Assay Detail
Binding
CHEMBL4674513
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Inhibition of GLK (unknown origin) by alphascreen assay
45
Total Activities
44
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
Mitogen-activated protein kinase kinase kinase kinase 3 (CHEMBL5432) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 6.69 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4749141 | — | — | 1 | 8.52 |
| CHEMBL4762312 | — | — | 1 | 8.30 |
| CHEMBL4753188 | — | — | 1 | 7.92 |
| CHEMBL4793665 | — | — | 1 | 7.77 |
| CHEMBL4782885 | — | — | 1 | 7.75 |
| CHEMBL4568440 | — | — | 2 | 7.62 |
| CHEMBL4790577 | — | — | 1 | 7.51 |
| CHEMBL4788727 | — | — | 1 | 7.48 |
| CHEMBL4785602 | — | — | 1 | 7.46 |
| CHEMBL518323 | — | — | 1 | 7.41 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.31 |
| CHEMBL4757394 | — | — | 1 | 7.13 |
| CHEMBL4790293 | — | — | 1 | 7.12 |
| CHEMBL4761177 | — | — | 1 | 7.11 |
| CHEMBL4742776 | — | — | 1 | 7.11 |
| CHEMBL4755070 | — | — | 1 | 7.06 |
| CHEMBL4757177 | — | — | 1 | 6.96 |
| CHEMBL4782953 | — | — | 1 | 6.92 |
| CHEMBL4744805 | — | — | 1 | 6.80 |
| CHEMBL4751159 | — | — | 1 | 6.75 |
| CHEMBL4778070 | — | — | 1 | 6.75 |
| CHEMBL4780336 | — | — | 1 | 6.72 |
| CHEMBL4757014 | — | — | 1 | 6.71 |
| CHEMBL4782872 | — | — | 1 | 6.70 |
| CHEMBL4743396 | — | — | 1 | 6.51 |
| CHEMBL4741426 | — | — | 1 | 6.48 |
| CHEMBL4788337 | — | — | 1 | 6.48 |
| CHEMBL4793638 | — | — | 1 | 6.29 |
| CHEMBL4749926 | — | — | 1 | 6.25 |
| CHEMBL1825141 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4749141 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4762312 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4753188 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4793665 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4782885 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4568440 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4790577 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4788727 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4785602 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL518323 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4757394 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4790293 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4742776 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4761177 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4755070 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4757177 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4782953 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4744805 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4751159 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4778070 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4780336 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4757014 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4782872 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4743396 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4741426 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4788337 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4793638 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4749926 | — | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL1825141 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4568440 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL4785806 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4800136 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4787335 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4755176 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4786008 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4741147 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4794231 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4741011 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4798428 | — | IC50 | = | 2135.0 | nM | 5.67 |
| CHEMBL4760886 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4749627 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4746702 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4779709 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4787817 | — | IC50 | > | 10000.0 | nM | - |