Assay Detail
Binding
CHEMBL3804232
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Inhibition of PKCtheta in human Jurkat cells after overnight incubation by luminescence analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKCθ inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.51 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3798011 | — | — | 1 | 7.96 |
| CHEMBL3798679 | — | — | 1 | 7.80 |
| CHEMBL3800310 | — | — | 1 | 6.77 |
| CHEMBL3800116 | — | — | 1 | - |
| CHEMBL3799399 | — | — | 1 | - |
| CHEMBL3798787 | — | — | 1 | - |
| CHEMBL3798933 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3798011 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3798679 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3800310 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3800116 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3799399 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3798787 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3798933 | — | IC50 | > | 1000.0 | nM | - |