Assay Detail
Binding
CHEMBL5629602
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Inhibition of PKC alpha (unknown origin) in presence of 1 mM ATP
33
Total Activities
33
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 a novel series of selective macrocyclic PKCTheta inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 5.91 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 7.70 |
| CHEMBL5631765 | — | — | 1 | 6.72 |
| CHEMBL3798011 | — | — | 1 | 6.36 |
| CHEMBL5632236 | — | — | 1 | 6.31 |
| CHEMBL5633664 | — | — | 1 | 6.26 |
| CHEMBL5631904 | — | — | 1 | 6.26 |
| CHEMBL5631570 | — | — | 1 | 6.21 |
| CHEMBL5631412 | — | — | 1 | 6.17 |
| CHEMBL5633180 | — | — | 1 | 6.10 |
| CHEMBL5632070 | — | — | 1 | 6.08 |
| CHEMBL5631499 | — | — | 1 | 6.03 |
| CHEMBL5632134 | — | — | 1 | 6.03 |
| CHEMBL5633970 | — | — | 1 | 5.96 |
| CHEMBL5632086 | — | — | 1 | 5.66 |
| CHEMBL5632287 | — | — | 1 | 5.66 |
| CHEMBL5631314 | — | — | 1 | 5.43 |
| CHEMBL5631319 | — | — | 1 | 5.32 |
| CHEMBL5633898 | — | — | 1 | 5.22 |
| CHEMBL5631838 | — | — | 1 | 5.19 |
| CHEMBL5633148 | — | — | 1 | 5.18 |
| CHEMBL5632103 | — | — | 1 | 5.17 |
| CHEMBL5631688 | — | — | 1 | 5.10 |
| CHEMBL5632327 | — | — | 1 | - |
| CHEMBL5633390 | — | — | 1 | - |
| CHEMBL5633746 | — | — | 1 | - |
| CHEMBL5633314 | — | — | 1 | - |
| CHEMBL5631515 | — | — | 1 | - |
| CHEMBL5633500 | — | — | 1 | - |
| CHEMBL5632646 | — | — | 1 | - |
| CHEMBL5631811 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5631765 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3798011 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL5632236 | — | IC50 | = | 487.0 | nM | 6.31 |
| CHEMBL5633664 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5631904 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5631570 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5631412 | — | IC50 | = | 679.0 | nM | 6.17 |
| CHEMBL5633180 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL5632070 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL5631499 | — | IC50 | = | 934.0 | nM | 6.03 |
| CHEMBL5632134 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5633970 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5632086 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5632287 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5631314 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL5631319 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5633898 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5631838 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL5633148 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5632103 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5631688 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL5632327 | — | IC50 | - | — | - | |
| CHEMBL5633390 | — | IC50 | - | — | - | |
| CHEMBL5633746 | — | IC50 | - | — | - | |
| CHEMBL5633314 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5631515 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5633500 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5632646 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5631811 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5631971 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5631596 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5633916 | — | IC50 | > | 10000.0 | nM | - |