Assay Detail
Binding
CHEMBL5141607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal recombinant PKMYT1 (76 to 362 residues) in CCNE1 amplified human FU-OV-1 cells assessed as phosphorylation of CDK1 at Thr14 incubated for 2 hrs by AlphaLisa assay
36
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | FU-OV-1 |
| 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
Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.99 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5190904 | — | — | 1 | 8.30 |
| CHEMBL5174072 | — | — | 1 | 8.15 |
| CHEMBL5199076 | LUNRESERTIB | 2.0 | 1 | 7.85 |
| CHEMBL5196713 | — | — | 1 | 7.77 |
| CHEMBL5181222 | — | — | 2 | 7.70 |
| CHEMBL5174684 | — | — | 1 | 7.62 |
| CHEMBL5200849 | — | — | 1 | 7.60 |
| CHEMBL5179743 | — | — | 1 | 7.58 |
| CHEMBL5204520 | — | — | 1 | 7.47 |
| CHEMBL5199806 | — | — | 1 | 7.47 |
| CHEMBL5198360 | — | — | 1 | 7.44 |
| CHEMBL5201803 | — | — | 1 | 7.38 |
| CHEMBL5182071 | — | — | 1 | 7.30 |
| CHEMBL5191665 | — | — | 1 | 7.16 |
| CHEMBL5200005 | — | — | 1 | 7.14 |
| CHEMBL5169330 | — | — | 1 | 6.97 |
| CHEMBL5169345 | — | — | 1 | 6.92 |
| CHEMBL5202826 | — | — | 1 | 6.89 |
| CHEMBL5172086 | — | — | 1 | 6.77 |
| CHEMBL5186220 | — | — | 1 | 6.72 |
| CHEMBL5187022 | — | — | 1 | 6.70 |
| CHEMBL5184178 | — | — | 1 | 6.52 |
| CHEMBL5196095 | — | — | 1 | 6.50 |
| CHEMBL5185146 | — | — | 1 | 6.44 |
| CHEMBL5203261 | — | — | 1 | 6.44 |
| CHEMBL5202444 | — | — | 1 | 6.42 |
| CHEMBL5175722 | — | — | 1 | 6.31 |
| CHEMBL5190822 | — | — | 1 | 6.26 |
| CHEMBL5184635 | — | — | 1 | 6.25 |
| CHEMBL5208938 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5190904 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5174072 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5199076 | LUNRESERTIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5196713 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5181222 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5181222 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5174684 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5200849 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5179743 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5204520 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5199806 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5198360 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5201803 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5182071 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5191665 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5200005 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5169330 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5169345 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5202826 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5172086 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5186220 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5187022 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5184178 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5196095 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5185146 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5203261 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5202444 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5175722 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL5190822 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5184635 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5208938 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL5177087 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5176413 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL5195417 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL3321809 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL5193896 | — | IC50 | > | 3000.0 | nM | - |