Assay Detail
Binding
CHEMBL4619369
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human PKCzeta using biotin-KKKKRFSFKKSFK substrate and ATP incubated for 30 mins by TR-FRET method
39
Total Activities
39
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 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ζ Inhibitors with Fragment-Merging Strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.29 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4635482 | — | — | 1 | 10.00 |
| CHEMBL4636488 | — | — | 1 | 9.70 |
| CHEMBL4646995 | — | — | 1 | 9.30 |
| CHEMBL4644939 | — | — | 1 | 9.22 |
| CHEMBL4636337 | — | — | 1 | 9.10 |
| CHEMBL4632523 | — | — | 1 | 9.05 |
| CHEMBL4643553 | — | — | 1 | 8.96 |
| CHEMBL4642166 | — | — | 1 | 8.85 |
| CHEMBL4637452 | — | — | 1 | 8.85 |
| CHEMBL4647780 | — | — | 1 | 8.47 |
| CHEMBL4643470 | — | — | 1 | 8.39 |
| CHEMBL4641918 | — | — | 1 | 8.19 |
| CHEMBL4632384 | — | — | 1 | 8.01 |
| CHEMBL4642061 | — | — | 1 | 7.89 |
| CHEMBL4644763 | — | — | 1 | 7.89 |
| CHEMBL4634517 | — | — | 1 | 7.82 |
| CHEMBL4645728 | — | — | 1 | 7.48 |
| CHEMBL4641607 | — | — | 1 | 7.46 |
| CHEMBL4648006 | — | — | 1 | 7.27 |
| CHEMBL4646074 | — | — | 1 | 6.96 |
| CHEMBL4639268 | — | — | 1 | 6.85 |
| CHEMBL4641149 | — | — | 1 | 6.85 |
| CHEMBL4633764 | — | — | 1 | 6.83 |
| CHEMBL4645229 | — | — | 1 | 6.82 |
| CHEMBL4640042 | — | — | 1 | 6.79 |
| CHEMBL4638383 | — | — | 1 | 6.49 |
| CHEMBL4641174 | — | — | 1 | 6.45 |
| CHEMBL4644160 | — | — | 1 | 6.22 |
| CHEMBL4644798 | — | — | 1 | 6.20 |
| CHEMBL4649466 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4635482 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4636488 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4646995 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4644939 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4636337 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4632523 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4643553 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4642166 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4637452 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4647780 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4643470 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4641918 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4632384 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4642061 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4644763 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4634517 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL4645728 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4641607 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4648006 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4646074 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4641149 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4639268 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4633764 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL4645229 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4640042 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL4638383 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL4641174 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL4644160 | — | IC50 | = | 604.0 | nM | 6.22 |
| CHEMBL4644798 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL4649466 | — | IC50 | = | 1014.0 | nM | 5.99 |
| CHEMBL4633447 | — | IC50 | = | 1074.0 | nM | 5.97 |
| CHEMBL4649829 | — | IC50 | = | 1253.0 | nM | 5.90 |
| CHEMBL4634587 | — | IC50 | = | 1394.0 | nM | 5.86 |
| CHEMBL4633862 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4648633 | — | IC50 | = | 3638.0 | nM | 5.44 |
| CHEMBL4645167 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4637961 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4633319 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL4634715 | — | IC50 | > | 40000.0 | nM | - |