | 7.29 |
| CHEMBL582038 | — | Ki | = | 67.19 | nM | 7.17 |
| CHEMBL574058 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL587965 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL288441 | BOSUTINIB | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL237347 | GW559768X | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL545839 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4241193 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL217092 | SARACATINIB | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL1976040 | ADAVOSERTIB | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL251549 | GW782612X | IC50 | = | 509.0 | nM | 6.29 |
| CHEMBL4246519 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL582038 | — | IC50 | = | 706.0 | nM | 6.15 |
| CHEMBL579952 | — | Ki | = | 720.2 | nM | 6.14 |
| CHEMBL218088 | GW435821X | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL7917 | TYRPHOSTIN AG-1478 | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL1976040 | ADAVOSERTIB | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL230911 | GSK-625137A | Ki | = | 5520.0 | nM | 5.26 |
| CHEMBL579952 | — | IC50 | = | 7560.0 | nM | 5.12 |
| CHEMBL218088 | GW435821X | IC50 | = | 14510.0 | nM | 4.84 |
| CHEMBL7917 | TYRPHOSTIN AG-1478 | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL230911 | GSK-625137A | IC50 | = | 57990.0 | nM | 4.24 |