Assay Detail
Binding
CHEMBL4370498
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Inhibition of recombinant human full length PKCtheta using biotin-labelled STK substrate-1 as substrate after 60 mins by fluorescence assay
19
Total Activities
19
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
Discovery of 2,4-diamino-5-cyanopyrimidine derivatives as protein kinase C theta inhibitors with mitigated time-dependent drug-drug interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 9.12 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4578497 | — | — | 1 | 10.00 |
| CHEMBL4547465 | — | — | 1 | 9.64 |
| CHEMBL4540382 | — | — | 1 | 9.42 |
| CHEMBL4580751 | — | — | 1 | 9.38 |
| CHEMBL4575526 | — | — | 1 | 9.36 |
| CHEMBL4524977 | — | — | 1 | 9.34 |
| CHEMBL4594002 | — | — | 1 | 9.24 |
| CHEMBL4439095 | — | — | 1 | 9.23 |
| CHEMBL4529215 | — | — | 1 | 9.18 |
| CHEMBL4526554 | — | — | 1 | 9.15 |
| CHEMBL4466775 | — | — | 1 | 9.03 |
| CHEMBL4464921 | — | — | 1 | 8.85 |
| CHEMBL4585918 | — | — | 1 | 8.72 |
| CHEMBL4441229 | — | — | 1 | 8.72 |
| CHEMBL4592349 | — | — | 1 | 7.50 |
| CHEMBL4447795 | — | — | 1 | - |
| CHEMBL4583637 | — | — | 1 | - |
| CHEMBL4545726 | — | — | 1 | - |
| CHEMBL4455647 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4578497 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4547465 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL4540382 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4580751 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL4575526 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL4524977 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL4594002 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4439095 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4529215 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL4526554 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4466775 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4464921 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4585918 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4441229 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4592349 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4447795 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4583637 | — | IC50 | - | — | - | |
| CHEMBL4545726 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4455647 | — | IC50 | < | 1.0 | nM | - |