Assay Detail
Binding
CHEMBL5141600
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal human recombinant PKMYT1 (76 to 362 residues) expressed in Escherichia coli (DE3) RIL preincubated with compound for 15 mins in presence of ATP followed by 1 hr incubation by ADP-glo luminescence assay
38
Total Activities
38
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 |
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 | 38 | 7.36 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5172086 | — | — | 1 | 8.40 |
| CHEMBL5198360 | — | — | 1 | 8.40 |
| CHEMBL5191665 | — | — | 1 | 8.30 |
| CHEMBL5195417 | — | — | 1 | 8.30 |
| CHEMBL5199806 | — | — | 1 | 8.30 |
| CHEMBL5184178 | — | — | 1 | 8.30 |
| CHEMBL5187022 | — | — | 1 | 8.30 |
| CHEMBL5196095 | — | — | 1 | 8.22 |
| CHEMBL5176413 | — | — | 1 | 8.10 |
| CHEMBL5177087 | — | — | 1 | 8.10 |
| CHEMBL5202826 | — | — | 1 | 8.10 |
| CHEMBL5193896 | — | — | 1 | 8.00 |
| CHEMBL5202444 | — | — | 1 | 8.00 |
| CHEMBL5184635 | — | — | 1 | 7.96 |
| CHEMBL5203261 | — | — | 1 | 7.92 |
| CHEMBL5196592 | — | — | 1 | 7.54 |
| CHEMBL5181291 | — | — | 1 | 7.28 |
| CHEMBL3321809 | — | — | 1 | 7.17 |
| CHEMBL5199564 | — | — | 1 | 6.74 |
| CHEMBL3321807 | — | — | 1 | 6.43 |
| CHEMBL5182326 | — | — | 1 | 6.16 |
| CHEMBL5175758 | — | — | 1 | 5.92 |
| CHEMBL5183951 | — | — | 1 | 5.62 |
| CHEMBL5204618 | — | — | 1 | 5.39 |
| CHEMBL5208771 | — | — | 1 | 5.28 |
| CHEMBL5208905 | — | — | 1 | 5.08 |
| CHEMBL5179836 | — | — | 1 | - |
| CHEMBL5186220 | — | — | 1 | - |
| CHEMBL5170848 | — | — | 1 | - |
| CHEMBL5185146 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5172086 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5198360 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5195417 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5199806 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5184178 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5187022 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5191665 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5196095 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5176413 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5177087 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5202826 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5193896 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5202444 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5184635 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5203261 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5196592 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5181291 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3321809 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5199564 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL3321807 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5182326 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5175758 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5183951 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5204618 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5208771 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5208905 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL3321800 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5189665 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5180729 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5208886 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5190822 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5169345 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5171366 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5181222 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5185146 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5170848 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5186220 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5179836 | — | IC50 | > | 20000.0 | nM | - |