Assay Detail
Binding
CHEMBL2216290
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Inhibition of N-terminal 6His-tagged full length human recombinant STK33 using myelin basic protein as substrate incubated for 15 mins before initiation of kinase reaction measured after 1 hr by ADP-glo assay
29
Total Activities
29
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 |
Publication
A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.57 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2203524 | — | — | 1 | 8.15 |
| CHEMBL2203525 | — | — | 1 | 7.96 |
| CHEMBL2204239 | — | — | 1 | 7.85 |
| CHEMBL2203528 | — | — | 1 | 7.12 |
| CHEMBL2204241 | — | — | 1 | 7.11 |
| CHEMBL2204238 | — | — | 1 | 6.96 |
| CHEMBL2203530 | — | — | 1 | 6.82 |
| CHEMBL2204235 | — | — | 1 | 6.80 |
| CHEMBL1992679 | — | — | 1 | 6.77 |
| CHEMBL2204237 | — | — | 1 | 6.60 |
| CHEMBL2204240 | — | — | 1 | 6.57 |
| CHEMBL1543343 | — | — | 1 | 6.55 |
| CHEMBL2203531 | — | — | 1 | 6.52 |
| CHEMBL2203526 | — | — | 1 | 6.42 |
| CHEMBL2204236 | — | — | 1 | 6.39 |
| CHEMBL2203527 | — | — | 1 | 6.28 |
| CHEMBL2203529 | — | — | 1 | 6.24 |
| CHEMBL2203532 | — | — | 1 | 6.01 |
| CHEMBL2204234 | — | — | 1 | 5.80 |
| CHEMBL2203536 | — | — | 1 | 5.80 |
| CHEMBL2204233 | — | — | 1 | 5.80 |
| CHEMBL2204232 | — | — | 1 | 5.40 |
| CHEMBL2204231 | — | — | 1 | 5.14 |
| CHEMBL2204230 | — | — | 1 | - |
| CHEMBL2203533 | — | — | 1 | - |
| CHEMBL2203534 | — | — | 1 | - |
| CHEMBL2203535 | — | — | 1 | - |
| CHEMBL2204228 | — | — | 1 | - |
| CHEMBL2204229 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2203524 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2203525 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2204239 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2203528 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2204241 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2204238 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2203530 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2204235 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1992679 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2204237 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2204240 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1543343 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2203531 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2203526 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2204236 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2203527 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL2203529 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2203532 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL2204234 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2203536 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2204233 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2204232 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2204231 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL2204230 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2203533 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2203534 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2203535 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2204228 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2204229 | — | IC50 | > | 10000.0 | nM | - |