Assay Detail
Binding
CHEMBL4674512
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GLK (unknown origin) transfected in human 293T cells co-transfected with GFP-fused PKCtheta assessed as reduction in PKCtheta phosphorylation by ELISA
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| 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 | 18 | 6.25 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4793665 | — | — | 1 | 7.11 |
| CHEMBL4761177 | — | — | 1 | 6.59 |
| CHEMBL4749141 | — | — | 1 | 6.56 |
| CHEMBL4753188 | — | — | 1 | 6.31 |
| CHEMBL4785602 | — | — | 1 | 6.19 |
| CHEMBL4568440 | — | — | 2 | 6.00 |
| CHEMBL4762312 | — | — | 1 | 5.91 |
| CHEMBL4782885 | — | — | 1 | 5.85 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.77 |
| CHEMBL518323 | — | — | 1 | - |
| CHEMBL4744805 | — | — | 1 | - |
| CHEMBL4779709 | — | — | 1 | - |
| CHEMBL4787817 | — | — | 1 | - |
| CHEMBL4741011 | — | — | 1 | - |
| CHEMBL4794231 | — | — | 1 | - |
| CHEMBL4749627 | — | — | 1 | - |
| CHEMBL1825141 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4793665 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4761177 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL4749141 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL4753188 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4785602 | — | IC50 | = | 645.0 | nM | 6.19 |
| CHEMBL4568440 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4762312 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4782885 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1825141 | — | IC50 | - | — | - | |
| CHEMBL4568440 | — | IC50 | - | — | - | |
| CHEMBL4749627 | — | IC50 | - | — | - | |
| CHEMBL4794231 | — | IC50 | - | — | - | |
| CHEMBL4787817 | — | IC50 | - | — | - | |
| CHEMBL4779709 | — | IC50 | - | — | - | |
| CHEMBL4744805 | — | IC50 | - | — | - | |
| CHEMBL4741011 | — | IC50 | - | — | - | |
| CHEMBL518323 | — | IC50 | - | — | - |