Assay Detail
Binding
CHEMBL4017958
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal FLAG-tagged PKCtheta (unknown origin) expressed in baculovirus expression system using fluorescein-PKC as substrate preincubated for 5 mins followed by substrate addition measured after 60 mins in presence of ATP by Lathascreen TR-FRET assay
11
Total Activities
11
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
Practical application of 3-substituted-2,6-difluoropyridines in drug discovery: Facile synthesis of novel protein kinase C theta inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.19 | 10.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4082370 | — | — | 1 | 10.07 |
| CHEMBL4065996 | — | — | 1 | 9.74 |
| CHEMBL4092652 | — | — | 1 | 9.06 |
| CHEMBL4100381 | — | — | 1 | 8.20 |
| CHEMBL4093591 | — | — | 1 | 8.17 |
| CHEMBL4099368 | — | — | 1 | 7.85 |
| CHEMBL4074629 | — | — | 1 | 7.75 |
| CHEMBL4101327 | — | — | 1 | 7.48 |
| CHEMBL4071874 | — | — | 1 | 7.00 |
| CHEMBL4063243 | — | — | 1 | 6.60 |
| CHEMBL4084895 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4082370 | — | IC50 | = | 0.086 | nM | 10.07 |
| CHEMBL4065996 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4092652 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL4100381 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4093591 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4099368 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4074629 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4101327 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4071874 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4063243 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4084895 | — | IC50 | > | 1000.0 | nM | - |