Assay Detail
Binding
CHEMBL4233137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-[3',6'-dihydroxy-3-oxo-3H-spiro(2-benzofuran-1,9'-xanthen)-5-yl]-N'-[2-(4-{4-[N-(2-chloro-6-methylphenyl)-5-carboxamido]-thiazol-2-yl})-amino-2-methyl-pyrimid-6-yl)piperazinyl]-ethyl]thiourea binding to human PKMYT1 kinase doamin expressed in Escherichia coli BL21 after 120 mins by fluorescence polarization asay
36
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 6.21 | 8.70 |
| IC50 | 18 | 5.92 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49120 | PD-0166285 | 1.0 | 2 | 8.70 |
| CHEMBL106772 | — | — | 2 | 8.09 |
| CHEMBL5416410 | DASATINIB | 4.0 | 2 | 7.14 |
| CHEMBL587965 | — | — | 2 | 6.98 |
| CHEMBL545839 | — | — | 2 | 6.75 |
| CHEMBL582038 | — | — | 2 | 6.70 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 2 | 6.52 |
| CHEMBL4241193 | — | — | 2 | 6.33 |
| CHEMBL218088 | GW435821X | — | 2 | 6.28 |
| CHEMBL237347 | GW559768X | — | 2 | 6.23 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 2 | 6.22 |
| CHEMBL251549 | GW782612X | — | 2 | 5.80 |
| CHEMBL574058 | — | — | 2 | 5.57 |
| CHEMBL217092 | SARACATINIB | 3.0 | 2 | 5.28 |
| CHEMBL230911 | GSK-625137A | — | 2 | 5.24 |
| CHEMBL4246519 | — | — | 2 | 5.21 |
| CHEMBL579952 | — | — | 2 | 4.83 |
| CHEMBL7917 | TYRPHOSTIN AG-1478 | — | 2 | 4.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49120 | PD-0166285 | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL106772 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL49120 | PD-0166285 | IC50 | = | 31.1 | nM | 7.51 |
| CHEMBL106772 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5416410 | DASATINIB | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL587965 | — | Ki | = | 104.3 | nM | 6.98 |
| CHEMBL587965 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL545839 | — | Ki | = | 179.9 | nM | 6.75 |
| CHEMBL582038 | — | Ki | = | 200.9 | nM | 6.70 |
| CHEMBL5416410 | DASATINIB | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL288441 | BOSUTINIB | Ki | = | 304.0 | nM | 6.52 |
| CHEMBL582038 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL545839 | — | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL4241193 | — | Ki | = | 461.9 | nM | 6.33 |
| CHEMBL218088 | GW435821X | Ki | = | 521.5 | nM | 6.28 |
| CHEMBL237347 | GW559768X | Ki | = | 588.0 | nM | 6.23 |
| CHEMBL1976040 | ADAVOSERTIB | Ki | = | 600.9 | nM | 6.22 |
| CHEMBL288441 | BOSUTINIB | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL237347 | GW559768X | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL4241193 | — | IC50 | = | 787.0 | nM | 6.10 |
| CHEMBL218088 | GW435821X | IC50 | = | 876.0 | nM | 6.06 |
| CHEMBL1976040 | ADAVOSERTIB | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL251549 | GW782612X | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL251549 | GW782612X | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL574058 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL217092 | SARACATINIB | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL230911 | GSK-625137A | Ki | = | 5810.0 | nM | 5.24 |
| CHEMBL4246519 | — | Ki | = | 6150.0 | nM | 5.21 |
| CHEMBL4246519 | — | IC50 | = | 9430.0 | nM | 5.03 |
| CHEMBL217092 | SARACATINIB | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL230911 | GSK-625137A | IC50 | = | 11430.0 | nM | 4.94 |
| CHEMBL574058 | — | Ki | = | 13500.0 | nM | 4.87 |
| CHEMBL579952 | — | Ki | = | 14740.0 | nM | 4.83 |
| CHEMBL579952 | — | IC50 | = | 18880.0 | nM | 4.72 |
| CHEMBL7917 | TYRPHOSTIN AG-1478 | Ki | = | 26200.0 | nM | 4.58 |
| CHEMBL7917 | TYRPHOSTIN AG-1478 | IC50 | = | 55000.0 | nM | 4.26 |